| Name | Growth hormone secretagogues |
|---|---|
| Synonyms | Appetite regulating hormone; Appetite regulating hormone precursor; GHRL; Ghrelin; Growth hormone releasing peptide; Growth hormone secretagogue; M46 protein; MTLRP… |
| Name | biphenyl |
|---|---|
| CAS | 1,1′-biphenyl |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 19625579 | Bennett KA, Langmead CJ, Wise A, Milligan G: Growth hormone secretagogues and growth hormone releasing peptides act as orthosteric super-agonists but not allosteric regulators for activation of the G protein Galpha (o1) by the Ghrelin receptor. Mol Pharmacol. 2009 Oct;76(4):802-11. Epub 2009 Jul 22. In membranes prepared from cells coexpressing the human ghrelin receptor and the G protein Galpha (o1), N-[1 (R)-1, 2-dihydro-1-ethanesulfonylspiro-3H--3,4'-piperidin)-1'-yl] carbonyl-2 -(phenylmethoxy)-ethyl-2-amino-2-methylpropanamide (MK-677), growth hormone-releasing peptide 6 (GHRP-6), and the 2 (R)-hydroxypropyl derivative of 3-amino-3-methyl-N-(2,3,4,5-tetrahydro-2-oxo-1-([2'-(1H-tetrazol-5-yl) (1,1'-biphenyl)-4-yl] methyl)-1H-1-benzazepin-3 (R)-yl)-butanamide (L-692,585) each functioned as direct agonists, and each displayed higher efficacy than ghrelin. |
85(1,1,1,5) | Details |
| 18923064 | Holst B, Frimurer TM, Mokrosinski J, Halkjaer T, Cullberg KB, Underwood CR, Schwartz TW: Overlapping binding site for the endogenous agonist, small-molecule agonists, and ago-allosteric modulators on the ghrelin receptor. Mol Pharmacol. 2009 Jan;75(1):44-59. Epub 2008 Oct 15. A library of robust ghrelin receptor mutants with single substitutions at 22 positions in the main ligand-binding pocket was employed to map binding sites for six different agonists: two peptides (the 28-amino-acid octanoylated endogenous ligand ghrelin and the hexapeptide growth hormone secretagogue GHRP-6) plus four nonpeptide agonists-the original benzolactam L-692,429 [3-amino-3-methyl-N-(2,3,4,5-tetrahydro-2-oxo-1-([2'-(1H-tetrazol-5-yl) (1,1'-biphenyl)-4-yl] methyl)-1H-1-benzazepin-3 (R)-yl)-butanamide], the spiroindoline sulfonamide MK-677 [N-[1 (R)-1, 2-dihydro-1-ethanesulfonylspiro-3H--3,4'-piperidin)-1'-yl] carbonyl-2 -(phenylmethoxy)-ethyl-2-amino-2-methylpropanamide], and two novel oxindole derivatives, SM-130686 [(+)-6-carbamoyl-3-(2-chlorophenyl)-(2-diethylaminoethyl)-4-trifluoromethy loxindole] and SM-157740 [(+/-)-6-carbamoyl-3-(2, 4-dichlorophenyl)-(2-diethylaminoethyl)-4-trifluoromethyloxindole)]. |
31(0,1,1,1) | Details |
| 18295486 | Li J, Chen SY, Tao S, Wang H, Li JJ, Swartz S, Musial C, Hernandez AA, Flynn N, Murphy BJ, Beehler B, Dickinson KE, Giupponi L, Grover G, Seethala R, Sleph P, Slusarchyk D, Yan M, Humphreys WG, Zhang H, Ewing WR, Robl JA, Gordon D, Tino JA: Design and synthesis of tetrazole-based growth hormone secretagogue: the SAR studies of the O-benzyl serine side chain. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1825-9. Epub 2008 Feb 13. Among them, the biphenyl compound 2p shows twofold improvement in potency compared to its parent compound BMS-317180 (2). |
2(0,0,0,2) | Details |