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[PMID]:28866099
[Au] Autor:Takano M; Kamei H; Nagahiro M; Kawami M; Yumoto R
[Ad] Endereço:Department of Pharmaceutics and Therapeutics, Graduate School of Biomedical & Health Sciences, Hiroshima University, 1-2-3 Kasumi, Minami-ku, Hiroshima 734-8553, Japan. Electronic address: takanom@hiroshima-u.ac.jp.
[Ti] Título:Nicotine transport in lung and non-lung epithelial cells.
[So] Source:Life Sci;188:76-82, 2017 Nov 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIMS: Nicotine is rapidly absorbed from the lung alveoli into systemic circulation during cigarette smoking. However, mechanism underlying nicotine transport in alveolar epithelial cells is not well understood to date. In the present study, we characterized nicotine uptake in lung epithelial cell lines A549 and NCI-H441 and in non-lung epithelial cell lines HepG2 and MCF-7. MATERIALS AND METHODS: Characteristics of [ H]nicotine uptake was studied using these cell lines. KEY FINDINGS: Nicotine uptake in A549 cells occurred in a time- and temperature-dependent manner and showed saturation kinetics, with a Km value of 0.31mM. Treatment with some organic cations such as diphenhydramine and pyrilamine inhibited nicotine uptake, whereas treatment with organic cations such as carnitine and tetraethylammonium did not affect nicotine uptake. Extracellular pH markedly affected nicotine uptake, with high nicotine uptake being observed at high pH up to 11.0. Modulation of intracellular pH with ammonium chloride also affected nicotine uptake. Treatment with valinomycin, a potassium ionophore, did not significantly affect nicotine uptake, indicating that nicotine uptake is an electroneutral process. For comparison, we assessed the characteristics of nicotine uptake in another lung epithelial cell line NCI-H441 and in non-lung epithelial cell lines HepG2 and MCF-7. Interestingly, these cell lines showed similar characteristics of nicotine uptake with respect to pH dependency and inhibition by various organic cations. SIGNIFICANCE: The present findings suggest that a similar or the same pH-dependent transport system is involved in nicotine uptake in these cell lines. A novel molecular mechanism of nicotine transport is proposed.
[Mh] Termos MeSH primário: Transporte Biológico/efeitos dos fármacos
Células Epiteliais/metabolismo
Pulmão/metabolismo
Nicotina/farmacocinética
[Mh] Termos MeSH secundário: Carnitina/farmacologia
Células Cultivadas
Difenidramina/farmacologia
Interações Medicamentosas
Seres Humanos
Concentração de Íons de Hidrogênio
Pirilamina/farmacologia
Temperatura Ambiente
Tetraetilamônio/farmacologia
Fatores de Tempo
Trítio/metabolismo
Valinomicina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
10028-17-8 (Tritium); 2001-95-8 (Valinomycin); 66-40-0 (Tetraethylammonium); 6M3C89ZY6R (Nicotine); 8GTS82S83M (Diphenhydramine); HPE317O9TL (Pyrilamine); S7UI8SM58A (Carnitine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170929
[Lr] Data última revisão:
170929
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170904
[St] Status:MEDLINE


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[PMID]:28436624
[Au] Autor:Zhang L; Chen G; Chen J; He X; Hu X
[Ad] Endereço:Department of Neurology, Sir Run Run Shaw Hospital, Zhejiang University School of Medicine, Hangzhou 310016, China.
[Ti] Título:[Mechanisms of histamine ameliorating memory impairment induced by pentylenetetrazole-kindling epilepsy in rats].
[So] Source:Zhejiang Da Xue Xue Bao Yi Xue Ban;46(1):1-6, 2017 Jan 25.
[Is] ISSN:1008-9292
[Cp] País de publicação:China
[La] Idioma:chi
[Ab] Resumo:To investigate the effects of neuronal histamine on spatial memory acquisition impairment in rats with pentylenetetrazole-kindling epilepsy, and to explore its mechanisms. A subconvulsive dose of pentylenetetrazole (35 mg/kg) was intraperitoneally injected in rats every 48 h to induce chemical kindling until fully kindled. Morris water maze was used to measure the spatial memory acquisition of the rats one week after fully pentylenetetrazole-kindled, and the histamine contents in different brain areas were measured spectrofluorometrically. Different dosages of hitidine (the precursor of histamine), pyrilamine (H1 receptor antagonist), and zolantidine (H2 receptor antagonist) were intraperitoneally injected, and their effects on spatial memory acquisition of the rats were observed. Compared with control group, escape latencies were significantly prolonged on Morris water maze training day 2 and day 3 in pentylenetetrazole-kindling epilepsy rats (all <0.05); and the histamine contents in hippocampus, thalamus and hypothalamus were decreased significantly (all <0.05). Escape latencies were markedly shortened on day 3 by intraperitoneally injected with histidine 500 mg/kg, and on day 2 and day 3 by intraperitoneally injected with histidine 1000 mg/kg in pentylenetetrazole-kindling epilepsy rats (all <0.05). The protection of histidine was reversed by zolantidine (10 and 20 mg/kg), but not by pyrilamine. Neuronal histamine can improve the spatial memory acquisition impairment in rats with pentylenetetrazole-kindling epilepsy, and the activation of H2 receptors is possibly involved in the protective effects of histamine.
