Title : Design and synthesis of propranolol analogues as serotonergic agents.

Pub. Date : 1989 Apr

PMID : 2539480






3 Functional Relationships(s)
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1 The beta-adrenergic antagonist propranolol binds stereoselectively both at 5-HT1A and 5-HT1B sites (with a several-fold selectivity for the latter) and, whereas it is a 5-HT1A antagonist, it appears to be a 5-HT1B agonist. Propranolol 5-hydroxytryptamine receptor 1B Homo sapiens
2 The purpose of the present study was to modify the structure of propranolol in such a manner so as to reduce its affinity for 5-HT1B and beta-adrenergic sites while, at the same time, retaining its affinity for 5-HT1A sites. Propranolol 5-hydroxytryptamine receptor 1B Homo sapiens
3 Removal of the side-chain hydroxyl group of propranolol, and conversion of its secondary amine to a tertiary amine, reduced affinity for 5-HT1B and beta-adrenergic sites. Propranolol 5-hydroxytryptamine receptor 1B Homo sapiens