2. Academic Validation
  3. Design, synthesis and pharmacological evaluation of novel naphthalenic derivatives as selective MT(1) melatoninergic ligands

Design, synthesis and pharmacological evaluation of novel naphthalenic derivatives as selective MT(1) melatoninergic ligands

  • Bioorg Med Chem. 2010 May 15;18(10):3426-36. doi: 10.1016/j.bmc.2010.04.008.
Christophe Mésangeau 1,  Basile Pérès,  Carole Descamps-François,  Philippe Chavatte,  Valérie Audinot,  Sophie Coumailleau,  Jean A Boutin,  Philippe Delagrange,  Caroline Bennejean,  Pierre Renard,  Daniel H Caignard,  Pascal Berthelot,  Saïd Yous
Affiliations

Affiliation

  • 1 Univ Lille Nord de France, F-59000 Lille, France.
PMID: 20444610 DOI: 10.1016/j.bmc.2010.04.008
Abstract

Novel heterodimer analogues of melatonin were synthesized, when agomelatine (1) and various aryl units are linked via a linear alkyl chain through the methoxy group. The compounds were tested for their actions at melatonin receptors. Several of these ligands are MT(1)-selective with nanomolar or subnanomolar affinity. In addition, while most of the derivatives behave as partial agonists on one or both receptor subtypes, N-[2-(7-{4-[6-(1-methoxycarbonylethyl)naphthalen-2-yloxy]butoxy}naphthalen-1-yl)ethyl]acetamide (36), a subnanomolar MT(1) ligand with an 11-fold preference over MT(2) receptors, is a full antagonist on both receptors. Our results also confirm that the selectivity seen for the MT(1) receptor arises predominantly from steric factors and is not a consequence of the bridging of Melatonin Receptor dimers.

Figures
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