[Mh] Termos MeSH primário: Transtornos da Memória/tratamento farmacológico
Receptores Histamínicos H2/efeitos dos fármacos
Receptores Histamínicos H2/fisiologia
Memória Espacial/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Benzotiazóis/farmacologia
Química Encefálica/efeitos dos fármacos
Epilepsia/induzido quimicamente
Epilepsia/complicações
Hipocampo/química
Antagonistas dos Receptores Histamínicos H1/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Histidina/farmacologia
Hipotálamo/química
Excitação Neurológica/fisiologia
Transtornos da Memória/etiologia
Pentilenotetrazol
Fenoxipropanolaminas/farmacologia
Piperidinas/farmacologia
Pirilamina/farmacologia
Ratos
Ratos Sprague-Dawley
Espectrometria de Fluorescência
Tálamo/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzothiazoles); 0 (Histamine H1 Antagonists); 0 (Histamine H2 Antagonists); 0 (Phenoxypropanolamines); 0 (Piperidines); 0 (Receptors, Histamine H2); 4QD397987E (Histidine); HPE317O9TL (Pyrilamine); M1108XAY01 (zolantidine); WM5Z385K7T (Pentylenetetrazole)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170425
[St] Status:MEDLINE


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[PMID]:27904941
[Au] Autor:Fischer L; Lavoranti MI; de Oliveira Borges M; Miksza AF; Sardi NF; Martynhak BJ; Tambeli CH; Parada CA
[Ad] Endereço:Division of Biological Sciences, Department of Physiology, Federal University of Parana, Curitiba, Parana, Brazil. fischer@ufpr.br.
[Ti] Título:TRPA1, substance P, histamine and 5-hydroxytryptamine interact in an interdependent way to induce nociception.
[So] Source:Inflamm Res;66(4):311-322, 2017 Apr.
[Is] ISSN:1420-908X
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Although TRPA1, SP, histamine and 5-hydroxytryptamine (5-HT) have recognized contribution to nociceptive mechanisms, little is known about how they interact with each other to mediate inflammatory pain in vivo. In this study we evaluated whether TRPA1, SP, histamine and 5-HT interact, in an interdependent way, to induce nociception in vivo. METHODS AND RESULTS: The subcutaneous injection of the TRPA1 agonist allyl isothiocyanate (AITC) into the rat's hind paw induced a dose-dependent and short lasting behavioral nociceptive response that was blocked by the co-administration of the TRPA1 antagonist, HC030031, or by the pretreatment with antisense ODN against TRPA1. AITC-induced nociception was significantly decreased by the co-administration of selective antagonists for the NK1 receptor for substance P, the H1 receptor for histamine and the 5-HT receptors for 5-HT. Histamine- or 5-HT-induced nociception was decreased by the pretreatment with antisense ODN against TRPA1. These findings suggest that AITC-induced nociception depends on substance P, histamine and 5-HT, while histamine- or 5-HT-induced nociception depends on TRPA1. Most important, AITC interact in a synergistic way with histamine, 5-HT or substance P, since their combination at non-nociceptive doses induced a nociceptive response much higher than that expected by the sum of the effect of each one alone. This synergistic effect is dependent on the H1, 5-HT receptors. CONCLUSION: Together, these findings suggest a self-sustainable cycle around TRPA1, no matter where the cycle is initiated each step is achieved and even subeffective activation of more than one step results in a synergistic activation of the overall cycle.
