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[PMID]: 28012310 [Au] Autor: Mazák K; Hosztafi S; Kraszni M; Noszál B [Ad] Endereço: Semmelweis University, Department of Pharmaceutical Chemistry, Research Group of Drugs of Abuse and Doping Agents, Hungarian Academy of Sciences, Hogyes E. u. 9., H-1092 Budapest, Hungary. Electronic address: mazak.karoly@pharma.semmelweis-univ.hu. [Ti] Título: Physico-chemical profiling of semisynthetic opioids. [So] Source: J Pharm Biomed Anal;135:97-105, 2017 Feb 20. [Is] ISSN: 1873-264X [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Species-specific acid-base and partition equilibrium constants were experimentally determined for the therapeutically important semisynthetic opioid receptor agonist hydromorphone, dihydromorphine, and mixed agonist-antagonist nalorphine and nalbuphine. The acid-base microequilibria were characterized by combining pH-potentiometry and deductive methods using synthesized auxiliary compounds. Independent of the pH, there are approximately 4.8 times as many zwitterionic microspecies than non-charged ones in nalbuphine solutions, while for nalorphine it is the non-charged form that predominates by the same ratio. The non-charged microspecies is the dominant one also in the case of hydromorphone, although its concentration exceeds only 1.3 times that of its zwitterionic protonation isomer. The pH-independent partition coefficients of the individual microspecies were determined by a combination of experimentally measured, pH-dependent, conditional distribution constants and a custom-tailored evaluation method, using highly similar auxiliary compounds. The pH-independent contribution of the zwitterionic microspecies to the distribution constant is 1380, 1070, 3160 and 72,440 times smaller than that of the inherently more lipophilic non-charged one for hydromorphone, dihydromorphine, nalbuphine and nalorphine, respectively. [Mh] Termos MeSH primário: Analgésicos Opioides/química Fenômenos Químicos Di-Hidromorfina/química Hidromorfona/química Nalbufina/química Nalorfina/química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Analgesics, Opioid); C3S5FRP6JW (Dihydromorphine); L2T84IQI2K (Nalbuphine); Q812464R06 (Hydromorphone); U59WB2WRY2 (Nalorphine) [Em] Mês de entrada: 1705 [Cu] Atualização por classe: 170524 [Lr] Data última revisão: 170524 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161225 [St] Status: MEDLINE

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[PMID]: 22580524 [Au] Autor: Leppert W; Mikolajczak P; Kaminska E; Szulc M [Ad] Endereço: Department of Palliative Medicine, Poznan University of Medical Sciences, Osiedle Rusa 25 A, PL 61-245 Poznan, Poland. wojciechleppert@wp.pl [Ti] Título: Analgesia and serum assays of controlled-release dihydrocodeine and metabolites in cancer patients with pain. [So] Source: Pharmacol Rep;64(1):84-93, 2012. [Is] ISSN: 1734-1140 [Cp] País de publicação: Poland [La] Idioma: eng [Ab] Resumo: Aim of the study was to assess dihydrocodeine (DHC) and metabolites concentrations and their correlations with DHC analgesia in cancer patients with pain. Thirty opioid-naive patients with nociceptive pain intensity assessed by VAS (visual analogue scale) > 40 received controlled-release DHC as the first (15 patients, 7 days) or as the second opioid (15 patients, 7 days). Blood samples were taken on day 2, 4 and 7 at each study period. DHC and its metabolites were assayed by HPLC. DHC provided satisfactory analgesia when administered as the first or the second opioid superior to that of tramadol. When DHC was the first opioid administered, DHC and dihydrocodeine-6-glucuronide (DHC-6-G) concentrations increased in the second and the third comparing to the first assay. A trend of nordihydromorphine (NDHM) level fall between the first and the third assay was noted; trends of dihydromorphine (DHM) level increase in the second relative to the first determination and decrease in the third compared to the second assay were observed. When DHC followed tramadol treatment a trend of DHC concentration increase in the second relative to the first assay was noted. DHC-6-G level increased in the second and in the third comparing to the first determination; NDHM and