Zobrazeno 1 - 10 of 31 pro vyhledávání: '"G. A. Brine"'
1
Ohmefentanyl and Its Stereoisomers: Chemistry and Pharmacology
Autor: G. A. Brine, F. I. Carroll, T. M. Richardson-Leibert, H. Xu, R. B. Rothman
Publikováno v: Current Medicinal Chemistry. 4:247-270
Ohmefentanyl., or β-hydroxy-3-methylfentanyl, is an unique member of the 4-anilidopiperidine class of opiates. This review summarizes both the initial studies on mixtures of ohmefentanyl stereoisomers and some more recent studies on the eight indivi
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e8991d11365d2ba5d44a48689c5c8907
https://doi.org/10.2174/0929867304666220313115017
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2
Enantiomers of Diastereomeric cis-N-[1-(2-Hydroxy-2-phenylethyl)-3-methyl-4-piperidyl]-N-phenylpropanamides: Synthesis, X-ray Analysis, and Biological Activities
Autor: P. Singh, P. A. Stark, G. A. Brine, Young Liu, Richard B. Rothman, Heng Xu, F. I. Carroll
Publikováno v: Journal of Medicinal Chemistry. 38:1547-1557
(±)-cis-N-[1-(2-Hydroxy-2-phenylethyl)-3-methyl-4-piperidyl]-N-phenylpropanamide (1) is a mixture of four stereoisomers [(2S,3R,4S)-1a, (2R,3R,4S)-1b, (2R,3S,4R)-1c, and (2S,3S,4R)-1d], which together constitute two diastereoisomeric pairs of optica
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d17fe01b9e9ed939f13e7849ba0c73f7
https://doi.org/10.1021/jm00009a015
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3
Synthesis of 4,4-disubstituted piperidine analogs of (±)-cis-N-[1-(2-hydroxy-2-phenylethyl)-3-methyl-4-piperidyl]-N-phenylpropanamide
Autor: Frank I. Carroll, P. A. Stark, G. A. Brine, P. Singh
Publikováno v: Journal of Heterocyclic Chemistry. 31:513-520
Condensation of (±)-1-benzyl-3-methyl-4-piperidone (1) with aniline followed by trapping of the intermediate imine with cyanide generated a mixture of isomeric nitriles 2A and 2B, the structures of which were established unambiguously by obtaining a
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ec3adc89898b4a8de83437e9709bdd45
https://doi.org/10.1002/jhet.5570310243
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9
Ligand-induced changes in surface mu-opioid receptor number: relationship to G protein activation?
Autor: P A, Zaki, D E, Keith, G A, Brine, F I, Carroll, C J, Evans
Publikováno v: The Journal of pharmacology and experimental therapeutics. 292(3)
In this study, we explored the relationship between regulation of surface mu-opioid receptor number, ligand-induced G protein activation (measured by [(35)]S]guanosine-5'-O-(3-thio)triphosphate (GTPgammaS) binding) and second messenger signaling (mea
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::d01743c29da10079f61172567a611096
https://pubmed.ncbi.nlm.nih.gov/10688632
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10
Opioid peptide receptor studies, 11: involvement of Tyr148, Trp318 and His319 of the rat mu-opioid receptor in binding of mu-selective ligands
Autor: H, Xu, Y F, Lu, J S, Partilla, Q X, Zheng, J B, Wang, G A, Brine, F I, Carroll, K C, Rice, K X, Chen, Z Q, Chi, R B, Rothman
Publikováno v: Synapse (New York, N.Y.). 32(1)
Previous data obtained with the cloned rat mu opioid receptor demonstrated that the "super-potent" opiates, ohmefentanyl (RTI-4614-4) and its four enantiomers, differ in binding affinity, potency, efficacy, and intrinsic efficacy. Molecular modeling
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::f99d89dc54976ddd0bb57a068f07d9d7
https://pubmed.ncbi.nlm.nih.gov/10188634
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