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[PMID]:28131770
[Au] Autor:Kim M; Lee S; Cho J; Kim G; Won C
[Ad] Endereço:Department of Veterinary Medicine, Institute of Animal Medicine, Gyeongsang National University, Jinju 660-701, South Korea.
[Ti] Título:Dopamine D3 receptor-modulated neuroprotective effects of lisuride.
[So] Source:Neuropharmacology;117:14-20, 2017 May 01.
[Is] ISSN:1873-7064
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Dopamine (DA) contributes to the regulation of voluntary movement, and a deficiency in DAergic neurons leads to movement disorders. The objective of this study was to examine the neuroprotective effect of DA D2-like receptor agonist, lisuride, and the role of DA receptors in this protection. Treatment with lisuride alleviated loss of tyrosine hydroxylase (TH) both direct and intraperitoneal injection in 6-hydroxydopamine (6-OHDA) mouse model. Similar results were obtained in primary neuronal cultures treated with lisuride. Lisuride protected TH expression against 6-OHDA-induced cytotoxicity in a concentration-dependent manner. Then, we evaluated the role of DA D2 and D3 receptor in neuroprotective effect of lisuride. Treatment of neuronal cultures with L-741,626, a DA D2 receptor-selective antagonist, did not alter neuroprotective effect of lisuride. However, protective effect of lisuride on TH expression was abolished when cells were treated with GR103691, a D3 receptor selective antagonist. Furthermore, whether lisuride can alleviate mitochondrial damage of DAergic neurons induced by 6-OHDA, we investigated the expression of the mitochondrial regulatory protein, paraplegin, and changes in mitochondria morphology. Treatment with lisuride countered a 6-OHDA-induced reduction in paraplegin and TH expression, and co-treatment with GR103691 blocked this effect of lisuride. Transmission electron microscopy confirmed the lisuride mitigation of 6-OHDA-induced damage to the mitochondrial membrane and cristae. These results suggest that the DA D3 receptor mediates the neuroprotective effects of lisuride by preventing mitochondrial damage.
[Mh] Termos MeSH primário: Lisurida/farmacologia
Fármacos Neuroprotetores/farmacologia
Receptores de Dopamina D3/agonistas
[Mh] Termos MeSH secundário: ATPases Associadas a Diversas Atividades Celulares
Animais
Compostos de Bifenilo/farmacologia
Antagonistas dos Receptores de Dopamina D2/farmacologia
Relação Dose-Resposta a Droga
Feminino
Indóis/farmacologia
Lisurida/antagonistas & inibidores
Masculino
Metaloendopeptidases/metabolismo
Camundongos
Mitocôndrias/efeitos dos fármacos
Mitocôndrias/ultraestrutura
Fármacos Neuroprotetores/antagonistas & inibidores
Oxidopamina/antagonistas & inibidores
Piperazinas/farmacologia
Piperidinas/farmacologia
Cultura Primária de Células
Receptores de Dopamina D3/antagonistas & inibidores
Tirosina 3-Mono-Oxigenase/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biphenyl Compounds); 0 (Dopamine D2 Receptor Antagonists); 0 (Indoles); 0 (Neuroprotective Agents); 0 (Piperazines); 0 (Piperidines); 0 (Receptors, Dopamine D3); 0Y0CM1A77L (GR 103691); 81226-60-0 (3-(4-(4-chlorophenyl-4-hydroxypiperidino)methyl)indole); 8HW4YBZ748 (Oxidopamine); E0QN3D755O (Lisuride); EC 1.14.16.2 (Tyrosine 3-Monooxygenase); EC 3.4.24.- (Metalloendopeptidases); EC 3.4.24.- (Spg7 protein, mouse); EC 3.6.4.- (ATPases Associated with Diverse Cellular Activities)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170130
[St] Status:MEDLINE


  2 / 712 MEDLINE  
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[PMID]:27133570
[Au] Autor:Lythgoe MP; Rhodes CJ; Ghataorhe P; Attard M; Wharton J; Wilkins MR
[Ad] Endereço:Department of Medicine, Imperial College London, W12 0NN, United Kingdom.
[Ti] Título:Why drugs fail in clinical trials in pulmonary arterial hypertension, and strategies to succeed in the future.
[So] Source:Pharmacol Ther;164:195-203, 2016 Aug.