DHM concentrations were stable. DHC and DHC-6-G concentrations increased similarly during both treatment periods which suggest their prominent role in DHC analgesia. Few significant correlations were found between DHC dose, DHC and metabolites serum concentrations with analgesia suggesting the individual DHC dose titration. [Mh] Termos MeSH primário: Codeína/análogos & derivados Neoplasias/sangue Neoplasias/complicações Dor Nociceptiva/sangue Dor Nociceptiva/tratamento farmacológico [Mh] Termos MeSH secundário: Idoso Idoso de 80 Anos ou mais Analgesia/métodos Analgésicos Opioides/administração & dosagem Analgésicos Opioides/sangue Analgésicos Opioides/metabolismo Codeína/administração & dosagem Codeína/sangue Codeína/metabolismo Di-Hidromorfina/metabolismo Feminino Seres Humanos Masculino Meia-Idade Manejo da Dor/métodos Medição da Dor/métodos [Pt] Tipo de publicação: CLINICAL TRIAL; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Analgesics, Opioid); C3S5FRP6JW (Dihydromorphine); N9I9HDB855 (dihydrocodeine); Q830PW7520 (Codeine) [Em] Mês de entrada: 1212 [Cu] Atualização por classe: 131121 [Lr] Data última revisão: 131121 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 120515 [St] Status: MEDLINE

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[PMID]: 16777416 [Au] Autor: Crooks PA; Kottayil SG; Al-Ghananeem AM; Byrn SR; Butterfield DA [Ad] Endereço: Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, 40536-0082, USA. pcrooks@email.uky.edu [Ti] Título: Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. [So] Source: Bioorg Med Chem Lett;16(16):4291-5, 2006 Aug 15. [Is] ISSN: 0960-894X [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: A series of 3-O-acyl-6-O-sulfate esters of morphine, dihydromorphine, N-methylmorphinium iodide, codeine, and dihydrocodeine were prepared and evaluated for their ability to bind to mu-, delta-, kappa(1)-, kappa(2)-, and kappa(3)-opiate receptors. Several compounds exhibited good affinity for the mu-opiate receptor. Morphine-3-O-propionyl-6-O-sulfate had four times greater affinity than morphine at the mu-opiate receptor and was the most selective compound at this receptor subtype. [Mh] Termos MeSH primário: Codeína/química Di-Hidromorfina/química Ésteres/química Morfina/química Sulfatos/química [Mh] Termos MeSH secundário: Animais Cobaias Concentração Inibidora 50 Cinética Ligantes Modelos Químicos Ligação Proteica [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Esters); 0 (Ligands); 0 (Sulfates); 76I7G6D29C (Morphine); C3S5FRP6JW (Dihydromorphine); Q830PW7520 (Codeine) [Em] Mês de entrada: 0610 [Cu] Atualização por classe: 131121 [Lr] Data última revisão: 131121 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 060617 [St] Status: MEDLINE

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[PMID]: 16718649 [Au] Autor: Baldacci A; Thormann W [Ad] Endereço: Department of Clinical Pharmacology, University of Bern, Bern, Switzerland. [Ti] Título: Capillary electrophoresis contributions to the hydromorphone metabolism in man. [So] Source: Electrophoresis;27(12):2444-57, 2006 Jun. [Is] ISSN: 0173-0835 [Cp] País de publicação: Germany [La] Idioma: eng [Ab] Resumo: CE-ESI multistage IT-MS (CE-MS(n), n < or = 4) and computer simulation of fragmentation are demonstrated to be effective tools to detect and identify phase I and phase II metabolites of hydromorphone (HMOR) in human urine. Using the same CE conditions as previously developed for the analysis of urinary oxycodone and its metabolites, HMOR and its phase I metabolites produced by N-demethylation, 6-keto-reduction and N-oxidation and phase II conjugates of HMOR and its metabolites formed with glucuronic acid, glucose, and sulfuric acid could be detected in urine samples of a patient that were collected during a pharmacotherapy episode with daily ingestion of 48 mg of HMOR chloride. The CE-MS(n) data obtained with the HMOR standard, synthesized hydromorphol and hydromorphone-N-oxide, and CYP3A4 in vitro produced norhydromorphone were employed to identify the metabolites. This approach led to the identification of previously unknown HMOR metabolites, including HMOR-3O-glucide and various N-oxides, structures for which no standard compounds or mass spectra