SHAPE CHANGE OF BLOOD PLATELETS—A MODEL FOR CEREBRAL 5‐HYDROXYTRYPTAMINE RECEPTORS?
British Journal of Pharmacology April 1, 1979 DOI: 10.1111/j.1476-5381.1979.tb07870.x (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Experimental study Peer reviewed |
|---|---|
| Population | Rabbit blood platelets |
| Interventions | tryptamine quipazine mescaline methysergide ergoline derivatives neuroleptic drugs LSD psilocine N' |
| Topics | Serotonin |
| Keywords | Platelet Receptor |
| Citations | 45 |
| Key findings | Platelet serotonin receptors show similarities to some central nervous system serotonin receptors but differ from others, suggesting platelets can model only certain central serotonin receptor subtypes. |
Abstract
In blood platelets of rabbits isolated by a stractan gradient and incubated in a protein‐poor medium, tryptamine, 5‐hydroxytryptamine (5‐HT) and derivatives, quipazine and mescaline caused a shape change. This shape change was inhibited by low concentrations of methysergide. The most potent antagonists of the 5‐HT‐induced shape change included ergoline derivatives and neuroleptic drugs, which showed high stereoselectivity. (‐f)‐Lysergic acid diethylamide ((+)‐LSD), psilocine and some N',N′‐dimethylated tryptamines acted as mixed agonist‐antagonists. The compounds found to be agonists or mixed agonist‐antagonists on platelets have previously been shown to act also as 5‐HT agonists in the central nervous system (CNS). With regard to 5‐HT antagonists, the 5‐HT receptors of platelets reacted differently from those described earlier in brain areas with dense 5‐hydroxytryptaminergic innervation, but showed similarities to 5‐HT receptors investigated previously in spinal cord, cerebral cortex and possibly reticular formation. It is concluded that platelets may be considered with caution as models for some, but not for all, 5‐HT receptors in the CNS.