| Name | melanocortin 4 receptor |
|---|---|
| Synonyms | MC4 R; MC4R; MCR receptor; Melanocortin 4 receptor; Melanocortin receptor 4; MCR receptors; Melanocortin 4 receptors; Melanocortin receptor 4s |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 16824757 | Chen CW, Tran JA, Jiang W, Tucci FC, Arellano M, Wen J, Fleck BA, Marinkovic D, White NS, Pontillo J, Saunders J, Madan A, Foster AC, Chen C: Propionylpiperazines as human melanocortin-4 receptor ligands. . Bioorg Med Chem Lett. 2006 Sep 15;16(18):4800-3. Epub 2006 Jul 7. |
2(0,0,0,2) | Details |
| 19058784 | Fujitsuka N, Asakawa A, Hayashi M, Sameshima M, Amitani H, Kojima S, Fujimiya M, Inui A: Selective reuptake inhibitors modify physiological gastrointestinal motor activities via 5-HT2c receptor and acyl ghrelin. Biol Psychiatry. 2009 May 1;65(9):748-59. Epub 2008 Dec 5. Our study identifies the importance and divergence of central 5-HT2cR pathways that regulate GI motor activities through ghrelin and feeding/energy metabolism via melanocortin 4 receptor signaling. |
1(0,0,0,1) | Details |
| 17983585 | Zhou L, Sutton GM, Rochford JJ, Semple RK, Lam DD, Oksanen LJ, Thornton-Jones ZD, Clifton PG, Yueh CY, Evans ML, McCrimmon RJ, Elmquist JK, Butler AA, Heisler LK: 2C receptor agonists improve type 2 diabetes via melanocortin-4 receptor signaling pathways. Cell Metab. 2007 Nov;6(5):398-405. |
1(0,0,0,1) | Details |
| 15740781 | Shimazaki T, Chaki S: Anxiolytic-like effect of a selective and non-peptidergic melanocortin 4 receptor antagonist, MCL0129, in a social interaction test. Pharmacol Biochem Behav. 2005 Mar;80(3):395-400. Epub 2005 Jan 16. We investigated the involvement of MC4 receptor in a social interaction test, using Ac-[Nle (4),Asp (5),D- (7),Lys (10)] alpha-MSH-(4-10)-NH2 (MT II), an MC4 receptor agonist, and 1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl) ethyl]-4-[4-(2-meth oxynaphthalen-1-yl) butyl] piperazine (MCL0129), a selective and nonpeptide MC4 receptor antagonist. |
1(0,0,0,1) | Details |
| 17267226 | Nozawa D, Okubo T, Ishii T, Takamori K, Chaki S, Okuyama S, Nakazato A: Novel piperazines: potent melanocortin-4 receptor antagonists with anxiolytic-like activity. Bioorg Med Chem. 2007 Mar 15;15(6):2375-85. Epub 2007 Jan 18. In the present study, we found that a novel piperazine compound, 11a, showed a moderate affinity (IC (50)=333nM) for the MC4 receptor. |
1(0,0,0,1) | Details |
| 17918824 | Chen C, Jiang W, Tucci F, Tran JA, Fleck BA, Hoare SR, Joppa M, Markison S, Wen J, Sai Y, Johns M, Madan A, Chen T, Chen CW, Marinkovic D, Arellano M, Saunders J, Foster AC: Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl) amino-2-methylpropyl]-4-methylphenyl] -4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl] piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia. J Med Chem. 2007 Nov 1;50(22):5249-52. Epub 2007 Oct 5. |
112(1,2,2,2) | Details |
| 15745810 | Fotsch C, Han N, Arasasingham P, Bo Y, Carmouche M, Chen N, Davis J, Goldberg MH, Hale C, Hsieh FY, Kelly MG, Liu Q, Norman MH, Smith DM, Stec M, Tamayo N, Xi N, Xu S, Bannon AW, Baumgartner JW: Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1623-7. The biological activity for a set of melanocortin-4 receptor (MC4R) agonists containing a piperazine core with an ortho-substituted aryl sulfonamide is described. |
83(1,1,1,3) | Details |
| 17162531 | Williams TM, Donnelly KB: Gastric mucosal damage following repeat administration of melanocortin subtype-4 receptor ligands to Fischer 344 rats. Toxicol Pathol. 2006;34(6):738-43. Ten structurally similar melanocortin subtype-4 receptor (MC4R) ligands from an aryl piperazine chemical platform were evaluated in female Fischer 344 rats to assess the toxicity of this class of compounds. |
81(1,1,1,1) | Details |