library data were available. Furthermore, the separation of alpha- and beta-hydromorphol, the stereoisomers of 6-keto-reduced HMOR, was achieved by CE in the presence of the single isomer heptakis(2,3-diacetyl-6-sulfato)-beta-CD. The obtained data indicate that the urinary excretion of alpha-hydromorphol is larger than that of beta-hydromorphol. [Mh] Termos MeSH primário: Analgésicos Opioides/metabolismo Di-Hidromorfina/urina Eletroforese Capilar/métodos Hidromorfona/metabolismo [Mh] Termos MeSH secundário: Analgésicos Opioides/urina Seres Humanos Hidromorfona/urina Masculino Óxidos/urina [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Analgesics, Opioid); 0 (Oxides); C3S5FRP6JW (Dihydromorphine); Q812464R06 (Hydromorphone) [Em] Mês de entrada: 0609 [Cu] Atualização por classe: 131121 [Lr] Data última revisão: 131121 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 060524 [St] Status: MEDLINE

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[PMID]: 15178355 [Au] Autor: Gilbert AK; Hosztafi S; Mahurter L; Pasternak GW [Ad] Endereço: Laboratory of Molecular Neuropharmacology, Department of Neurology, Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, New York, NY 10021, USA. [Ti] Título: Pharmacological characterization of dihydromorphine, 6-acetyldihydromorphine and dihydroheroin analgesia and their differentiation from morphine. [So] Source: Eur J Pharmacol;492(2-3):123-30, 2004 May 25. [Is] ISSN: 0014-2999 [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: The present study examined the pharmacology of dihydromorphine, 6-acetyldihydromorphine and dihydroheroin (3,6-diacetyldihydromorphine). Like morphine, dihydromorphine and its acetylated derivatives all were highly selective mu-opioids in receptor binding assays. All the compounds were potent mu-selective analgesics, as shown by their sensitivity towards the mu-selective opioid receptor antagonists naloxonazine and beta-funaltrexamine. However, the actions of dihydromorphine and its analogs were readily distinguished from those of morphine, differences that were surprising in view of the very limited structural differences among them that consisted of only the reduction of the 7,8-double bond. Like heroin and morphine-6beta-glucuronide, the analgesic actions of dihydromorphine and its two acetylated derivatives were antagonized by 3-O-methylnaltrexone at a dose that was inactive against morphine analgesia. Antisense mapping also distinguished between morphine and the dihydromorphine compounds. Antisense oligodeoxynucleotides targeting exon 2 of the cloned MOR-1 gene decreased dihydromorphine analgesia and that of its acetylated derivatives, but not morphine analgesia. Conversely, the exon 1 antisense that effectively lowered morphine analgesia was inactive against dihydromorphine and its analogs. Finally, dihydromorphine and its analogs retained their analgesic activity in a mouse model of morphine tolerance, consistent with incomplete cross-tolerance. Together, these findings imply that the mu-opioid receptor mechanisms mediating the analgesic actions of dihydromorphine and its acetylated analogs are distinct from morphine and more similar to those of heroin and morphine-6beta-glucuronide. [Mh] Termos MeSH primário: Analgésicos Opioides/farmacologia Di-Hidromorfina/análogos & derivados Di-Hidromorfina/farmacologia Heroína/análogos & derivados Heroína/farmacologia Dor/tratamento farmacológico [Mh] Termos MeSH secundário: Analgésicos Opioides/uso terapêutico Animais Di-Hidromorfina/química Di-Hidromorfina/uso terapêutico Tolerância a Medicamentos Calefação Heroína/química Heroína/uso terapêutico Injeções Subcutâneas Masculino Camundongos Camundongos Endogâmicos ICR Morfina/farmacologia Morfina/uso terapêutico Oligonucleotídeos Antissenso/farmacologia Receptores Opioides mu/genética Receptores Opioides mu/metabolismo Reação em Cadeia da Polimerase Via Transcriptase Reversa Relação Estrutura-Atividade [Pt] Tipo de publicação: COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, U.S. GOV'T, P.H.S. [Nm] Nome de substância: 0 (Analgesics, Opioid); 0 (Oligonucleotides, Antisense); 0 (Receptors, Opioid, mu); 0 (dihydroheroin (3,6-diacetyldihydromorphine)); 70D95007SX (Heroin); 76I7G6D29C (Morphine); C3S5FRP6JW (Dihydromorphine) [Em] Mês de entrada: 0506 [Cu] Atualização por classe: 131121 [Lr] Data última revisão: 131121 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 040605 [St] Status: MEDLINE