[Mh] Termos MeSH primário: Histamina/metabolismo
Dor/metabolismo
Serotonina/metabolismo
Substância P/metabolismo
Canais de Cátion TRPC/metabolismo
[Mh] Termos MeSH secundário: Acetanilidas/farmacologia
Animais
Antagonistas dos Receptores Histamínicos H1/farmacologia
Isotiocianatos
Masculino
Oligonucleotídeos Antissenso/farmacologia
Dor/induzido quimicamente
Piperazinas/farmacologia
Purinas/farmacologia
Pirilamina/farmacologia
Quinuclidinas/farmacologia
Ratos Wistar
Receptor 5-HT1A de Serotonina/metabolismo
Receptores Histamínicos H1/metabolismo
Receptores da Neurocinina-1/metabolismo
Receptores 5-HT3 de Serotonina/metabolismo
Antagonistas da Serotonina/farmacologia
Canal de Cátion TRPA1
Canais de Cátion TRPC/agonistas
Canais de Cátion TRPC/antagonistas & inibidores
Canais de Cátion TRPC/genética
p-Metoxi-N-metilfenetilamina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(4-isopropylphenyl)acetamide); 0 (Acetanilides); 0 (Histamine H1 Antagonists); 0 (Isothiocyanates); 0 (Oligonucleotides, Antisense); 0 (Piperazines); 0 (Purines); 0 (Quinuclidines); 0 (Receptors, Histamine H1); 0 (Receptors, Neurokinin-1); 0 (Receptors, Serotonin, 5-HT3); 0 (Serotonin Antagonists); 0 (TRPA1 Cation Channel); 0 (TRPC Cation Channels); 0 (Trpa1 protein, rat); 112692-38-3 (Receptor, Serotonin, 5-HT1A); 133025-23-7 (WAY 100135); 144425-84-3 (L 703606); 333DO1RDJY (Serotonin); 33507-63-0 (Substance P); 4091-50-3 (p-Methoxy-N-methylphenethylamine); 820484N8I3 (Histamine); BN34FX42G3 (allyl isothiocyanate); HPE317O9TL (Pyrilamine)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161202
[St] Status:MEDLINE
[do] DOI:10.1007/s00011-016-1015-1


  4 / 1723 MEDLINE  
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[PMID]:27831743
[Au] Autor:Ortiz MI
[Ad] Endereço:Área Académica de Medicina del Instituto de Ciencias de la Salud, Universidad Autónoma del Estado de Hidalgo, Pachuca, Hidalgo, México.
[Ti] Título:Synergistic interaction between diclofenac and pyrilamine on nociception, inflammation, and gastric damage in rats.
[So] Source:Can J Physiol Pharmacol;95(1):51-58, 2017 Jan.
[Is] ISSN:1205-7541
[Cp] País de publicação:Canada
[La] Idioma:eng
[Ab] Resumo:Experiments using nonsteroidal anti-inflammatory drugs (NSAIDs) alone have produced limited antinociceptive effects in animal models. For this reason, the number of studies involving the administration of NSAIDs along with an adjuvant drug harboring different mechanisms of action has increased enormously. Here, combinations of diclofenac and pyrilamine were used to determine their influence on nociception (formalin test), inflammation (paw inflammation produced by carrageenan), and gastric damage in rodents. Diclofenac, pyrilamine, or combinations of diclofenac and pyrilamine produced antinociceptive and anti-inflammatory effects in the rat. The systemic administration of diclofenac alone and in combination with pyrilamine produced significant gastric damage. Effective dose (ED) values were determined for each individual drug, and isobolograms were prepared. The theoretical ED values for the antinociceptive (systemic, 35.4 mg/kg; local, 343.4 µg/paw) and the anti-inflammatory (37.9 mg/kg) effects differed significantly from the experimental ED values (systemic antinociception, 18.1 mg/kg; local antinociception, 183.3 µg/paw; anti-inflammation, 10.6 mg/kg). Therefore, it was concluded that the interactions between diclofenac and pyrilamine are synergistic. The data suggest that the diclofenac-pyrilamine combinations can interact at the systemic and local peripheral levels, thereby offering a therapeutic alternative for the clinical management of inflammatory pain.
[Mh] Termos MeSH primário: Diclofenaco/farmacologia
Diclofenaco/uso terapêutico
Inflamação/tratamento farmacológico
Nociceptividade/efeitos dos fármacos
Pirilamina/farmacologia
Pirilamina/uso terapêutico
Estômago/efeitos dos fármacos
Estômago/patologia
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios não Esteroides/efeitos adversos
Anti-Inflamatórios não Esteroides/farmacologia
Anti-Inflamatórios não Esteroides/uso terapêutico
Carragenina
Diclofenaco/efeitos adversos
Relação Dose-Resposta a Droga
Sinergismo Farmacológico
Quimioterapia Combinada/efeitos adversos
Feminino
Inflamação/induzido quimicamente
Destreza Motora/efeitos dos fármacos
Medição da Dor/efeitos dos fármacos
Pirilamina/efeitos adversos
Ratos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 144O8QL0L1 (Diclofenac); 9000-07-1 (Carrageenan); HPE317O9TL (Pyrilamine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170502
[Lr] Data última revisão:
170502
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161111
[St] Status:MEDLINE
[do] DOI:10.1139/cjpp-2016-0306


  5 / 1723 MEDLINE  
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[PMID]:27813503
[Au] Autor:Ortiz MI; Murguía-Cánovas G; Vargas-López LC; Silva R; González-de la Parra M
[Ad] Endereço:Área Académica de Medicina del Instituto de Ciencias de la Salud de la Universidad Autónoma del Estado de Hidalgo, Pachuca, Hidalgo, México. Address: Área Académica de Medicina del Instituto de Ciencias de la Salud, Universidad Autónoma Del Estado de Hidalgo, Eliseo Ramírez Ulloa 400, Colonia Doctor
[Ti] Título:Naproxen, paracetamol and pamabrom versus paracetamol, pyrilamine and pamabrom in primary dysmenorrhea: a randomized, double-blind clinical trial.
