Antagonism of histamine-activated adenylate cyclase in brain by D-lysergic acid diethylamide.
J P Green, C L Johnson, Harel Weinstein, Saul Maayani
Proceedings of the National Academy of Sciences December 1, 1977 DOI: 10.1073/pnas.74.12.5697 via OpenAlex
Summary
AI-generated from the abstractD-Lysergic acid diethylamide (LSD) and D-2-bromolysergic acid diethylamide (BOL) act as competitive antagonists of histamine-activated adenylate cyclase in broken cell preparations from guinea pig hippocampus and cortex. The adenylate cyclase is linked to the histamine H2-receptor. Both compounds show structural similarity to potent H2-antagonists. BOL is 10 times more potent as an H2-antagonist than cimetidine, the most potent H2-antagonist previously reported, while LSD is about equipotent to cimetidine. Blockade of H2-receptors may contribute to the behavioral effects of these compounds.
Study at a glance
| Characteristics | Experimental study Peer reviewed |
|---|---|
| Population | Guinea pig brain hippocampus and cortex cells |
| Interventions | D-Lysergic acid diethylamide D-2-bromolysergic acid diethylamide |
| Topics | LSD Serotonin |
| Keywords | Cimetidine Histamine h2 receptor Cyclase Adenylate kinase |
| Citations | 91 |
| Key finding | LSD and BOL are competitive antagonists of histamine H2-receptor-linked adenylate cyclase, with BOL being 10 times more potent than cimetidine. |
Abstract
D-Lysergic acid diethylamide and D-2-bromolysergic acid diethylamide are competitive antagonists of the histamine activation of adenylate cyclase [ATP pyrophosphate-lyase (cyclizing); E.C. 4.6.1.1] in broken cell preparations of the hippocampus and cortex of guinea pig brain. The adenylate cyclase is linked to the histamine H2-receptor. Both D-lysergic acid diethylamide and D-2-bromolysergic acid diethylamide show topological congruency with potent H2-antagonists. D-2-Bromolysergic acid diethylamide is 10 times more potent as an H2-antagonist than cimetidine, which has been the most potent H2-antagonist reported, and D-lysergic acid diethylamide is about equipotent to cimetidine. Blockade of H2-receptors could contribute to the behavioral effects of D-2-bromolysergic acid diethylamide and D-lysergic acid diethylamide.