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THE NATURE OF THE BINDING BETWEEN LSD AND A 5‐HT RECEPTOR: A POSSIBLE EXPLANATION FOR HALLUCINOGENIC ACTIVITY

M J Berridge, William D. Prince

British Journal of Pharmacology June 1, 1974 DOI: 10.1111/j.1476-5381.1974.tb09657.x (opens in new tab)

Study at a glance

AI-extracted from the abstract
Characteristics Experimental study Peer reviewed
Population Isolated salivary glands of Calliphora (blowfly)
Interventions LSD tryptamine gramine
Topics LSD Serotonin
Keywords Tryptamine Agonist Hallucinogen Endocrinology 5-HT Receptor Pharmacology
Citations 26
Key findings LSD acts as a slow-dissociating agonist at serotonin receptors in blowfly salivary glands, which may underlie its potent central nervous system effects.

Abstract

(+)‐Lysergic acid diethylamide (LSD) mimicked 5‐hydroxytryptamine (5‐HT) in its ability to stimulate fluid secretion, to change transepithelial and intracellular potentials as well as to increase the cyclic 3′,5′‐adenosine monophosphate (cyclic AMP) concentrations of isolated salivary glands of Calliphora . Unlike 5‐HT, LSD disengages slowly from the receptor and fluid secretion continues despite repeated washing. Both 5‐HT and tryptamine prevented LSD from acting on the glands. LSD bound to the receptor was slowly displaced when glands were treated with agonists (tryptamine) or antagonists (gramine). The property of LSD which permits it to function as an agonist despite remaining tightly bound to the receptor is discussed as a possible basis for its profound effects within the central nervous system.

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

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