[Ti] Título:Naproxeno, paracetamol y pamabrom versus paracetamol, pirilamina y pamabrom en dismenorrea primaria: estudio aleatorizado, doble ciego..
[So] Source:Medwave;16(9):e6587, 2016 Oct 24.
[Is] ISSN:0717-6384
[Cp] País de publicação:Chile
[La] Idioma:spa; eng
[Ab] Resumo:INTRODUCTION: Dysmenorrhea is caused by the discharge of prostaglandins into the uterine tissue; therefore, non-steroidal anti-inflammatory drugs (NSAIDs) are the established initial therapy for dysmenorrhea. Dysmenorrhea therapy may include the administration of drug monotherapy or combination therapy. However, clinical scientific evidence on the efficacy of medications with two or three drugs combined is scarce or nonexistent. OBJECTIVE: To evaluate and compare the efficacy and safety of two oral fixed-dose combinations for the relief of the symptoms of primary dysmenorrhea among Mexican women. One of the combinations is widely used in Mexico (paracetamol, pyrilamine and pamabrom) and the selected comparison was a medication with naproxen sodium, paracetamol and pamabrom based on the pathophysiology of primary dysmenorrhea. METHODS: This was a single-centre, double blind, experimental, parallel group, randomized trial. Female patients with primary dysmenorrhea, older than 17 years and with pain intensity greater than 45 mm on a visual analogue scale, were included. The patients were then randomized to receive tablets with naproxen sodium, paracetamol and pamabrom or tablets with paracetamol, pyrilamine and pamabrom for one menstrual cycle. Patient evaluations of symptomatology and pain intensity were recorded throughout one menstrual period. Descriptive and inferential statistical analyses were utilized. RESULTS: An intention-to-treat population of 91 women, with a mean age of 21.3 ± 3.2 years, received paracetamol, pyrilamine and pamabrom tablets, and 98 participants, with a mean age of 21.0 ± 3.2 years, received naproxen sodium, paracetamol and pamabrom tablets. The participants’ assessments of pain on the Visual Analogue Scale during the menstrual cycle demonstrated a significant reduction in both treatment groups (p<0.05). There is no significant difference in efficacy between both groups (p>0.05). CONCLUSIONS: The results showed that both drug combinations were not different in reducing dysmenorrheic pain. Likewise, both treatments were well tolerated. Therefore, both treatments may be used for the treatment of primary dysmenorrhea.
[Mh] Termos MeSH primário: Acetaminofen/administração & dosagem
Dismenorreia/tratamento farmacológico
Naproxeno/administração & dosagem
Propanolaminas/administração & dosagem
Pirilamina/administração & dosagem
Teofilina/análogos & derivados
[Mh] Termos MeSH secundário: Acetaminofen/efeitos adversos
Adolescente
Analgésicos não Entorpecentes/administração & dosagem
Analgésicos não Entorpecentes/efeitos adversos
Anti-Inflamatórios não Esteroides/administração & dosagem
Anti-Inflamatórios não Esteroides/efeitos adversos
Método Duplo-Cego
Combinação de Medicamentos
Dismenorreia/fisiopatologia
Feminino
Seres Humanos
México
Naproxeno/efeitos adversos
Medição da Dor
Propanolaminas/efeitos adversos
Pirilamina/efeitos adversos
Comprimidos
Teofilina/administração & dosagem
Teofilina/efeitos adversos
Resultado do Tratamento
Adulto Jovem
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Analgesics, Non-Narcotic); 0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Drug Combinations); 0 (Propanolamines); 0 (Tablets); 362O9ITL9D (Acetaminophen); 57Y76R9ATQ (Naproxen); C137DTR5RG (Theophylline); HPE317O9TL (Pyrilamine); UA8U0KJM72 (pamabrom)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170807
[Lr] Data última revisão:
170807
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161105
[St] Status:MEDLINE
[do] DOI:10.5867/medwave.2016.09.6587


  6 / 1723 MEDLINE  
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[PMID]:27342775
[Au] Autor:Yu J; Tang YY; Wang RR; Lou GD; Hu TT; Hou WW; Yue JX; Ohtsu H; Shi LY; Zhang SH; Chen Z
[Ad] Endereço:Department of Pharmacology, Key Laboratory of Medical Neurobiology of the Ministry of Health of China, School of Basic Medical Sciences, Zhejiang University, Hangzhou, 310058, Zhejiang, China.
