2. Academic Validation
  3. Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist

Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist

  • J Med Chem. 2002 Oct 10;45(21):4589-93. doi: 10.1021/jm025539h.
Iyassu K Sebhat 1,  William J Martin,  Zhixiong Ye,  Khaled Barakat,  Ralph T Mosley,  David B R Johnston,  Raman Bakshi,  Brenda Palucki,  David H Weinberg,  Tanya MacNeil,  Rubana N Kalyani,  Rui Tang,  Ralph A Stearns,  Randy R Miller,  Constantin Tamvakopoulos,  Alison M Strack,  Erin McGowan,  Doreen E Cashen,  Jennifer E Drisko,  Gary J Hom,  Andrew D Howard,  D Euan MacIntyre,  Lex H T van der Ploeg,  Arthur A Patchett,  Ravi P Nargund
Affiliations

Affiliation

  • 1 Department of Chemistry, Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065-0900, USA. iyassu_sebhat@merck.com
PMID: 12361385 DOI: 10.1021/jm025539h
Abstract

Synthetic and natural Peptides that act as nonselective Melanocortin Receptor agonists have been found to be anorexigenic and to stimulate erectile activity. We report the design and development of 1, a potent, selective (1184-fold vs MC3R, 350-fold vs MC5R), small-molecule agonist of the MC4 receptor. Pharmacological testing confirms the food intake lowering effects of MC4R agonism and suggests another role for the receptor in the stimulation of erectile activity.

Figures
Products
我们的 Cookie 政策

我们使用 Cookies 和类似技术以提高网站的性能和提升您的浏览体验，部分功能也使用 Cookies 帮助我们更好地理解您的需求，为您提供相关的服务。 如果您有任何关于我们如何处理您个人信息的疑问，请阅读我们的《隐私声明》。

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z