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[PMID]: 12608825 [Au] Autor: Przybyl AK; Flippen-Anderson JL; Jacobson AE; Rice KC [Ad] Endereço: Laboratory of Medicinal Chemistry, Building 8, Room B1-22, National Institutes of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, 8 Center Drive, MSC 0815, Bethesda, Maryland 20892, USA. [Ti] Título: Practical and high-yield syntheses of dihydromorphine from tetrahydrothebaine and efficient syntheses of (8S)-8-bromomorphide. [So] Source: J Org Chem;68(5):2010-3, 2003 Mar 07. [Is] ISSN: 0022-3263 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: A practical method for the conversion of tetrahydrothebaine to dihydromorphine in 92% yield is described. The procedure should allow more efficient production of opium products and may be easily modified for large-scale synthesis. The conversion of codeine to (8S)-8-bromomorphide, a potentially valuable intermediate to 6-demethoxyoripavine and derivatives, is also described. The absolute configuration of (8S)-8-bromomorphide was determined by a single-crystal X-ray diffraction study of the hydrobromide salt. [Mh] Termos MeSH primário: Di-Hidromorfina/síntese química Derivados da Morfina/síntese química [Mh] Termos MeSH secundário: Catálise Cromatografia em Camada Delgada Cristalografia por Raios X Di-Hidromorfina/análise Indicadores e Reagentes Estrutura Molecular Derivados da Morfina/análise Estereoisomerismo Tebaína/análogos & derivados Tebaína/química [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.; RESEARCH SUPPORT, U.S. GOV'T, P.H.S. [Nm] Nome de substância: 0 (8-bromomorphide); 0 (Indicators and Reagents); 0 (Morphine Derivatives); 2P9MKG8GX7 (Thebaine); C3S5FRP6JW (Dihydromorphine) [Em] Mês de entrada: 0308 [Cu] Atualização por classe: 131121 [Lr] Data última revisão: 131121 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 030301 [St] Status: MEDLINE

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[PMID]: 12065064 [Au] Autor: Zheng M; McErlane KM; Ong MC [Ad] Endereço: Faculty of Pharmaceutical Sciences, University of British Columbia, 2146 East Mall, Vancouver, BC V6T 1Z3, Canada. [Ti] Título: Hydromorphone metabolites: isolation and identification from pooled urine samples of a cancer patient. [So] Source: Xenobiotica;32(5):427-39, 2002 May. [Is] ISSN: 0049-8254 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: 1. Hydromorphone-3-glucuronide, dihydromorphine, dihydroisomorphine, dihydromorphine-3-glucuronide and dihydroisomorphine-3-glucuronide were isolated from a cancer patient's urine and identified as metabolites of hydromorphone by comparison with synthetic standards using LC/MS/MS with gradient elution. 2. The relative urinary recovery of dihydroisomorphine-3-glucuronide was estimated to be 17-fold higher than previously reported. 3. Three new metabolites, including hydromorphone-3-sulphate, norhydromorphone and nordihydroisomorphine, were tentatively identified. [Mh] Termos MeSH primário: Analgésicos Opioides/metabolismo Hidromorfona/análogos & derivados Hidromorfona/metabolismo [Mh] Termos MeSH secundário: Analgésicos Opioides/química Analgésicos Opioides/urina Cromatografia Líquida de Alta Pressão Di-Hidromorfina/urina Feminino Glucuronatos/urina Glucuronídeos/química Glucuronídeos/urina Seres Humanos Hidromorfona/química Hidromorfona/urina Espectrometria de Massas Estrutura Molecular Neoplasias/metabolismo Neoplasias/urina [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Analgesics, Opioid); 0 (Glucuronates); 0 (Glucuronides); 0 (hydromorphone-3-glucuronide); C3S5FRP6JW (Dihydromorphine); Q812464R06 (Hydromorphone) [Em] Mês de entrada: 0207 [Cu] Atualização por classe: 131121 [Lr] Data última revisão: 131121 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 020618 [St] Status: MEDLINE

