Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines |
| |
Authors: | Tran Joe A Pontillo Joseph Arellano Melissa White Nicole S Fleck Beth A Marinkovic Dragan Tucci Fabio C Lanier Marion Nelson Jodie Saunders John Foster Alan C Chen Chen |
| |
Affiliation: | Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., El Camino Real, San Diego, CA 92130, USA. |
| |
Abstract: | SAR studies of a series of piperazinebenzylamines resulted in identification of potent agonists and antagonists of the human melanocortin-4 receptor. Thus, the 1,2,3,4-tetrahydroisoquinolin-1-ylacetyl compound 12e and the quinolin-3-ylcarbonyl analogue 12l possessed K(i) values of 6.3 and 4.5 nM, respectively. Interestingly, 12e was a full agonist with an EC(50) value of 31 nM, and 12l was a weak partial agonist (IA=17%) and functioned as an antagonist (IC(50)=300 nM). |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|