[Is] ISSN:1879-016X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The past three decades have witnessed a welcome expansion of the therapeutic armamentarium for the management of pulmonary arterial hypertension (PAH). However, against this backdrop, there have been some notable disappointments in drug development. Here we use these as case studies to emphasize the importance of informed drug target selection, the early evaluation of dose-response relationships in human studies, and the value of the deep phenotyping of patients in clinical studies to better understand inter-individual variation in patient response. The integration of "omics" technologies and advanced clinical imaging offer the potential to reduce the risk, and so cost, of drug development in PAH and bring much needed new medicines to those patients most likely to benefit with greater efficiency.
[Mh] Termos MeSH primário: Estudos Clínicos como Assunto/métodos
Hipertensão Pulmonar/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Biomarcadores
Modelos Animais de Doenças
Relação Dose-Resposta a Droga
Combinação de Medicamentos
Seres Humanos
Inibidores de Hidroximetilglutaril-CoA Redutases/farmacologia
Hipertensão Pulmonar/patologia
Hipertensão Pulmonar/fisiopatologia
Lisurida/análogos & derivados
Lisurida/farmacologia
Fenótipo
Fentolamina/farmacologia
Proteínas Tirosina Quinases/antagonistas & inibidores
Peptídeo Intestinal Vasoativo/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Biomarkers); 0 (Drug Combinations); 0 (Hydroxymethylglutaryl-CoA Reductase Inhibitors); 0 (aviptadil); 21OJT43Q88 (dironyl); 37221-79-7 (Vasoactive Intestinal Peptide); E0QN3D755O (Lisuride); EC 2.7.10.1 (Protein-Tyrosine Kinases); Z468598HBV (Phentolamine)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170731
[Lr] Data última revisão:
170731
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160503
[St] Status:MEDLINE


  3 / 712 MEDLINE  
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[PMID]:24637012
[Au] Autor:Karaki S; Becamel C; Murat S; Mannoury la Cour C; Millan MJ; Prézeau L; Bockaert J; Marin P; Vandermoere F
[Ad] Endereço:CNRS, UMR-5203, Institut de Génomique Fonctionnelle, F-34094 Montpellier, France;
[Ti] Título:Quantitative phosphoproteomics unravels biased phosphorylation of serotonin 2A receptor at Ser280 by hallucinogenic versus nonhallucinogenic agonists.
[So] Source:Mol Cell Proteomics;13(5):1273-85, 2014 May.
[Is] ISSN:1535-9484
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The serotonin 5-HT(2A) receptor is a primary target of psychedelic hallucinogens such as lysergic acid diethylamine, mescaline, and psilocybin, which reproduce some of the core symptoms of schizophrenia. An incompletely resolved paradox is that only some 5-HT(2A) receptor agonists exhibit hallucinogenic activity, whereas structurally related agonists with comparable affinity and activity lack such a psychoactive activity. Using a strategy combining stable isotope labeling by amino acids in cell culture with enrichment in phosphorylated peptides by means of hydrophilic interaction liquid chromatography followed by immobilized metal affinity chromatography, we compared the phosphoproteome in HEK-293 cells transiently expressing the 5-HT(2A) receptor and exposed to either vehicle or the synthetic hallucinogen 1-[2,5-dimethoxy-4-iodophenyl]-2-aminopropane (DOI) or the nonhallucinogenic 5-HT(2A) agonist lisuride. Among the 5995 identified phosphorylated peptides, 16 sites were differentially phosphorylated upon exposure of cells to DOI versus lisuride. These include a serine (Ser(280)) located in the third intracellular loop of the 5-HT(2A) receptor, a region important for its desensitization. The specific phosphorylation of Ser(280) by hallucinogens was further validated by quantitative mass spectrometry analysis of immunopurified receptor digests and by Western blotting using a phosphosite specific antibody. The administration of DOI, but not of lisuride, to mice, enhanced the phosphorylation of 5-HT(2A) receptors at Ser(280) in the prefrontal cortex. Moreover, hallucinogens induced a less pronounced desensitization of receptor-operated signaling in HEK-293 cells and neurons than did nonhallucinogenic agonists. The mutation of Ser(280) to aspartic acid (to mimic phosphorylation) reduced receptor desensitization by nonhallucinogenic agonists, whereas its mutation to alanine increased the ability of hallucinogens to desensitize the receptor. This study reveals a biased phosphorylation of the 5-HT(2A) receptor in response to hallucinogenic versus nonhallucinogenic agonists, which underlies their distinct capacity to desensitize the receptor.
