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The following term was not found in PubMed: 3-bromo-4-sulfamoyl-phenyl
Page 1
Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764).
Wager TT, Pettersen BA, Schmidt AW, Spracklin DK, Mente S, Butler TW, Howard H, Lettiere DJ, Rubitski DM, Wong DF, Nedza FM, Nelson FR, Rollema H, Raggon JW, Aubrecht J, Freeman JK, Marcek JM, Cianfrogna J, Cook KW, James LC, Chatman LA, Iredale PA, Banker MJ, Homiski ML, Munzner JB, Chandrasekaran RY. Wager TT, et al. J Med Chem. 2011 Nov 10;54(21):7602-20. doi: 10.1021/jm200939b. Epub 2011 Oct 7. J Med Chem. 2011. PMID: 21928839
Ligand efficacy and potency at recombinant human MT2 melatonin receptors: evidence for agonist activity of some mt1-antagonists.
Nonno R, Pannacci M, Lucini V, Angeloni D, Fraschini F, Stankov BM. Nonno R, et al. Br J Pharmacol. 1999 Jul;127(5):1288-94. doi: 10.1038/sj.bjp.0702658. Br J Pharmacol. 1999. PMID: 10455277 Free PMC article.
The order of apparent affinity for selected compounds was: 4-phenyl-2-propionamidotetralin (4P-PDOT) > 2-phenylmelatonin > 2-iodomelatonin > 2-bromomelatonin > 6-chloromelatonin > or = melatonin > luzindole > N-acetyl-tryptamine > or = N-[(2- …
The order of apparent affinity for selected compounds was: 4-phenyl-2-propionamidotetralin (4P-PDOT) > 2-phenylmelatonin > 2-iodomelat …
Characterization of a melatonin binding site in Siberian hamster brown adipose tissue.
Le Gouic S, Atgié C, Viguerie-Bascands N, Hanoun N, Larrouy D, Ambid L, Raimbault S, Ricquier D, Delagrange P, Guardiola-Lemaitre B, Pénicaud L, Casteilla L. Le Gouic S, et al. Eur J Pharmacol. 1997 Nov 27;339(2-3):271-8. doi: 10.1016/s0014-2999(97)01373-3. Eur J Pharmacol. 1997. PMID: 9473145
The rank order of potency of a variety of drugs to displace 2-[125I]iodomelatonin from binding sites on Siberian hamster brown adipose tissue was as follows: 2-iodomelatonin > melatonin = prazosin > GR135531 (5-methoxycarbonylamino-N-acetyltryptamine) > N-a …
The rank order of potency of a variety of drugs to displace 2-[125I]iodomelatonin from binding sites on Siberian hamster brown adipose tissu …
Quantitative projection of human brain penetration of the H3 antagonist PF-03654746 by integrating rat-derived brain partitioning and PET receptor occupancy.
Sawant-Basak A, Chen L, Shaffer CL, Palumbo D, Schmidt A, Tseng E, Spracklin DK, Gallezot JD, Labaree D, Nabulsi N, Huang Y, Carson RE, McCarthy T. Sawant-Basak A, et al. Xenobiotica. 2017 Feb;47(2):119-126. doi: 10.3109/00498254.2016.1166531. Epub 2016 Jun 29. Xenobiotica. 2017. PMID: 27353353
Unbound brain drug concentration (C(b,u)), a valid surrogate of interstitial fluid drug concentration (C(ISF)), cannot be directly determined in humans, which limits accurately defining the human C(b,u):C(p,u) of investigational molecules. 2. For the H(3)R antagonist (1R,3R)-N …
Unbound brain drug concentration (C(b,u)), a valid surrogate of interstitial fluid drug concentration (C(ISF)), cannot be directly determine …
Direct bis-arylation of cyclobutanecarboxamide via double C-H activation: an auxiliary-aided diastereoselective Pd-catalyzed access to trisubstituted cyclobutane scaffolds having three contiguous stereocenters and an all-cis stereochemistry.
Parella R, Gopalakrishnan B, Babu SA. Parella R, et al. J Org Chem. 2013 Dec 6;78(23):11911-34. doi: 10.1021/jo4019733. Epub 2013 Nov 20. J Org Chem. 2013. PMID: 24188021
The auxiliary-attached cyclobutanecarboxamides 15a, 15g, and 15h, prepared from the auxiliaries such as, 8-aminoquinoline, 2-(methylthio)aniline, and N',N'-dimethylethane-1,2-diamine were found to undergo an efficient direct bis-arylation. The Pd-catalyzed arylation …
The auxiliary-attached cyclobutanecarboxamides 15a, 15g, and 15h, prepared from the auxiliaries such as, 8-aminoquinoline, 2-(methylthio)ani …
Vasoconstrictor effects of various melatonin analogs on the rat tail artery in the presence of phenylephrine.
Bucher B, Gauer F, Pévet P, Masson-Pévet M. Bucher B, et al. J Cardiovasc Pharmacol. 1999 Feb;33(2):316-22. doi: 10.1097/00005344-199902000-00021. J Cardiovasc Pharmacol. 1999. PMID: 10028943
We performed a pharmacologic analysis of the increase in perfusion pressure induced by melatonin and related analogues in the perfused rat tail artery precontracted by 1 microM phenylephrine. Melatonin, 2-iodomelatonin, 6-chloromelatonin, and S20098 (N-[2-(7-methoxy-1-naph …
We performed a pharmacologic analysis of the increase in perfusion pressure induced by melatonin and related analogues in the perfused rat t …
Methods for the evaluation of drug action at the human melatonin receptor subtypes.
Nonno R, Fraschini F, Stankov BM. Nonno R, et al. Biol Signals Recept. 1999 Jan-Apr;8(1-2):32-40. doi: 10.1159/000014566. Biol Signals Recept. 1999. PMID: 10085460
Luzindole did not increase basal [35S]GTPgammaS binding but competitively inhibited melatonin-stimulated [35S]GTPgammaS binding, thus exhibiting antagonist action. Two other mt1 antagonists, 4P-PDOT and N-[(2-phenyl-1H-indol-3-yl)ethyl]cyclobutanecarboxamide, behave …
Luzindole did not increase basal [35S]GTPgammaS binding but competitively inhibited melatonin-stimulated [35S]GTPgammaS binding, thus exhibi …
Pharmacological characterization of the human melatonin Mel1a receptor following stable transfection into NIH3T3 cells.
Nonno R, Lucini V, Pannacci M, Mazzucchelli C, Angeloni D, Fraschini F, Stankov BM. Nonno R, et al. Br J Pharmacol. 1998 Jun;124(3):485-92. doi: 10.1038/sj.bjp.0701860. Br J Pharmacol. 1998. PMID: 9647472 Free PMC article.
The full agonists 2-phenylmelatonin, 2-bromomelatonin and 6-chloromelatonin equally induced an increase of the GDP-GTP exchange. 5-Hydroxy-N-acetyltryptamine activated the GTP-GDP exchange to a much lesser extent (53%) than melatonin, thus behaving as a partial agonist. As …
The full agonists 2-phenylmelatonin, 2-bromomelatonin and 6-chloromelatonin equally induced an increase of the GDP-GTP exchange. 5-Hydroxy- …
26 results