[Ti] Título:A critical time window for the analgesic effect of central histamine in the partial sciatic ligation model of neuropathic pain.
[So] Source:J Neuroinflammation;13(1):163, 2016 Jun 24.
[Is] ISSN:1742-2094
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: It is known that histamine participates in pain modulation. However, the effect of central histamine on neuropathic pain is not fully understood. Here, we report a critical time window for the analgesic effect of central histamine in the partial sciatic nerve ligation model of neuropathic pain. METHODS: Neuropathic pain was induced by partial sciatic nerve ligation (PSL) in rats, wild-type (C57BL/6J) mice and HDC(-/-) (histidine decarboxylase gene knockout) and IL-1R(-/-) (interleukin-1 receptor gene knockout) mice. Histidine, a precursor of histamine that can increase the central histamine levels, was administered intraperitoneally (i.p.). Histidine decarboxylase (HDC) enzyme inhibitor α-fluoromethylhistidine was administered intracerebroventricularly (i.c.v.). Histamine H1 receptor antagonist mepyramine and H2 receptor antagonist cimetidine were given intrathecally (i.t.) and intracisternally (i.c.). Withdrawal thresholds to tactile and heat stimuli were measured with a set of von Frey hairs and infrared laser, respectively. Immunohistochemistry and Western blot were carried out to evaluate the morphology of microglia and IL-1ß production, respectively. RESULTS: Histidine (100 mg/kg, i.p.) administered throughout days 0-3, 0-7, or 0-14 postoperatively (PO) alleviated mechanical allodynia and thermal hyperalgesia in the hindpaw following PSL in rats. Intrathecal histamine reversed PSL-induced thermal hyperalgesia in a dose-dependent manner and intracisternal histamine alleviated both mechanical allodynia and thermal hyperalgesia. Moreover, α-fluoromethylhistidine (i.c.v.) abrogated the analgesic effect of histidine. However, histidine treatment initiated later than the first postoperative day (treatment periods included days 2-3, 4-7, and 8-14 PO) did not show an analgesic effect. In addition, histidine treatment initiated immediately, but not 3 days after PSL, inhibited microglial activation and IL-1ß upregulation in the lumbar spinal cord, in parallel with its effects on behavioral hypersensitivity. Moreover, the inhibitory effects on pain hypersensitivity and spinal microglial activation were absent in HDC(-/-) mice and IL-1R(-/-) mice. H1 receptor antagonist mepyramine (200 ng/rat i.t. or i.c.), but not H2 receptor antagonist cimetidine (200, 500 ng/rat i.t. or 500 ng/rat i.c.), blocked the effects of histidine on pain behavior and spinal microglia. CONCLUSIONS: These results demonstrate that central histamine is analgesic within a critical time window in the PSL model of neuropathic pain via histamine H1 receptors. This effect may partly relate to the inhibition of microglial activation and IL-1ß production in the spinal cord following nerve injury.
[Mh] Termos MeSH primário: Analgésicos/uso terapêutico
Sistema Nervoso Central/metabolismo
Histidina/uso terapêutico
Neuropatia Ciática
[Mh] Termos MeSH secundário: Analgésicos/farmacologia
Animais
Sistema Nervoso Central/efeitos dos fármacos
Cimetidina/farmacologia
Modelos Animais de Doenças
Vias de Administração de Medicamentos
Antagonistas dos Receptores Histamínicos H1/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Histidina/farmacologia
Histidina Descarboxilase/deficiência
Histidina Descarboxilase/genética
Hiperalgesia/tratamento farmacológico
Hiperalgesia/etiologia
Camundongos
Camundongos Endogâmicos C57BL
Camundongos Knockout
Limiar da Dor/efeitos dos fármacos
Pirilamina/farmacologia
Ratos
Ratos Sprague-Dawley
Receptores de Interleucina-1/deficiência
Receptores de Interleucina-1/genética
Neuropatia Ciática/tratamento farmacológico
Neuropatia Ciática/metabolismo
Neuropatia Ciática/patologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics); 0 (Histamine H1 Antagonists); 0 (Histamine H2 Antagonists); 0 (Receptors, Interleukin-1); 4QD397987E (Histidine); 80061L1WGD (Cimetidine); EC 4.1.1.22 (Histidine Decarboxylase); HPE317O9TL (Pyrilamine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170929
[Lr] Data última revisão:
170929
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160626
[St] Status:MEDLINE
[do] DOI:10.1186/s12974-016-0637-0


  7 / 1723 MEDLINE  
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[PMID]:26830082
[Au] Autor:Tega Y; Yuzurihara C; Kubo Y; Akanuma SI; Ehrhardt C; Hosoya KI
[Ad] Endereço:Department of Pharmaceutics, Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan. Electronic address: d1361305@ems.u-toyama.ac.jp.
