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Details

Stereochemistry ACHIRAL
Molecular Formula C21H31N5O2.ClH
Molecular Weight 421.9648
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BUSPIRONE HYDROCHLORIDE

SMILES

C1CCC2(C1)CC(=O)N(CCCCN3CCN(CC3)c4ncccn4)C(=O)C2.Cl

InChI

InChIKey=RICLFGYGYQXUFH-UHFFFAOYSA-N
InChI=1S/C21H31N5O2.ClH/c27-18-16-21(6-1-2-7-21)17-19(28)26(18)11-4-3-10-24-12-14-25(15-13-24)20-22-8-5-9-23-20;/h5,8-9H,1-4,6-7,10-17H2;1H

HIDE SMILES / InChI

Molecular Formula C21H31N5O2
Molecular Weight 385.5039
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula ClH
Molecular Weight 36.4609
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: https://www.ncbi.nlm.nih.gov/pubmed/6151170

Buspirone is the first of a new class of anxioselective agents, the azaspirodecanediones. Animal studies have suggested antianxiety activity and the absence of abuse potential. Behavioural, electrophysiological and receptor binding experiments gradually led to the idea that buspirone owes much of its anxiolytic activity to its ability to attenuate central 5-hydroxytryptamine neurotransmission. In vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. The drug was approved by FDA for the treatment of anxiety.

Originator

Sources: ISBN-13: 978-1285845227

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
24 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
BUSPIRONE HYDROCHLORIDE

Approved Use

Buspirone hydrochloride tablets are indicated for the management of anxiety disorders or the short-term relief of the symptoms of anxiety. Anxiety or tension associated with the stress of everyday life usually does not require treatment with an anxiolytic.

Launch Date

985737600000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1.613 ng/mL
15 mg 2 times / day steady-state, oral
dose: 15 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BUSPIRONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1.711 ng/mL
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BUSPIRONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
6.837 ng × h/mL
15 mg 2 times / day steady-state, oral
dose: 15 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BUSPIRONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
9.402 ng × h/mL
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BUSPIRONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3.062 h
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BUSPIRONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
14%
BUSPIRONE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
30 mg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
Health Status: unhealthy
Age Group: 6–17 years
Sex: M+F
Sources:
Other AEs: Headache, Asthenia...
Other AEs:
Headache (29 patients)
Asthenia (10 patients)
Accidental injury (16 patients)
Nausea (13 patients)
Dyspepsia (5 patients)
Diarrhea (6 patients)
Vomiting (34 patients)
Lightheadedness (14 patients)
Somnolence (5 patients)
Insomnia (5 patients)
Nervousness (5 patients)
Upper respiratory tract infection (5 patients)
Sources:
15 mg 2 times / day steady, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: steady
Dose: 15 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Other AEs: Nausea, Headache...
Other AEs:
Nausea (below serious, 1 patient)
Headache (below serious, 1 patient)
Fatigue (below serious, 1 patient)
Sources:
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Other AEs: Light headedness...
Other AEs:
Light headedness (below serious, 1 patient)
Sources:
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Other AEs: Lightheadedness, Drowsiness...
Other AEs:
Lightheadedness (below serious, 36 patients)
Drowsiness (below serious, 17 patients)
Gastrointestinal disorder (below serious, 36 patients)
Headache (below serious, 28 patients)
Insomnia (below serious, 16 patients)
Allergic sinusitis (below serious, 13 patients)
Sources:
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Other AEs: Frozen gait, Tremor...
Other AEs:
Frozen gait (below serious, 5 patients)
Tremor (below serious, 3 patients)
Dizziness (below serious, 2 patients)
Fatigue (below serious, 2 patients)
Bradycardia (below serious, 1 patient)
Constipation (below serious, 1 patient)
Dysphagia (below serious, 1 patient)
Gastritis and duodenitis (below serious, 1 patient)
Gastrointestinal disorder (NOS) (below serious, 1 patient)
Cramp in hand (below serious, 1 patient)
Headache (below serious, 1 patient)
Increased agitation (below serious, 1 patient)
Increased appetite (below serious, 1 patient)
Balance impaired NOS (below serious, 1 patient)
Dystonia (below serious, 1 patient)
Irritability (below serious, 1 patient)
Pain in knee (below serious, 1 patient)
Pain (below serious, 1 patient)
Insomnia (below serious, 1 patient)
Joint stiffness (below serious, 1 patient)
Pain neck/shoulder (below serious, 1 patient)
Leg pain (below serious, 1 patient)
Nasal congestion (below serious, 1 patient)
Numbness (below serious, 1 patient)
Infection respiratory (below serious, 1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Asthenia 10 patients
30 mg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
Health Status: unhealthy
Age Group: 6–17 years
Sex: M+F
Sources:
Nausea 13 patients
30 mg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
Health Status: unhealthy
Age Group: 6–17 years
Sex: M+F
Sources:
Lightheadedness 14 patients
30 mg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
Health Status: unhealthy
Age Group: 6–17 years
Sex: M+F
Sources:
Accidental injury 16 patients
30 mg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
Health Status: unhealthy
Age Group: 6–17 years
Sex: M+F
Sources:
Headache 29 patients
30 mg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
Health Status: unhealthy
Age Group: 6–17 years
Sex: M+F
Sources:
Vomiting 34 patients
30 mg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
Health Status: unhealthy
Age Group: 6–17 years
Sex: M+F
Sources:
Dyspepsia 5 patients
30 mg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
Health Status: unhealthy
Age Group: 6–17 years
Sex: M+F
Sources:
Insomnia 5 patients
30 mg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
Health Status: unhealthy
Age Group: 6–17 years
Sex: M+F
Sources:
Nervousness 5 patients
30 mg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
Health Status: unhealthy
Age Group: 6–17 years
Sex: M+F
Sources:
Somnolence 5 patients
30 mg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
Health Status: unhealthy
Age Group: 6–17 years
Sex: M+F
Sources:
Upper respiratory tract infection 5 patients
30 mg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
Health Status: unhealthy
Age Group: 6–17 years
Sex: M+F
Sources:
Diarrhea 6 patients
30 mg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
Health Status: unhealthy
Age Group: 6–17 years
Sex: M+F
Sources:
Fatigue below serious, 1 patient
15 mg 2 times / day steady, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: steady
Dose: 15 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Headache below serious, 1 patient
15 mg 2 times / day steady, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: steady
Dose: 15 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Nausea below serious, 1 patient
15 mg 2 times / day steady, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: steady
Dose: 15 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Light headedness below serious, 1 patient
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Allergic sinusitis below serious, 13 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Insomnia below serious, 16 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Drowsiness below serious, 17 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Headache below serious, 28 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Gastrointestinal disorder below serious, 36 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Lightheadedness below serious, 36 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Balance impaired NOS below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Bradycardia below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Constipation below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Cramp in hand below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Dysphagia below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Dystonia below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Gastritis and duodenitis below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Gastrointestinal disorder (NOS) below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Headache below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Increased agitation below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Increased appetite below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Infection respiratory below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Insomnia below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Irritability below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Joint stiffness below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Leg pain below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Nasal congestion below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Numbness below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Pain in knee below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Pain neck/shoulder below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Pain below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Dizziness below serious, 2 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Fatigue below serious, 2 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Tremor below serious, 3 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Frozen gait below serious, 5 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG


OverviewOther

Other InhibitorOther SubstrateOther Inducer

Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: coadministration of buspirone (10 mg as a single dose) with verapamil (80 mg t.i.d.) or diltiazem (60 mg t.i.d.) increased plasma buspirone concentrations; coadministration of buspirone (10 mg as a single dose) with erythromycin (1.5 g/day for 4 days) increased plasma buspirone concentrations (5-fold increase in Cmax and 6-fold increase in AUC); coadministration of buspirone (10 mg as a single dose) with itraconazole (200 mg/day for 4 days) increased plasma buspirone concentrations (13-fold increase in Cmax and 19-fold increase in AUC); coadministration of buspirone (2.5 or 5 mg b.i.d.) with nefazodone (250 mg b.i.d.) resulted in marked increases in plasma buspirone concentrations (increases up to 20-fold in Cmax and up to 50-fold in AUC); coadministration of buspirone (30 mg as a single dose) with rifampin (600 mg/day for 5 days) decreased the plasma concentrations (83.7% decrease in Cmax; 89.6% decrease in AUC);
Page: 3
minor
minor
PubMed