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[PMID]: 11453888 [Au] Autor: Webb JA; Rostami-Hodjegan A; Abdul-Manap R; Hofmann U; Mikus G; Kamali F [Ad] Endereço: Wolfson Unit of Clinical Pharmacology, University of Newcastle, Newcastle upon Tyne, UK. [Ti] Título: Contribution of dihydrocodeine and dihydromorphine to analgesia following dihydrocodeine administration in man: a PK-PD modelling analysis. [So] Source: Br J Clin Pharmacol;52(1):35-43, 2001 Jul. [Is] ISSN: 0306-5251 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: AIMS: It is not clear whether the analgesic effect following dihydrocodeine (DHC) administration is due to either DHC itself or its metabolite, dihydromorphine (DHM). We examined the relative contribution of DHC and DHM to analgesia following DHC administration in a group of healthy volunteers using a PK-PD link modelling approach. METHODS: A single oral dose of DHC (90 mg) was administered to 10 healthy volunteers in a randomised, double-blind, placebo-controlled study. A computerized cold pressor test (CPT) was used to measure analgesia. On each study day, the volunteers performed the CPT before study medication and at 1.25, 2.75, 4.25 and 5.75 h postdose. Blood samples were taken at 0.25 h (predose) and then at half hourly intervals for 5.75 h postdose. PK-PD link modelling was used to describe the relationships between DHC, DHM and analgesic effect. RESULTS: Mean pain AUCs following DHC administration were significantly different to those following placebo administration (P = 0.001). Mean pain AUC changes were 91 score x s(-1) for DHC and -17 score x s(-1) for placebo (95% CI = +/- 36.5 for both treatments). The assumption of a simple linear relationship between DHC concentration and effect provided a significantly better fit than the model containing DHM as the active moiety (AIC = 4.431 vs 4.668, respectively). The more complex models did not improve the likelihood of model fits significantly. CONCLUSIONS: The findings suggest that the analgesic effect following DHC ingestion is mainly attributed to the parent drug rather than its DHM metabolite. It can thus be inferred that polymorphic differences in DHC metabolism to DHM have little or no effect on the analgesic affect. [Mh] Termos MeSH primário: Analgesia Analgésicos Opioides/farmacologia Codeína/análogos & derivados Codeína/farmacologia Di-Hidromorfina/farmacologia Dor/etiologia [Mh] Termos MeSH secundário: Administração Oral Adulto Analgésicos Opioides/farmacocinética Área Sob a Curva Codeína/farmacocinética Estudos Cross-Over Di-Hidromorfina/farmacocinética Método Duplo-Cego Feminino Seres Humanos Masculino Modelos Biológicos Dor/metabolismo Medição da Dor Limiar da Dor/efeitos dos fármacos Fenômenos Fisiológicos da Pele/efeitos dos fármacos [Pt] Tipo de publicação: CLINICAL TRIAL; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL [Nm] Nome de substância: 0 (Analgesics, Opioid); C3S5FRP6JW (Dihydromorphine); N9I9HDB855 (dihydrocodeine); Q830PW7520 (Codeine) [Em] Mês de entrada: 0109 [Cu] Atualização por classe: 140613 [Lr] Data última revisão: 140613 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 010717 [St] Status: MEDLINE

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[PMID]: 11360685 [Au] Autor: Rialas CM; Weeks B; Cadet P; Goumon Y; Stefano GB [Ad] Endereço: Neuroscience Research Institute, State University of New York at Old Westbury, Old Westbury, NY 11568-0210, USA. [Ti] Título: Nociceptin, endomorphin-1 and -2 do not interact with invertebrate immune and neural mu 3 opiate receptor. [So] Source: Acta Pharmacol Sin;21(6):516-20, 2000 Jun. [Is] ISSN: 1671-4083 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: AIM: To determine if endomorphin-1, -2 and nociceptin (orphanin FQ) bind to the mu 3 opiate receptor subtype or release nitric oxide as mu 3 selective ligands do. METHODS: These opioid peptides were examined for their ability to displace [3H]dihydromorphine (DHM) binding from the invertebrate (immunocytes and pedal ganglia) mu 3 opiate receptor in membrane homogenates. The ligands were also tested for their ability to release nitric oxide from the same intact tissues utilizing an amperometric probe that measures nitric oxide in real-time. RESULTS: Endomorphin-1, -2 and nociceptin do not displace [3H]DHM binding from immunocyte or pedal ganglia membrane homogenates nor do they release nitric oxide from these tissues. CONCLUSION: Since these newly discovered opioid