[Ti] Título:Functional expression of nicotine influx transporter in A549 human alveolar epithelial cells.
[So] Source:Drug Metab Pharmacokinet;31(1):99-101, 2016 Feb.
[Is] ISSN:1880-0920
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Nicotine is a potent addictive alkaloid, and is rapidly absorbed through the alveoli of the lung. However, the transport mechanism of nicotine at the human alveolar epithelial barrier has not been investigated in great detail. In the present study, the transport mechanism of nicotine across alveolar epithelium was investigated in vitro using A549 cells, a human adenocarcinoma-derived cell line with an alveolar epithelial cell like phenotype. Nicotine uptake by A549 cells exhibited time-, temperature-, and concentration-dependence with a Km of 50.4 µM. These results suggest that a carrier-mediated transport process is involved in nicotine transport in human alveolar epithelial cells. Nicotine uptake by A549 cells was insensitive to change in extracellular pH. Moreover, nicotine uptake by A549 cells could be inhibited by organic cations such as verapamil and pyrilamine, but not typical substrates of organic cation transporters and ß2-agonist. These results suggest that a novel, not yet molecularly identified, organic cation transporter plays a role in nicotine transport which is unlikely to interact with ß2-agonist transport. This nicotine influx transporter in human alveolar epithelium might have implications for the rapid absorption of nicotine into the systemic circulation.
[Mh] Termos MeSH primário: Transporte Biológico/fisiologia
Células Epiteliais/metabolismo
Nicotina/metabolismo
Alvéolos Pulmonares/metabolismo
[Mh] Termos MeSH secundário: Agonistas Adrenérgicos beta/metabolismo
Linhagem Celular Tumoral
Seres Humanos
Proteínas de Transporte de Cátions Orgânicos/metabolismo
Pirilamina/metabolismo
Verapamil/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-Agonists); 0 (Organic Cation Transport Proteins); 6M3C89ZY6R (Nicotine); CJ0O37KU29 (Verapamil); HPE317O9TL (Pyrilamine)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:170731
[Lr] Data última revisão:
170731
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160203
[St] Status:MEDLINE


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[PMID]:26704812
[Au] Autor:Briggs SA; Hall BJ; Wells C; Slade S; Jaskowski P; Morrison M; Rezvani AH; Rose JE; Levin ED
[Ad] Endereço:Department of Psychiatry and Behavioral Sciences, Duke University Medical Center, USA.
[Ti] Título:Dextromethorphan interactions with histaminergic and serotonergic treatments to reduce nicotine self-administration in rats.
[So] Source:Pharmacol Biochem Behav;142:1-7, 2016 Mar.
[Is] ISSN:1873-5177
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Combining effective treatments with diverse mechanisms of action for smoking cessation may provide better therapy by targeting multiple points of control in the neural circuits underlying addiction. Previous research in a rat model has shown that dextromethorphan, which has α3ß4 nicotinic and NMDA glutamatergic antagonist actions, significantly decreases nicotine self-administration. We have found in the rat model that the H1 histamine antagonist pyrilamine and the serotonin 5HT2C agonist lorcaserin also significantly reduce nicotine self-administration. The current studies were conducted to determine the interactive effects of dextromethorphan with pyrilamine and lorcaserin on nicotine self-administration in rats. Young adult female rats were fitted with jugular IV catheters and trained to self-administer a nicotine infusion dose of 0.03-mg/kg/infusion. In an initial dose-effect function study of dextromethorphan, we found a monotonic decrease in nicotine self-administration over a dose range of 1 to 30-mg/kg with the lowest effective dose of 3-mg/kg. Then, with two separate cohorts of rats, dextromethorphan (0, 3.3, and 10-mg/kg) interactions with pyrilamine (0, 4.43, and 13.3-mg/kg) were investigated as well as interactions with lorcaserin (0, 0.3125 and 0.625-mg/kg). In the pyrilamine-dextromethorphan interaction study, an acute dose of pyrilamine (13.3-mg/kg) as well as an acute dose of dextromethorphan caused a significant decrease in nicotine self-administration. There were mutually augmenting effects of these two drugs. The combination of dextromethorphan (10-mg/kg) and pyrilamine (13.3-mg/kg) significantly lowered nicotine self-administration relative to either 10-mg/kg of dextromethorphan alone (p<0.05) or 13.3-mg/kg of pyrilamine alone (p<0.0005). In the lorcaserin-dextromethorphan study, an acute dose of lorcaserin (0.312-mg/kg) as well as an acute dose of dextromethorphan (10-mg/kg) caused a significant decrease in nicotine self-administration replicating previous findings. Augmenting interactions were observed with dextromethorphan and pyrilamine as well as lorcaserin. These findings suggest that combination therapy may be more effective smoking cessation treatments than monotherapy.