[Mh] Termos MeSH primário: Anfetaminas/farmacologia
Alucinógenos/farmacologia
Lisurida/farmacologia
Receptor 5-HT2A de Serotonina/metabolismo
Serina/metabolismo
Agonistas de Receptores 5-HT2 de Serotonina/farmacologia
[Mh] Termos MeSH secundário: Animais
Células Cultivadas
Regulação da Expressão Gênica/efeitos dos fármacos
Células HEK293
Seres Humanos
Camundongos
Neurônios/metabolismo
Fosforilação
Córtex Pré-Frontal/metabolismo
Proteômica/métodos
Transdução de Sinais/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amphetamines); 0 (Hallucinogens); 0 (Receptor, Serotonin, 5-HT2A); 0 (Serotonin 5-HT2 Receptor Agonists); 452VLY9402 (Serine); E0QN3D755O (Lisuride); OOM10GW9UE (4-iodo-2,5-dimethoxyphenylisopropylamine)
[Em] Mês de entrada:1501
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140319
[St] Status:MEDLINE
[do] DOI:10.1074/mcp.M113.036558


  4 / 712 MEDLINE  
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[PMID]:24057816
[Au] Autor:Der-Ghazarian T; Widarma CB; Gutierrez A; Amodeo LR; Valentine JM; Humphrey DE; Gonzalez AE; Crawford CA; McDougall SA
[Ad] Endereço:Department of Psychology, California State University, 5500 University Parkway, San Bernardino, CA, 92407, USA.
[Ti] Título:Behavioral effects of dopamine receptor inactivation in the caudate-putamen of preweanling rats: role of the D2 receptor.
[So] Source:Psychopharmacology (Berl);231(4):651-62, 2014 Feb.
[Is] ISSN:1432-2072
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:RATIONALE: Inactivating dopamine (DA) receptors in the caudate-putamen (CPu) attenuates basal and DA agonist-induced behaviors of adult rats while paradoxically increasing the locomotor activity of preweanling rats. OBJECTIVE: The purpose of this study was to determine (a) whether D1 or D2 receptor inactivation is responsible for the elevated locomotion shown by preweanling rats and (b) whether DA receptor inactivation produces a general state in which any locomotor-activating drug will cause a potentiated behavioral response. METHODS: Dimethyl sulfoxide (DMSO) or N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) was bilaterally infused into the CPu on postnatal day (PD) 17. In experiment 1, DA receptors were selectively protected from EEDQ-induced alkylation by pretreating rats with D1 and/or D2 antagonists. On PD 18, rats received bilateral microinjections of the DA agonist R(-)-propylnorapomorphine into the dorsal CPu, and locomotor activity was measured for 40 min. In subsequent experiments, the locomotion of DMSO- and EEDQ-pretreated rats was assessed after intraCPu infusions of the selective DA agonists SKF82958 and quinpirole, the partial agonist terguride, or after systemic administration of nonDAergic compounds. RESULTS: Experiment 1 showed that EEDQ's ability to enhance the locomotor activity of preweanling rats was primarily due to the inactivation of D2 receptors. Consistent with this finding, only drugs that directly or indirectly stimulated D2 receptors produced a potentiated locomotor response in EEDQ-treated rats. CONCLUSIONS: These results show that DA receptor inactivation causes dramatically different behavioral effects in preweanling and adult rats, thus providing additional evidence that the D2 receptor system is not functionally mature by the end of the preweanling period.
[Mh] Termos MeSH primário: Núcleo Caudado/metabolismo
Putamen/metabolismo
Receptores de Dopamina D2/metabolismo
[Mh] Termos MeSH secundário: Envelhecimento
Alquilantes/farmacologia
Animais
Apomorfina/análogos & derivados
Apomorfina/farmacologia
Benzazepinas/farmacologia
Núcleo Caudado/efeitos dos fármacos
Núcleo Caudado/crescimento & desenvolvimento
Dimetil Sulfóxido/farmacologia
Agonistas de Dopamina/farmacologia
Antagonistas de Dopamina/farmacologia
Antagonistas dos Receptores de Dopamina D2
Feminino
Lisurida/análogos & derivados
Lisurida/farmacologia
Masculino
Atividade Motora/efeitos dos fármacos
Atividade Motora/fisiologia
Putamen/efeitos dos fármacos
Putamen/crescimento & desenvolvimento
Quinolinas/farmacologia
Quimpirol/farmacologia
Ratos
Ratos Sprague-Dawley
Receptores de Dopamina D1/agonistas
Receptores de Dopamina D1/antagonistas & inibidores
Receptores de Dopamina D1/metabolismo
Receptores de Dopamina D2/agonistas
Desmame
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Alkylating Agents); 0 (Benzazepines); 0 (Dopamine Agonists); 0 (Dopamine Antagonists); 0 (Dopamine D2 Receptor Antagonists); 0 (Quinolines); 0 (Receptors, Dopamine D1); 0 (Receptors, Dopamine D2); 20OP60125T (Quinpirole); 21OJT43Q88 (dironyl); 58479-52-0 (N-n-propylnorapomorphine); 60O971AN19 (EEDQ); 80751-65-1 (SK&F 82958); E0QN3D755O (Lisuride); N21FAR7B4S (Apomorphine); YOW8V9698H (Dimethyl Sulfoxide)
[Em] Mês de entrada:1410
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130924
[St] Status:MEDLINE
[do] DOI:10.1007/s00213-013-3280-9


  5 / 712 MEDLINE  
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[PMID]:24030470
[Au] Autor:Baladi MG; Newman AH; France CP
[Ad] Endereço:Department of Pharmacology, University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Drive, Mail Code 7764, San Antonio, TX, 78229, USA.
