학술논문

Initial Evaluation of Novel Selective Ligands for Imidazoline2 Receptors in Rat Whole Brain
Document Type
Academic Journal
Source
Annals of the New York Academy of Sciences. Jan 01, 2003 1009:357-360
Subject
Language
English
ISSN
0077-8923
Abstract
Indazim, the indazole analogue of 2BFI, and four methyl-substituted analogues were tested for their affinity at the imidazoline2 binding site (I2-BS), and this affinity was compared with their affinity at the α2-adrenoceptor to determine their structure, affinity relationship, and selectivity at the I2-BS. These studies showed that these ligands were highly selective for the I2-BS compared with 2BFI and that substitution at the 4 and 7 positions increased affinity without affecting selectivity.