[Mh] Termos MeSH primário: Benzazepinas/farmacologia
Dextrometorfano/farmacologia
Antagonistas dos Receptores Histamínicos H1/farmacologia
Nicotina/administração & dosagem
Pirilamina/farmacologia
Agonistas de Receptores de Serotonina/farmacologia
[Mh] Termos MeSH secundário: Animais
Feminino
Ratos
Ratos Sprague-Dawley
Autoadministração
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzazepines); 0 (Histamine H1 Antagonists); 0 (Serotonin Receptor Agonists); 637E494O0Z (lorcaserin); 6M3C89ZY6R (Nicotine); 7355X3ROTS (Dextromethorphan); HPE317O9TL (Pyrilamine)
[Em] Mês de entrada:1610
[Cu] Atualização por classe:170301
[Lr] Data última revisão:
170301
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151226
[St] Status:MEDLINE


  9 / 1723 MEDLINE  
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[PMID]:26467607
[Au] Autor:Khan N; Saad A; Nurulain SM; Darras FH; Decker M; Sadek B
[Ad] Endereço:Department of Pharmacology and Therapeutics, College of Medicine & Health Sciences, P.O. Box 17666, Al Ain 0097, United Arab Emirates University, United Arab Emirates.
[Ti] Título:The dual-acting H3 receptor antagonist and AChE inhibitor UW-MD-71 dose-dependently enhances memory retrieval and reverses dizocilpine-induced memory impairment in rats.
[So] Source:Behav Brain Res;297:155-64, 2016 Jan 15.
[Is] ISSN:1872-7549
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Both the histamine H3 receptor (H3R) and acetylcholine esterase (AChE) are involved in the regulation of release and metabolism of acetylcholine and several other central neurotransmitters. Therefore, dual-active H3R antagonists and AChE inhibitors (AChEIs) have shown in several studies to hold promise to treat cognitive disorders like Alzheimer's disease (AD). The novel dual-acting H3R antagonist and AChEI 7-(3-(piperidin-1-yl)propoxy)-1,2,3,9-tetrahydropyrrolo[2,1-b]quinazoline (UW-MD-71) with excellent selectivity profiles over both the three other HRs as well as the AChE's isoenzyme butyrylcholinesterase (BChE) shows high and balanced in vitro affinities at both H3R and AChE with IC50 of 33.9nM and hH3R antagonism with Ki of 76.2nM, respectively. In the present study, the effects of UW-MD-71 (1.25-5mg/kg, i.p.) on acquisition, consolidation, and retrieval in a one-trial inhibitory avoidance task in male rats were investigated applying donepezil (DOZ) and pitolisant (PIT) as reference drugs. Furthermore, the effects of UW-MD-71 on memory deficits induced by the non-competitive N-methyl-d-aspartate (NMDA) antagonist dizocilpine (DIZ) were tested. Our results indicate that administration of UW-MD-71 before the test session dose-dependently increased performance and enhanced procognitive effect on retrieval. However neither pre- nor post-training acute systemic administration of UW-MD-71 facilitated acquisition or consolidation. More importantly, UW-MD-71 (2.5mg/kg, i.p.) ameliorated the DIZ-induced amnesic effects. Furthermore, the procognitive activity of UW-MD-71 in retrieval was completely reversed and partly abrogated in DIZ-induced amnesia when rats were pretreated with the centrally-acting H2R antagonist zolantidine (ZOL), but not with the CNS penetrant H1R antagonist pyrilamine (PYR). These results demonstrate the procognitive effects of UW-MD-71 in two in vivo memory models, and are to our knowledge the first demonstration in vivo that a potent dual-acting H3R antagonist and AChEI is effective in improving retrieval processes in the one-trial inhibitory avoidance task and provide evidence to such compounds to treat cognitive disorders.