[Ti] Título:Feeding condition and the relative contribution of different dopamine receptor subtypes to the discriminative stimulus effects of cocaine in rats.
[So] Source:Psychopharmacology (Berl);231(3):581-91, 2014 Feb.
[Is] ISSN:1432-2072
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:RATIONALE: The contribution of dopamine receptor subtypes in mediating the discriminative stimulus effects of cocaine is not fully established. Many drug discrimination studies use food to maintain responding, necessitating food restriction, which can alter drug effects. OBJECTIVE: This study established stimulus control with cocaine (10 mg/kg) in free-feeding and food-restricted rats responding under a schedule of stimulus shock termination (SST) and in food-restricted rats responding under a schedule of food presentation to examine whether feeding condition or the reinforcer used to maintain responding impacts the effects of cocaine. METHOD: Dopamine receptor agonists and antagonists were examined for their ability to mimic or attenuate, respectively, the effects of cocaine. RESULTS: Apomorphine, quinpirole, and lisuride occasioned >90 % responding on the cocaine-associated lever in free-feeding rats responding under a schedule of SST; apomorphine, but not quinpirole or lisuride, occasioned >90 % responding on the cocaine lever in food-restricted rats responding under a schedule of SST. In food-restricted rats responding for food these drugs occasioned little cocaine lever responding and were comparatively more potent in decreasing responding. In free-feeding rats, the effects of cocaine were attenuated by the D2/D3 receptor antagonist raclopride and the D3 receptor-selective antagonist PG01037. In food-restricted rats, raclopride and the D2 receptor-selective antagonist L-741,626 attenuated the effects of cocaine. Raclopride antagonized quinpirole in all groups while PG01037 antagonized quinpirole only in free-feeding rats. CONCLUSION: These results demonstrate significant differences in the discriminative stimulus of cocaine that are due to feeding conditions and not to the use of different reinforcers across procedures.
[Mh] Termos MeSH primário: Cocaína/farmacologia
Discriminação (Psicologia)/efeitos dos fármacos
Agonistas de Dopamina/farmacologia
Antagonistas de Dopamina/farmacologia
Inibidores da Captação de Dopamina/farmacologia
Privação de Alimentos/fisiologia
[Mh] Termos MeSH secundário: Animais
Apomorfina/farmacologia
Benzamidas/farmacologia
Condicionamento Operante/efeitos dos fármacos
Condicionamento Operante/fisiologia
Discriminação (Psicologia)/fisiologia
Eletrochoque
Indóis/farmacologia
Lisurida/farmacologia
Masculino
Piperidinas/farmacologia
Piridinas/farmacologia
Quimpirol/farmacologia
Racloprida/farmacologia
Ratos Sprague-Dawley
Reforço (Psicologia)
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, N.I.H., INTRAMURAL
[Nm] Nome de substância:
0 (Benzamides); 0 (Dopamine Agonists); 0 (Dopamine Antagonists); 0 (Dopamine Uptake Inhibitors); 0 (Indoles); 0 (N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)but-2-enyl)-4-pyridine-2-ylbenzamide); 0 (Piperidines); 0 (Pyridines); 20OP60125T (Quinpirole); 430K3SOZ7G (Raclopride); 81226-60-0 (3-(4-(4-chlorophenyl-4-hydroxypiperidino)methyl)indole); E0QN3D755O (Lisuride); I5Y540LHVR (Cocaine); N21FAR7B4S (Apomorphine)
[Em] Mês de entrada:1501
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130914
[St] Status:MEDLINE
[do] DOI:10.1007/s00213-013-3271-x


  6 / 712 MEDLINE  
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[PMID]:23909604
[Au] Autor:Huang J; Gong Q; Huang C; Li G
[Ti] Título:Relationships between serotoninergic system and skin fibrotic.
