QUINUCLIDIN-2-ENE - BASED MUSCARINIC ANTAGONISTS

Authors
HACKSELL U NILSSON BM NORDVALL G JOHANSSON G SUNDQUIST S NILVEBRANT L
Citation
U. Hacksell et al., QUINUCLIDIN-2-ENE - BASED MUSCARINIC ANTAGONISTS, Life sciences, 56(11-12), 1995, pp. 831-836
Citations number
11
Categorie Soggetti
Biology,"Medicine, Research & Experimental","Pharmacology & Pharmacy
Journal title
Life sciences → ACNP
ISSN journal
00243205
Volume
56
Issue
11-12
Year of publication
1995
Pages
831 - 836
Database
ISI
SICI code
0024-3205(1995)56:11-12<831:Q-BMA>2.0.ZU;2-J
Abstract
A series of achiral 3-heteroaryl substituted quinuclidin-2-ene derivat ives and related compounds have been synthesized by facile methods. Th e compounds were evaluated for muscarinic and antimuscarinic propertie s in receptor binding studies using (-)-[H-3]-QNB as the radioligand a nd ina functional assay using isolated guinea pig urinary bladder. 3-( 2-Benzofuranyl)-quinuclidin-2-ene (15) displayed the highest M(1)-rece ptor affinity in the present series (K-i = 9.6 nM).