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Complex Interaction of a 2 ‐Adrenoceptor Binding Sites with Bovine Brain and Lung Extracts Containing Clonidine‐Displacing Substance
Author(s) -
PINTHONG D,
KENDALL DA,
WILSON VG
Publication year - 2003
Publication title -
annals of the new york academy of sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.712
H-Index - 248
eISSN - 1749-6632
pISSN - 0077-8923
DOI - 10.1196/annals.1304.026
Subject(s) - potency , chemistry , clonidine , agonist , antagonist , binding site , histamine , pharmacology , adrenergic receptor , stereochemistry , receptor , lung , endocrinology , medicine , biochemistry , in vitro
A bstract : Previous studies have established that methanolic extracts of bovine brain and lung possess CDS activity with an agonist‐like profile at a 2 ‐adrenoceptor binding sites (i.e., greater potency against [ 3 H]‐clonidine sites than against [ 3 H]‐RX‐821001 sites). Following prolonged reflux in ethylacetate, monovalent cations and histamine were removed from the lung extract, and the resulting extract exhibited similar potency against both radioligands, indicative of an antagonist‐like profile. These observations help explain the absence of biologic activity at a 2 ‐adrenoceptors in the methanolic extracts as reported in our companion paper.