Abstract
Human platelets contain α2-adrenoceptors which are negatively coupled to the enzyme adenylate cyclase. In order to better understand the interaction of this subtype of α receptor with this key enzyme, we have initiated a program to isolate and characterize the a2-adrenoceptor. This report describes the synthesis and biological characterization of a series of molecules that were prepared as affinity ligands for this purpose. The best of these is 9-(allyloxy)-6-chloro-3-methyl-2, 3,4, 5-tetrahydro-1H-3-benzazepine (SK&F 101253). This compound is an α2-adrenoceptor antagonist, which was obtained by synthetic modification of 6-chloro-3-methyl-2, 3,4, 5-tetrahydro-lH-3-benzazepine (SK&F 86466), a novel antagonist with high affinity for the α2-receptor.
Original language | English (US) |
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Pages (from-to) | 918-921 |
Number of pages | 4 |
Journal | Journal of Medicinal Chemistry |
Volume | 27 |
Issue number | 7 |
DOIs | |
State | Published - Oct 1984 |
Externally published | Yes |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery