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Mescaline effects on rat behavior and its time profile in serum and brain tissue after a single subcutaneous dose

Tomáš Páleníček, Marie Balı́ková, Vĕra Bubeníková‐valešová, Jiřı́ Horáček

Psychopharmacology October 6, 2007 DOI: 10.1007/s00213-007-0926-5 via OpenAlex

Summary

AI-generated from the abstract

Mescaline, a nonselective serotonin receptor agonist, produced significant inhibitory effects on locomotion in rats at low doses and a biphasic effect at the highest dose. In tests of sensorimotor gating (prepulse inhibition of acoustic startle), all doses disrupted gating only when tested 60 minutes after administration. Approximately 50% of animals receiving 100 mg/kg died within 12 hours. Serum mescaline levels rose rapidly within 30 minutes and then quickly declined, while brain concentrations peaked 1 hour after administration and remained elevated for another 60 minutes. The delayed onset of behavioral changes correlated with the drug's pharmacokinetics.

Study at a glance

Characteristics Experimental study Peer reviewed
Population Rats
Intervention Mescaline
Dose 10, 20, and 100 mg/kg subcutaneously
Duration 15 and 60 minutes post-administration for behavioral tests; up to 12 hours for mortality observation; pharmacokinetics measured over time up to 60 minutes post-peak brain concentration
Topics Mescaline
Keywords Prepulse inhibition Pharmacology Pharmacokinetics Open field
Citations 61
Key finding Mescaline produced delayed behavioral effects—inhibitory on locomotion at low doses and biphasic at the highest dose, and disrupted prepulse inhibition only at 60 minutes post-injection—which correlated with its pharmacokinetics in serum and brain.

Abstract

RationaleMescaline is a nonselective serotonin receptor agonist. It has relatively delayed onset of action and prolonged duration. Mescaline attenuates various behavioral parameters in rats; however, no information is available about its pharmacokinetics in rats and its relation to the behavioral changes produced by the drug.ObjectivesThe present study evaluates the spontaneous locomotor activity and sensorimotor gating in relation to mescaline concentrations in the serum and the brain of ratsMaterials and methodsBehavioral changes induced by mescaline [10, 20, and 100 mg/kg subcutaneously (s.c.)] were evaluated in an open-field test and testing of the prepulse inhibition of acoustic startle reaction (PPI) 15 and 60 min after drug administration. The time disposition of mescaline 20 mg/kg s.c. in rat serum and brain homogenates was analyzed by gas chromatography-mass spectrometry.ResultsMescaline produced significant inhibitory effects on locomotion in low doses and a biphasic effect with the highest dose. In the PPI test, only when tested 60 min after drug administration, all doses of mescaline disrupted PPI. Besides the experimental protocol, we have observed that approximately 50% of animals receiving 100 mg/kg died within 12 h post-injection. The serum levels of mescaline rapidly increased within 30 min and subsequently quickly decreased; however, the brain concentrations reached a maximum 1 h after administration and remained high for an additional 60 min.ConclusionsMescaline had a delayed onset of the main behavioral changes in rats compared to other hallucinogens. Behavioral changes correlated with the pharmacokinetics of the drug.

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