[So] Source:Antiinflamm Antiallergy Agents Med Chem;13(1):9-16, 2014 Mar.
[Is] ISSN:1875-614X
[Cp] País de publicação:United Arab Emirates
[La] Idioma:eng
[Ab] Resumo:Cutaneous fibrosis seen in systemic sclerosis (SSc) is a generalized connective tissue disorder, characterized by a wide spectrum of microvascular and immunological abnormalities. Serotonin (5-hydroxytryptamine; 5-HT) is a neurotransmitter and immune modulator, is also an important mediator of bidirectional interactions between the vasoactive amines and the skin.5-HT, a commonly secreted amine, is a known inducer of fibrosis, although the mechanistic basis for it and growth factors regulating fibrosis and proliferation in the microenvironment are unclear. We review that as serotonin has powerful vasodilator, immunomodulator, and growth factor actions, this pathway could be involved in skin fibrotic. Since serotoninergic system play a role in skin fibrotic, and 5-HTs drugs, an usual treatment for this type of patients. These provides a future perspective for research and drug development.
[Mh] Termos MeSH primário: Agonistas de Dopamina/uso terapêutico
Lisurida/análogos & derivados
Escleroderma Sistêmico/tratamento farmacológico
Inibidores da Captação de Serotonina/uso terapêutico
Serotonina/metabolismo
Pele/patologia
[Mh] Termos MeSH secundário: Animais
Processos de Crescimento Celular/efeitos dos fármacos
Fibrose
Seres Humanos
Lisurida/uso terapêutico
Medicina de Precisão
Receptor 5-HT1A de Serotonina/metabolismo
Pele/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Dopamine Agonists); 0 (Serotonin Uptake Inhibitors); 112692-38-3 (Receptor, Serotonin, 5-HT1A); 21OJT43Q88 (dironyl); 333DO1RDJY (Serotonin); E0QN3D755O (Lisuride)
[Em] Mês de entrada:1410
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130806
[St] Status:MEDLINE


  7 / 712 MEDLINE  
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[PMID]:23863695
[Au] Autor:Jantschak F; Brosda J; Franke RT; Fink H; Möller D; Hübner H; Gmeiner P; Pertz HH
[Ad] Endereço:Institute of Pharmacy, Free University of Berlin, Berlin, Germany (F.J., H.H.P.); Institute of Pharmacology and Toxicology, School of Veterinary Medicine, Free University of Berlin, Berlin, Germany (J.B., R.T.F., H.F.); and Department of Chemistry and Pharmacy, Emil Fischer Center, Friedrich Alexander University, Erlangen, Germany (D.M., H.H., P.G.).
[Ti] Título:Pharmacological profile of 2-bromoterguride at human dopamine D2, porcine serotonin 5-hydroxytryptamine 2A, and α2C-adrenergic receptors, and its antipsychotic-like effects in rats.
[So] Source:J Pharmacol Exp Ther;347(1):57-68, 2013 Oct.
[Is] ISSN:1521-0103
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Dopaminergic, serotonergic, and adrenergic receptors are targets for therapeutic actions in schizophrenia. Dopamine D2 receptor partial agonists such as aripiprazole represent a treatment option for patients with this severe disorder. The ineffectiveness of terguride, another D2 receptor partial agonist, in treating schizophrenia was recently attributed to its considerably high intrinsic activity at D2 receptors. In this study, we used functional assays for recombinant D2 receptors and native 5-hydroxytryptamine 2A (5-HT2A), α2C-adrenergic, and histamine H1 receptors to compare the pharmacological properties of terguride and three of its halogenated derivatives (2-chloro-, 2-bromo-, 2-iodoterguride) with those of aripiprazole. Subsequently, we studied the antidopaminergic effects of 2-bromoterguride using amphetamine-induced locomotion (AIL). Its influence on spontaneous behavior was tested in the open field. Extrapyramidal side effect (EPS) liability was evaluated by catalepsy test. In a guanosine 5'-O-(3-[(35)S]thio)triphosphate ([(35)S]GTPγS) binding assay, 2-chloro-, 2-bromo-, and 2-iodoterguride produced intrinsic activities at human D2short (hD2S) receptors that were half as high as the intrinsic activity for terguride; aripiprazole lacked agonist activity. 2-Bromoterguride and aripiprazole activated D2S receptor-mediated inhibition of cAMP accumulation to the same extent; intrinsic activity was half as high as that of terguride. All compounds tested behaved as antagonists at human D2long/Gαo (hD2L/Gαo) receptors. Compared with aripiprazole, terguride and its derivatives displayed higher affinity at porcine 5-HT2A receptors and α2C-adrenoceptors and lower affinity at H1 receptors. 2-Bromoterguride inhibited AIL and did not induce catalepsy in rats. Because of its in vitro and in vivo properties, 2-bromoterguride may be a strong candidate for the treatment of schizophrenia with a lower risk to induce EPS.
