2. Academic Validation
  3. Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders

Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders

  • J Med Chem. 2006 Jan 12;49(1):35-8. doi: 10.1021/jm051065l.
Simon C Goodacre 1,  Leslie J Street,  David J Hallett,  James M Crawforth,  Sarah Kelly,  Andrew P Owens,  Wesley P Blackaby,  Richard T Lewis,  Joanna Stanley,  Alison J Smith,  Pushpinder Ferris,  Bindi Sohal,  Susan M Cook,  Andrew Pike,  Nicola Brown,  Keith A Wafford,  George Marshall,  José L Castro,  John R Atack
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Sharp Laboratory, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, UK.
PMID: 16392789 DOI: 10.1021/jm051065l
Abstract

A series of high-affinity GABA(A) agonists with good oral bioavailability in rat and dog and functional selectivity for the GABA(A)alpha2 and -alpha3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimidine 14k are anxiolytic in both conditioned and unconditioned animal models of anxiety with minimal sedation observed at full BZ binding site occupancy.

Figures
Products
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