Protein Information

Name MCH1R
Synonyms G protein coupled receptor 24; GPR24; MCH receptor 1; MCH 1R; MCH R1; MCH1R; MCHR; MCHR 1…

Compound Information

Name biphenyl
CAS 1,1′-biphenyl

Reference List

PubMed Abstract RScore(About this table)
17897032 Hertzog DL, Witty DR: Biphenyl amides and isosteres as MCH R1 antagonists. . Curr Top Med Chem. 2007;7(15):1455-70.
65(0,2,2,5) Details
19137910 Cirauqui N, Ceras J, Galiano S, Perez-Silanes S, Juanenea L, Rivera G, Aldana I, Monge A: New amide derivatives as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity. Arzneimittelforschung. 2008;58(11):585-91.

The results showed that diphenyl substituents on the amide lead to better activity than biphenyl substituents.
2(0,0,0,2) Details
17897030 DeVita RJ: Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1-R) antagonists. Curr Top Med Chem. 2007;7(15):1433-9.

Improvements to the original screening lead were made by addition of lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl and hydrocinnamyl carboxamides at the 6-position.
Transposition of the 4-amino group to the 2-position of the quinoline core structure provided the 2-aminoquinoline lead class with similar MCH1R binding affinity.
2(0,0,0,2) Details
19540226 Able SL, Ivarsson M, Fish RL, Clarke TL, McCourt C, Duckworth JM, Napier C, Katugampola SD: Localisation of melanin-concentrating hormone receptor 1 in rat brain and evidence that sleep parameters are not altered despite high central receptor occupancy. Eur J Pharmacol. 2009 Aug 15;616(1-3):101-6. Epub 2009 Jun 18.


The present study describes the optimisation of an autoradiography assay that provides a means to measure the in vitro potency of melanin-concentrating hormone receptor 1 (MCH (1)) antagonists in native tissues and their ex vivo receptor occupancy.
1(0,0,0,1) Details