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 (opens in new tab)
Study at a glance
AI-extracted from the abstract| 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 Antagonist Pharmacology Endocrinology Biochemistry |
| Citations | 91 |
| Key findings | 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.
Comparable studies
Other experimental studies on LSD, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| Neural correlates of the LSD experience revealed by multimodal neuroimaging. Human participants | 2016 | Experimental study | |
| Crystal structure of an LSD-bound human serotonin receptor | 2017 | Experimental study with structural biology and molecular dynamics simulations | |
| Lysergic Acid Diethylamide: Sensitive Neuronal Units in the Midbrain Raphe Midbrain neurons containing serotonin | 1968 | Experimental study | |
| Connectome-harmonic decomposition of human brain activity reveals dynamical repertoire re-organization under LSD. Human brain | 2017 | Experimental study | |
| LSD-Assisted Psychotherapy in Patients with Terminal Cancer Cancer patients | 1973 | Experimental study | n = 60 |
Citations in the library
Cited by 4
- Localization of serotonin 5‐HT2 receptors in living human brain by positron emission tomography using N1‐([11C]‐methyl)‐2‐BR‐LSD Synapse 1987
- Effects of hallucinogenic drugs on the human heart Frontiers in Pharmacology February 2, 2024
- TCB-2 [(7R)-3-bromo-2, 5-dimethoxy-bicyclo[4.2.0]octa-1,3,5-trien-7-yl]methanamine]: A hallucinogenic drug, a selective 5-HT2A receptor pharmacological tool, or none of the above? Neuropharmacology November 2018
- Selective labeling of serotonin receptors by d-[3H]lysergic acid diethylamide in calf caudate. Proceedings of the National Academy of Sciences December 1, 1978
Cites 5
- THE DISTRIBUTION AND METABOLISM OF LYSERGIC ACID DIETHYLAMIDE Annals of the New York Academy of Sciences March 1, 1957
- Stereospecific receptor sites for d-lysergic acid diethylamide in rat brain: effects of neurotransmitters, amine antagonists, and other psychotropic drugs. Molecular Pharmacology July 1, 1976
- Psychopathology and Psychophysiology of Minimal LSD-25 Dosage A M A Archives of Neurology & Psychiatry February 1, 1958
- Lysergic Acid Diethylamide (LSD-25) Antagonists A M A Archives of Neurology & Psychiatry February 1, 1958
- Comparative effects of hallucinogenic drugs on rotational behavior in rats with unilateral 6-hydroxydopamine lesions. European Journal of Pharmacology July 15, 1977