| 12538838 | Chaki S, Hirota S, Funakoshi T, Suzuki Y, Suetake S, Okubo T, Ishii T, Nakazato A, Okuyama S: Anxiolytic-like and antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl) ethyl]-4-[4-(2-met hoxynaphthalen-1-yl) butyl] piperazine), a novel and potent nonpeptide antagonist of the melanocortin-4 receptor. J Pharmacol Exp Ther. 2003 Feb;304(2):818-26. |
81(1,1,1,1) | Details |
| 18417348 | Chen C, Tucci FC, Jiang W, Tran JA, Fleck BA, Hoare SR, Wen J, Chen T, Johns M, Markison S, Foster AC, Marinkovic D, Chen CW, Arellano M, Harman J, Saunders J, Bozigian H, Marks D: Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists. Bioorg Med Chem. 2008 May 15;16(10):5606-18. Epub 2008 Apr 1. |
65(0,2,2,5) | Details |
| 16650763 | Briner K, Collado I, Fisher MJ, Garcia-Paredes C, Husain S, Kuklish SL, Mateo AI, O'Brien TP, Ornstein PL, Zgombick J, de Frutos O: Privileged structure based ligands for melanocortin-4 receptors--aliphatic piperazine derivatives. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3449-53. Epub 2006 May 2. |
33(0,1,1,3) | Details |
| 15317471 | Mutulis F, Yahorava S, Mutule I, Yahorau A, Liepinsh E, Kopantshuk S, Veiksina S, Tars K, Belyakov S, Mishnev A, Rinken A, Wikberg JE: New substituted piperazines as ligands for melanocortin receptors. J Med Chem. 2004 Aug 26;47(18):4613-26. A series of piperazine analogues of the melanocortin 4 receptor (MC4R) specific small-molecule agonist "THIQ" was synthesized and characterized structurally and pharmacologically. |
33(0,1,1,3) | Details |
| 14552781 | Dyck B, Parker J, Phillips T, Carter L, Murphy B, Summers R, Hermann J, Baker T, Cismowski M, Saunders J, Goodfellow V: Aryl piperazine melanocortin MC4 receptor agonists. . Bioorg Med Chem Lett. 2003 Nov 3;13(21):3793-6. Incorporation of substituted phenyl piperazine privileged structures into a known MC4 specific dipeptoid consensus sequence resulted in a series of potent (EC (50)=24 nM) and selective MC4-R agonists. |
31(0,1,1,1) | Details |
| 16169215 | Fisher MJ, Backer RT, Collado I, de Frutos O, Husain S, Hsiung HM, Kuklish SL, Mateo AI, Mullaney JT, Ornstein PL, Paredes CG, O'Brian TP, Richardson TI, Shah J, Zgombick JM, Briner K: Privileged structure based ligands for melanocortin receptors--substituted benzylic piperazine derivatives. Bioorg Med Chem Lett. 2005 Nov 15;15(22):4973-8. Replacement of the aryl piperazine moiety in compound 1 with a variety of substituted benzylic piperazines (6) yields compounds that afford melanocortin receptor 4 (MCR4) activity. |
6(0,0,1,1) | Details |
| 15615531 | Chen C, Pontillo J, Fleck BA, Gao Y, Wen J, Tran JA, Tucci FC, Marinkovic D, Foster AC, Saunders J: 4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl) propionyl}-1-{2-[(2- thienyl) ethylaminomethyl] phenyl}piperazine as a potent and selective melanocortin-4 receptor antagonist--design, synthesis, and characterization. J Med Chem. 2004 Dec 30;47(27):6821-30. |
3(0,0,0,3) | Details |
| 17964151 | Chen CW, Tran JA, Fleck BA, Tucci FC, Jiang W, Chen C: Synthesis and characterization of trans-4-(4-chlorophenyl) pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 receptor. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6825-31. Epub 2007 Oct 17. |
3(0,0,0,3) | Details |
| 16777413 | Jiang W, Tucci FC, Chen CW, Arellano M, Tran JA, White NS, Marinkovic D, Pontillo J, Fleck BA, Wen J, Saunders J, Madan A, Foster AC, Chen C: Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4674-8. Epub 2006 Jun 13. |
2(0,0,0,2) | Details |
| 15664867 | Tran JA, Pontillo J, Arellano M, White NS, Fleck BA, Marinkovic D, Tucci FC, Lanier M, Nelson J, Saunders J, Foster AC, Chen C: Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines. Bioorg Med Chem Lett. 2005 Feb 1;15(3):833-7. |
2(0,0,0,2) | Details |