Naunyn-Schmiedeberg's archives of pharmacology
January 1, 2024
Ulrich Gergs, Hannes Jacob, Pauline Braekow et al.
16 citations
Lysergic acid diethylamide (LSD) increases the force and rate of heart contractions by activating two types of receptors: 5-HT4 serotonin receptors and H2 histamine receptors. In transgenic mouse hearts overexpressing human 5-HT4 or H2 receptors, LSD (up to 10 µM) increased contraction force and beating rate, effects blocked by specific antagonists (tropisetron for 5-HT4, cimetidine and GR 125487 for H2). In human atrial muscle strips from bypass surgery patients, LSD (10 µM) also increased contraction force after cilostamide pre-stimulation. These findings indicate LSD directly stimulates cardiac function through both receptor pathways.
Frontiers in Pharmacology
February 2, 2024
Joachim Neumann, Stefan Dhein, Uwe Kirchhefer et al.
12 citations
Hallucinogenic drugs like LSD, psilocybin, and DMT affect the brain by stimulating serotonin receptors, particularly 5-HT2A receptors, which likely causes their hallucinogenic effects. However, these drugs also act on the heart, potentially increasing the force of contraction and heart rate, and may lead to arrhythmias. This review examines the inotropic and chronotropic actions of bufotenin, psilocin, psilocybin, LSD, ergotamine, ergometrine, N,N-dimethyltryptamine, and 5-methoxy-N,N-dimethyltryptamine in the human heart.
Research Square
Ulrich Gergs, Hannes Jacob, Pauline Braekow et al.
1 citation
LSD increases the force and rate of heart muscle contraction by activating H2-histamine receptors in humans, and also acts as a partial agonist at 5-HT4 serotonin receptors in mice. In human atrial tissue from heart surgery patients, LSD's contractile effects were blocked by cimetidine, an H2-receptor antagonist. These findings clarify the cardiac effects of LSD, which is being studied again for psychiatric uses.
Pharmaceuticals
July 6, 2025
Pauline Braekow, Joachim Neumann, Uwe Kirchhefer et al.
Psilocybin and psilocin enhance the force of contraction and increase phospholamban phosphorylation in isolated mouse hearts that overexpress human 5-HT4 receptors, but have little effect in hearts overexpressing human H2 receptors. LSD increases both force and phosphorylation in hearts with either receptor. Ergometrine and ergotamine only increase force in H2-receptor-overexpressing hearts, with ergometrine also increasing phosphorylation. None of these substances affect force or phosphorylation in wild-type mouse hearts. The findings suggest that phospholamban phosphorylation partly explains the positive inotropic and relaxant effects of these hallucinogenic compounds in these animal models.