Characterisation of [3H]lysergic acid diethylamide binding to a 5-hydroxytryptamine receptor on human platelet membranes
David P. Geaney, Michael Schächter, Jonathan Elliot, David G. Grahame‐smith
European Journal of Pharmacology 1984 DOI: 10.1016/0014-2999(84)90515-6 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Observational study Peer reviewed |
|---|---|
| Sample size | 19 |
| Population | Human control subjects |
| Topics | LSD Serotonin |
| Keywords | Spiperone Membrane Platelet Receptor Binding site Biophysics Stereochemistry Biochemistry |
| Citations | 90 |
| Key findings | Specific [3H]LSD binding to human platelet membranes has characteristics of a 5-HT receptor and correlates with binding in human frontal cortex. |
Abstract
Specific binding of [3H]lysergic acid diethylamide (LSD) to human platelet membranes, as defined by 300 nM spiperone, was saturable over the concentration range of 0.25-2.5 nM [3H]LSD. At 0.5 nM [3H]LSD the half-time for association at 37 degrees C was 56 min, half-time for dissociation was 173 min, and the kinetically derived affinity was 0.24 nM. In 19 control subjects equilibrium binding studies gave an affinity of 0.53 +/- 0.02 nM (mean +/- S.E.M.) and capacity of 57.1 +/- 5.6 fmol/mg protein (mean +/- S.E.M.). The inhibition profile was consistent with that of a 5-hydroxytryptamine (5-HT) receptor. There was a significant correlation between the inhibition of [3H]LSD binding and the inhibition of 5-HT-induced shape change, but not inhibition of active platelet uptake of 5-HT. There was also a significant correlation between the inhibition of [3H]LSD binding to human platelet membranes and human frontal cortex. Platelet [3H]LSD binding may therefore be a useful model for study of peripheral and central 5-HT receptors in man.
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| Psychedelics not linked to mental health problems or suicidal behavior: A population study Randomly selected United States adults | 2015 | Observational cohort | n = 135,095 |
| Whole-Brain Multimodal Neuroimaging Model Using Serotonin Receptor Maps Explains Non-linear Functional Effects of LSD. Healthy human participants | 2018 | Observational study with computational modeling |
Citations in the library
Cited by 4
- Increased serotonin2 (5-HT2) receptor binding as measured by 3H-lysergic acid diethylamide (3H-LSD) in the blood platelets of depressed patients Life Sciences 1989
- Increased platelet membrane [3H]‐LSD binding in patients on chronic neuroleptic treatment. British Journal of Clinical Pharmacology April 1, 1985
- Human platelet 5-hydroxytryptamine receptors: Binding of [3H]-lysergic acid diethylamide (LSD). Effects of chronic neuroleptic and antidepressant drug administration Cellular and Molecular Life Sciences February 1, 1988
- Lysergic acid diethylamide is a partial agonist at 5-HT2 receptors in ovine uterine artery of late pregnancy European Journal of Pharmacology January 5, 1993
Cites 3
- Stereospecific binding ofd-lysergic acid diethylamide (LSD) to brain membranes: Relationship to serotonin receptors Brain Research September 1, 1975
- SHAPE CHANGE OF BLOOD PLATELETS—A MODEL FOR CEREBRAL 5‐HYDROXYTRYPTAMINE RECEPTORS? British Journal of Pharmacology April 1, 1979
- Interaction of D-LSD with blood platelets of rabbits: shape change and specific binding. Journal of Pharmacology and Experimental Therapeutics February 1, 1981