[Mh] Termos MeSH primário: Antipsicóticos/administração & dosagem
Antipsicóticos/metabolismo
Agonistas de Dopamina/metabolismo
Lisurida/análogos & derivados
Receptor 5-HT2A de Serotonina/metabolismo
Receptor 5-HT2C de Serotonina/metabolismo
Receptores de Dopamina D2/metabolismo
[Mh] Termos MeSH secundário: Animais
Células CHO
Vasos Coronários/efeitos dos fármacos
Vasos Coronários/metabolismo
Cricetinae
Cricetulus
Agonistas de Dopamina/química
Agonistas de Dopamina/farmacologia
Células HEK293
Seres Humanos
Lisurida/química
Lisurida/metabolismo
Lisurida/farmacologia
Masculino
Atividade Motora/efeitos dos fármacos
Atividade Motora/fisiologia
Técnicas de Cultura de Órgãos
Ligação Proteica/efeitos dos fármacos
Ligação Proteica/fisiologia
Ratos
Ratos Sprague-Dawley
Receptores de Dopamina D2/agonistas
Suínos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Dopamine Agonists); 0 (Receptor, Serotonin, 5-HT2A); 0 (Receptor, Serotonin, 5-HT2C); 0 (Receptors, Dopamine D2); 21OJT43Q88 (dironyl); E0QN3D755O (Lisuride)
[Em] Mês de entrada:1311
[Cu] Atualização por classe:130919
[Lr] Data última revisão:
130919
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130719
[St] Status:MEDLINE
[do] DOI:10.1124/jpet.113.205997


  8 / 712 MEDLINE  
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[PMID]:23565891
[Au] Autor:Agúndez JA; García-Martín E; Alonso-Navarro H; Jiménez-Jiménez FJ
[Ad] Endereço:University of Extremadura, Department of Pharmacology, Avda. de la Universidad s/n, E-10071, Cáceres, Spain. jagundez@unex.es
[Ti] Título:Anti-Parkinson's disease drugs and pharmacogenetic considerations.
[So] Source:Expert Opin Drug Metab Toxicol;9(7):859-74, 2013 Jul.
[Is] ISSN:1744-7607
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: The development of pharmacogenetic-based clinical practice guidelines for the use of anti-Parkinson's disease drugs requires, as a pre-requisite, the identification and validation of genetic biomarkers. These biomarkers are then used as surrogate endpoints. This review analyzes potential genetic biomarkers which can be used to improve anti-Parkinson's disease therapy. AREAS COVERED: The authors present an overview of current knowledge of pharmacogenetic implications of anti-Parkinson's disease drugs, including genes coding for the corresponding drug-metabolizing enzymes and drug targets. The gene/drug pairings with the strongest potential for pharmacogenetic recommendations include: CYP2C19/benztropine, COMT/levodopa and entacapone, CYP2B6/selegiline, UGT1A/entacapone, DRD2/ropinirole, pramipexole and cabergoline, and DRD3/ropinirole and pramipexole. Evidence supporting the effect of substrates, inhibitor or inducers for drug specific metabolizing enzymes in anti-Parkinson's disease drug response includes CYP1A2 in the response to ropinirole and rasagiline, and CYP3A4 in the response to bromocriptine, lisuride, pergolide and cabergoline. The authors present and discuss the current information on gene variations according to the 1000 genomes catalog and other databases with regards to anti-Parkinson's disease drugs. They also review and discuss the clinical implications of these variations. EXPERT OPINION: The goal of pharmacogenomic testing for anti-Parkinson's disease drugs should be conservative and aimed at selecting determined drugs for determined patients. However, much additional research is still needed to obtain reliable pre-prescription tests.