[Mh] Termos MeSH primário: Inibidores da Colinesterase/farmacologia
Antagonistas dos Receptores Histamínicos H3/farmacologia
Transtornos da Memória/tratamento farmacológico
Memória/efeitos dos fármacos
Nootrópicos/farmacologia
Pirróis/farmacologia
Quinazolinas/farmacologia
[Mh] Termos MeSH secundário: Animais
Aprendizagem da Esquiva/efeitos dos fármacos
Aprendizagem da Esquiva/fisiologia
Benzotiazóis/farmacologia
Modelos Animais de Doenças
Maleato de Dizocilpina
Relação Dose-Resposta a Droga
Avaliação Pré-Clínica de Medicamentos
Indanos/farmacologia
Masculino
Memória/fisiologia
Transtornos da Memória/metabolismo
Fenoxipropanolaminas/farmacologia
Piperidinas/farmacologia
Pirilamina/farmacologia
Distribuição Aleatória
Ratos Wistar
Receptores Histamínicos H3/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (7-(3-(piperidin-1-yl)propoxy)-1,2,3,9-tetrahydropyrrolo(2,1-b)quinazoline); 0 (Benzothiazoles); 0 (Cholinesterase Inhibitors); 0 (Histamine H3 Antagonists); 0 (Indans); 0 (Nootropic Agents); 0 (Phenoxypropanolamines); 0 (Piperidines); 0 (Pyrroles); 0 (Quinazolines); 0 (Receptors, Histamine H3); 4BC83L4PIY (1-(3-(3-(4-chlorophenyl)propoxy)propyl)piperidine); 6LR8C1B66Q (Dizocilpine Maleate); 8SSC91326P (donepezil); HPE317O9TL (Pyrilamine); M1108XAY01 (zolantidine)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151016
[St] Status:MEDLINE


  10 / 1723 MEDLINE  
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[PMID]:25377246
[Au] Autor:Wilton J; Kurenova E; Pitzonka L; Gaudy A; Curtin L; Sexton S; Cance W; Fetterly G
[Ad] Endereço:PK/PD Core Resource, CGP L1-140, Roswell Park Cancer Institute, Elm and Carlton Streets, Buffalo, NY, 14263, USA. john.wilton@roswellpark.org.
[Ti] Título:Pharmacokinetic analysis of the FAK scaffold inhibitor C4 in dogs.
[So] Source:Eur J Drug Metab Pharmacokinet;41(1):55-67, 2016 Feb.
[Is] ISSN:2107-0180
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Inhibition of focal adhesion kinase-vascular endothelial growth factor receptor 3 complex by C4 was previously shown to reduce tumor growth alone and synergistically with other chemotherapeutic agents in animal tumor models. Single and multiple dose IV and oral dosing studies were performed in dogs to determine C4 pharmacokinetics. C4 was administered to 4 dogs at 1.25 or 2.50 mg/kg IV, or 7.50 mg/kg oral gavage. Single- (IV and oral) and multiple- (IV) dose pharmacokinetic samples were collected on days 1 and 3 at pre-dose and 0.5, 1, 2, 4, 8, 24, 120, 144, and 168 h post-dose. C4 concentrations were determined using liquid chromatography with tandem mass spectral detection with a limit of quantitation of 2.50 pg/mL. Pharmacokinetics of C4 was characterized by a 3-compartment model with linear distributional and elimination clearances using Phoenix 64 WinNonlin 6.3. Mean C4 plasma concentration-time profiles revealed a triexponential decline following either IV or oral administration, independent of dose with no accumulation. For the 2.5 mg/kg dose, the median half-life was ~21 h. Median C max and area under the curve (AUC0-24) were similar for days 1 and 3. Oral bioavailability for formulations of PBS, TPGS, Maalox(®), and Pepcid(®) was greatest with TPGS (45 %), followed by Maalox(®) (42 %), Pepcid(®) (37 %), and PBS (30 %). The pharmacokinetic study revealed that C4 has linear pharmacokinetics and does not accumulate following multiple-dose administration. Characterization of C4 pharmacokinetics provides a better understanding of the novel targeted agent, which will help facilitate further development of C4.
[Mh] Termos MeSH primário: Proteína-Tirosina Quinases de Adesão Focal/antagonistas & inibidores
Proteína-Tirosina Quinases de Adesão Focal/metabolismo
Antagonistas dos Receptores Histamínicos H1/química
Antagonistas dos Receptores Histamínicos H1/farmacocinética
Pirilamina/análogos & derivados
Pirilamina/farmacocinética
[Mh] Termos MeSH secundário: Animais
Cães
Relação Dose-Resposta a Droga
Feminino
Masculino
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Histamine H1 Antagonists); EC 2.7.10.2 (Focal Adhesion Protein-Tyrosine Kinases); HPE317O9TL (Pyrilamine)
[Em] Mês de entrada:1610
[Cu] Atualização por classe:170201
[Lr] Data última revisão:
170201
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141108
[St] Status:MEDLINE
[do] DOI:10.1007/s13318-014-0233-6



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