peptides do not interact with the mu 3 opiate receptor subtype, endogenous morphine's significance is enhanced because it appears to be the only naturally occurring opiate ligand for the receptor. Furthermore, since this study involves invertebrate tissues, this signal system had to evolve early during evolution. [Mh] Termos MeSH primário: Bivalves/metabolismo Gânglios dos Invertebrados/metabolismo Oligopeptídeos/farmacologia Peptídeos Opioides/farmacologia Receptores Opioides mu/efeitos dos fármacos [Mh] Termos MeSH secundário: Analgésicos Opioides/farmacologia Animais Ligação Competitiva Di-Hidromorfina/farmacologia Hemócitos/metabolismo Óxido Nítrico/metabolismo Receptores Opioides/agonistas [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, P.H.S. [Nm] Nome de substância: 0 (Analgesics, Opioid); 0 (Oligopeptides); 0 (Opioid Peptides); 0 (Receptors, Opioid); 0 (Receptors, Opioid, mu); 0 (endomorphin 1); 31C4KY9ESH (Nitric Oxide); 3PH5M0466G (endomorphin 2); 7AYI9N34FF (nociceptin); C3S5FRP6JW (Dihydromorphine) [Em] Mês de entrada: 0105 [Cu] Atualização por classe: 161124 [Lr] Data última revisão: 161124 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 010522 [St] Status: MEDLINE

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[PMID]: 10745087 [Au] Autor: Eckhardt K; Nevo I; Levy R; Mikus G; Eichelbaum M; Vogel Z [Ad] Endereço: Dr. Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstr. 112, 70376, Stuttgart, Germany. [Ti] Título: Morphine-related metabolites differentially activate adenylyl cyclase isozymes after acute and chronic administration. [So] Source: FEBS Lett;470(3):309-14, 2000 Mar 31. [Is] ISSN: 0014-5793 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Morphine-3- and morphine-6-glucuronide are morphine's major metabolites. As morphine-6-glucuronide produces stronger analgesia than morphine, we investigated the effects of acute and chronic morphine glucuronides on adenylyl cyclase (AC) activity. Using COS-7 cells cotransfected with representatives of the nine cloned AC isozymes, we show that AC-I and V are inhibited by acute morphine and morphine-6-glucuronide, and undergo superactivation upon chronic exposure, while AC-II is stimulated by acute and inhibited by chronic treatment. Morphine-3-glucuronide had no effect. The weak opiate agonists codeine and dihydrocodeine are also addictive. These opiates, in contrast to their 3-O-demethylated metabolites morphine and dihydromorphine (formed by cytochrome P450 2D6), demonstrated neither acute inhibition nor chronic-induced superactivation. These results suggest that metabolites of morphine (morphine-6-glucuronide) and codeine/dihydrocodeine (morphine/dihydromorphine) may contribute to the development of opiate addiction. [Mh] Termos MeSH primário: Adenilil Ciclases/metabolismo Derivados da Morfina/administração & dosagem Derivados da Morfina/farmacologia Morfina/administração & dosagem Morfina/farmacologia [Mh] Termos MeSH secundário: Inibidores de Adenilil Ciclase Adenilil Ciclases/genética Animais Células CHO Codeína/administração & dosagem Codeína/análogos & derivados Codeína/farmacologia Cricetinae Di-Hidromorfina/administração & dosagem Di-Hidromorfina/metabolismo Di-Hidromorfina/farmacologia Relação Dose-Resposta a Droga Ativação Enzimática/efeitos dos fármacos Isoenzimas/antagonistas & inibidores Isoenzimas/genética Isoenzimas/metabolismo Morfina/metabolismo Derivados da Morfina/metabolismo Transtornos Relacionados ao Uso de Opioides Receptores Opioides mu/genética Receptores Opioides mu/metabolismo Tireotropina/farmacologia Transfecção [Pt] Tipo de publicação: COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, P.H.S. [Nm] Nome de substância: 0 (Adenylyl Cyclase Inhibitors); 0 (Isoenzymes); 0 (Morphine Derivatives); 0 (Receptors, Opioid, mu); 64Y9KYM60R (morphine-6-glucuronide); 76I7G6D29C (Morphine); 9002-71-5 (Thyrotropin); C3S5FRP6JW (Dihydromorphine); EC 4.6.1.1 (Adenylyl Cyclases); O27Z9CH39A (morphine-3-glucuronide); Q830PW7520 (Codeine) [Em] Mês de entrada: 0005 [Cu] Atualização por classe: 161124 [Lr] Data última revisão: 161124 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 000404 [St] Status: MEDLINE

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