[Mh] Termos MeSH primário: Doença de Parkinson/tratamento farmacológico
Doença de Parkinson/genética
Farmacogenética
[Mh] Termos MeSH secundário: Hidrocarboneto de Aril Hidroxilases/genética
Hidrocarboneto de Aril Hidroxilases/metabolismo
Benzotiazóis/uso terapêutico
Benzotropina/uso terapêutico
Bromocriptina/uso terapêutico
Catecóis/uso terapêutico
Citocromo P-450 CYP1A2/metabolismo
Inibidores do Citocromo P-450 CYP1A2
Citocromo P-450 CYP2B6
Citocromo P-450 CYP2C19
Citocromo P-450 CYP3A/genética
Citocromo P-450 CYP3A/metabolismo
Ergolinas/uso terapêutico
Marcadores Genéticos
Seres Humanos
Indanos/uso terapêutico
Indóis/uso terapêutico
Levodopa/uso terapêutico
Lisurida/uso terapêutico
Nitrilos/uso terapêutico
Pergolida/uso terapêutico
Receptores de Dopamina D2/genética
Receptores de Dopamina D2/metabolismo
Receptores de Dopamina D3/genética
Receptores de Dopamina D3/metabolismo
Reprodutibilidade dos Testes
Selegilina/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; REVIEW
[Nm] Nome de substância:
0 (Benzothiazoles); 0 (Catechols); 0 (Cytochrome P-450 CYP1A2 Inhibitors); 0 (DRD2 protein, human); 0 (DRD3 protein, human); 0 (Ergolines); 0 (Genetic Markers); 0 (Indans); 0 (Indoles); 0 (Nitriles); 0 (Receptors, Dopamine D2); 0 (Receptors, Dopamine D3); 003N66TS6T (rasagiline); 030PYR8953 (ropinirole); 1NHL2J4X8K (Benztropine); 24MJ822NZ9 (Pergolide); 2K1V7GP655 (Selegiline); 3A64E3G5ZO (Bromocriptine); 46627O600J (Levodopa); 4975G9NM6T (entacapone); 83619PEU5T (pramipexole); E0QN3D755O (Lisuride); EC 1.14.13.67 (CYP3A4 protein, human); EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases); EC 1.14.14.1 (CYP1A2 protein, human); EC 1.14.14.1 (CYP2B6 protein, human); EC 1.14.14.1 (CYP2C19 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP1A2); EC 1.14.14.1 (Cytochrome P-450 CYP2B6); EC 1.14.14.1 (Cytochrome P-450 CYP2C19); EC 1.14.14.1 (Cytochrome P-450 CYP3A); LL60K9J05T (cabergoline)
[Em] Mês de entrada:1402
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130410
[St] Status:MEDLINE
[do] DOI:10.1517/17425255.2013.789018


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[PMID]:23407781
[Au] Autor:Halberstadt AL; Geyer MA
[Ad] Endereço:Department of Psychiatry, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093-0804, USA. ahalbers@ucsd.edu
[Ti] Título:Characterization of the head-twitch response induced by hallucinogens in mice: detection of the behavior based on the dynamics of head movement.
[So] Source:Psychopharmacology (Berl);227(4):727-39, 2013 Jun.
[Is] ISSN:1432-2072
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:RATIONALE: The head-twitch response (HTR) is a rapid side-to-side rotational head movement that occurs in rats and mice after administration of serotonergic hallucinogens and other 5-HT2A agonists. The HTR is widely used as a behavioral assay for 5-HT2A activation and to probe for interactions between the 5-HT2A receptor and other transmitter systems. OBJECTIVE: High-speed video recordings were used to analyze the head movement that occurs during head twitches in C57BL/6J mice. Experiments were also conducted in C57BL/6J mice to determine whether a head-mounted magnet and a magnetometer coil could be used to detect the HTR induced by serotonergic hallucinations based on the dynamics of the response. RESULTS: Head movement during the HTR was highly rhythmic and occurred within a specific frequency range (mean head movement frequency of 90.3 Hz). Head twitches produced wave-like oscillations of magnetometer coil voltage that matched the frequency of head movement during the response. The magnetometer coil detected the HTR induced by the serotonergic hallucinogens 2,5-dimethoxy-4-iodoamphetamine (DOI; 0.25, 0.5, and 1.0 mg/kg, i.p.) and lysergic acid diethylamide (LSD; 0.05, 0.1, 0.2, and 0.4 mg/kg, i.p.) with extremely high sensitivity and specificity. Magnetometer coil recordings demonstrated that the non-hallucinogenic compounds (+)-amphetamine (2.5 and 5.0 mg/kg, i.p.) and lisuride (0.8, 1.6, and 3.2 mg/kg, i.p.) did not induce the HTR. CONCLUSIONS: These studies confirm that a magnetometer coil can be used to detect the HTR induced by hallucinogens. The use of magnetometer-based HTR detection provides a high-throughput, semi-automated assay for this behavior, and offers several advantages over traditional assessment methods.
