化合物详情

CAS33386-08-2

分子式C21H31N5O2·HCl

分子量421.964 g/mol g/mol

危化品

Buspirone hydrochloride is a hydrochloride salt resulting from the reaction of equimolar amounts of buspirone and hydrogen chloride. It has a role as an anxiolytic drug, a sedative, a serotonergic agonist and an EC 3.4.21.26 (prolyl oligopeptidase) inhibitor. It contains a buspirone(1+).

科学粮草官-词典编辑部，修订于：2026-07-06

Toxicity

Symptoms

Symptoms of overdose include dizziness, drowsiness, nausea or vomiting, severe stomach upset, and unusually small pupils.

Treatment

General symptomatic and supportive measures should be used along with immediate gastric lavage. Respiration, pulse, and blood pressure should be monitored as in all cases of drug overdosage. No specific antidote is known to buspirone, and dialyzability of buspirone has not been determined. (L1712)

Toxicity Data

LD50: 136 mg/kg (Oral, rat)

Exposure Routes

Oral. Rapidly absorbed in man. Bioavailability is low and variable (approximately 5%) due to extensive first pass metabolism.

Toxicity Summary

Buspirone binds to 5-HT type 1A serotonin receptors on presynaptic neurons in the dorsal raphe and on postsynaptic neurons in the hippocampus, thus inhibiting the firing rate of 5-HT-containing neurons in the dorsal raphe. Buspirone also binds at dopamine type 2 (DA2) receptors, blocking presynaptic dopamine receptors. Buspirone increases firing in the locus ceruleus, an area of brain where norepinephrine cell bodies are found in high concentration. The net result of buspirone actions is that serotonergic activity is suppressed while noradrenergic and dopaminergic cell firing is enhanced.

Carcinogen Classification

No indication of carcinogenicity to humans (not listed by IARC).

Drug Induced Liver Injury

References: DOI:10.1016/j.drudis.2016.02.015