[Mh] Termos MeSH primário: Anfetaminas/farmacologia
Comportamento Animal/efeitos dos fármacos
Alucinógenos/farmacologia
Dietilamida do Ácido Lisérgico/farmacologia
[Mh] Termos MeSH secundário: Anfetamina/administração & dosagem
Anfetamina/farmacologia
Anfetaminas/administração & dosagem
Animais
Alucinógenos/administração & dosagem
Movimentos da Cabeça/efeitos dos fármacos
Ensaios de Triagem em Larga Escala/métodos
Lisurida/administração & dosagem
Lisurida/farmacologia
Dietilamida do Ácido Lisérgico/administração & dosagem
Magnetometria
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Sensibilidade e Especificidade
Gravação em Vídeo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Amphetamines); 0 (Hallucinogens); 8NA5SWF92O (Lysergic Acid Diethylamide); CK833KGX7E (Amphetamine); E0QN3D755O (Lisuride); OOM10GW9UE (4-iodo-2,5-dimethoxyphenylisopropylamine)
[Em] Mês de entrada:1312
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130215
[St] Status:MEDLINE
[do] DOI:10.1007/s00213-013-3006-z


  10 / 712 MEDLINE  
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[PMID]:23204120
[Au] Autor:Sitbon O; Morrell N
[Ad] Endereço:Université Paris-Sud, Hôpital de Bicêtre, Le Kremlin-Bicêtre, France.
[Ti] Título:Pathways in pulmonary arterial hypertension: the future is here.
[So] Source:Eur Respir Rev;21(126):321-7, 2012 Dec 01.
[Is] ISSN:1600-0617
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:It is well established that the endothelin, nitric oxide and prostacyclin pathways play an important role in the development of pulmonary arterial hypertension (PAH). Indeed, the therapeutic options currently available for the management of PAH all act on one of these mechanistic pathways. However, this is an exciting time for both clinicians and scientists, as increased understanding of the mechanisms involved in the pathogenesis and progression of PAH has resulted in the development of a number of novel therapeutic options. This article highlights how the introduction of new compounds such as macitentan, riociguat and selexipag, which act on the endothelin, nitric oxide and prostacyclin pathways, respectively, have the potential to further improve the prognosis for patients with PAH.
[Mh] Termos MeSH primário: Hipertensão Pulmonar/tratamento farmacológico
Hipertensão Pulmonar/metabolismo
[Mh] Termos MeSH secundário: Acetamidas/uso terapêutico
Animais
Anti-Hipertensivos/uso terapêutico
Benzamidas/uso terapêutico
Ensaios Clínicos como Assunto
Drogas em Investigação
Antagonistas do Receptor de Endotelina A
Antagonistas do Receptor de Endotelina B
Endotelina-1/metabolismo
Epoprostenol/análogos & derivados
Epoprostenol/metabolismo
Epoprostenol/uso terapêutico
Guanilato Ciclase/antagonistas & inibidores
Seres Humanos
Mesilato de Imatinib
Lisurida/análogos & derivados
Lisurida/uso terapêutico
Óxido Nítrico/metabolismo
Inibidores da Fosfodiesterase 5/uso terapêutico
Piperazinas/uso terapêutico
Inibidores de Proteínas Quinases/uso terapêutico
Pirazinas/uso terapêutico
Pirazóis/uso terapêutico
Pirimidinas/uso terapêutico
Antagonistas da Serotonina/uso terapêutico
Sulfonamidas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Acetamides); 0 (Antihypertensive Agents); 0 (Benzamides); 0 (Drugs, Investigational); 0 (Endothelin A Receptor Antagonists); 0 (Endothelin B Receptor Antagonists); 0 (Endothelin-1); 0 (Phosphodiesterase 5 Inhibitors); 0 (Piperazines); 0 (Protein Kinase Inhibitors); 0 (Pyrazines); 0 (Pyrazoles); 0 (Pyrimidines); 0 (Serotonin Antagonists); 0 (Sulfonamides); 21OJT43Q88 (dironyl); 31C4KY9ESH (Nitric Oxide); 35E3NJJ4O6 (beraprost); 5EXC0E384L (selexipag); 8A1O1M485B (Imatinib Mesylate); DCR9Z582X0 (Epoprostenol); E0QN3D755O (Lisuride); EC 4.6.1.2 (Guanylate Cyclase); RU3FE2Y4XI (riociguat); RUM6K67ESG (treprostinil); Z9K9Y9WMVL (macitentan)
[Em] Mês de entrada:1305
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:121204
[St] Status:MEDLINE
[do] DOI:10.1183/09059180.00004812



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