PubMed

TitleDatePubMed
5-HT1A receptor agonists buspirone and gepirone attenuate apomorphine-induced aggressive behaviour in adult male Wistar rats.
2000 Dec
Cerebellar Ataxia.
2000 May
Involvement of 5-hydroxytryptamine(1A) receptors in nicotine-induced tail tremor in rats.
2000 Nov 10
Separation anxiety disorder in children and adolescents: epidemiology, diagnosis and management.
2001
Contemporary management of comorbid anxiety and depression in geriatric patients.
2001
Pharmacotherapy of generalized anxiety disorder.
2001
New developments in the pharmacotherapy of alcohol dependence.
2001
Strategies for the treatment of antidepressant-related sexual dysfunction.
2001
Effect of anxiolytics on blood sugar level in rabbits.
2001 Apr
Synthesis and pharmacological evaluation of aryl/heteroaryl piperazinyl alkyl benzotriazoles as ligands for some serotonin and dopamine receptor subtypes.
2001 Apr
Molecular dynamics of buspirone analogues interacting with the 5-HT1A and 5-HT2A serotonin receptors.
2001 Apr
Does pretreatment anxiety predict response to either bupropion SR or sertraline?
2001 Apr
A comparative multidose pharmacokinetic study of buspirone extended-release tablets with a reference immediate-release product.
2001 Aug
Ataxia from lithium toxicity successfully treated with high-dose buspirone: a single-case experimental design.
2001 Aug
An open study of buspirone augmentation of neuroleptics in patients with schizophrenia.
2001 Aug
The impact of impulsivity on cocaine use and retention in treatment.
2001 Dec
Anxiety-like behavior in elevated plus-maze tests in repeatedly cold-stressed mice.
2001 Feb
Behavioral effects of buspirone in the marmoset employing a predator confrontation test of fear and anxiety.
2001 Feb
Extracellular serotonin is enhanced in the striatum, but not in the dorsal hippocampus or prefrontal cortex, in rats subjected to an operant conflict procedure.
2001 Feb
Comparison of antidepressant activity in 4- and 40-week-old male mice in the forced swimming test: involvement of 5-HT1A and 5-HT1B receptors in old mice.
2001 Feb
Prenatal stress and postnatal development of neonatal rats--sex-dependent effects on emotional behavior and learning ability of neonatal rats.
2001 Feb
Acute hypokalemic paralysis associated with long-term lithium therapy.
2001 Feb
Citalopram-induced bruxism.
2001 Feb
Female sexual dysfunction and antidepressant use.
2001 Feb
Treatment of the agitation of late-life psychosis and Alzheimer's disease.
2001 Jan
Use of negatively reinforcing electrical brain stimulation to detect conventional and nonconventional anxiolytics as well as an anxiogenic drug.
2001 Jan
Recovery from chronic fatigue syndrome associated with changes in neuroendocrine function.
2001 Jan
Enhanced cortical extracellular levels of cholecystokinin-like material in a model of anticipation of social defeat in the rat.
2001 Jan 1
An open trial of divalproex sodium in autism spectrum disorders.
2001 Jul
Pharmacokinetics of buspirone extended-release tablets: a single-dose study.
2001 Jul
Common effects of chronically administered antipanic drugs on brainstem GABA(A) receptor subunit gene expression.
2001 Jul
Behavioral and biochemical effects of L-tryptophan and buspirone in a model of cerebellar atrophy.
2001 Jul-Aug
SSRI discontinuation and buspirone.
2001 Jun
Potential involvement of S100B in the protective effects of a serotonin-1a agonist on ethanol-treated astrocytes.
2001 Jun 29
Discriminative stimulus properties of indorenate in a conditioned taste aversion paradigm.
2001 Mar
Discriminative stimulus properties of indorenate, a 5-HT1A, 5-HT1B and 5-HT2C agonist: a study in rats.
2001 Mar
Is imipramine or buspirone treatment effective in patients wishing to discontinue long-term benzodiazepine use?
2001 Mar
Generalized anxiety disorder in children and adolescents.
2001 Mar
Pharmacologic treatment of generalized anxiety disorder.
2001 Mar
Population pharmacokinetic-pharmacodynamic modelling of S 15535, a 5-HT(1A) receptor agonist, using a behavioural model in rats.
2001 Mar 2
Ligand induced conformational states of the 5-HT(1A) receptor.
2001 Mar 23
Quantifying drug-related 5-HT1A receptor occupancy with.
2001 May
Biochemical, electrophysiological and neurohormonal studies with B-20991, a selective 5-HT1A receptor agonist.
2001 May
5-HT1A receptor activation and antidepressant-like effects: F 13714 has high efficacy and marked antidepressant potential.
2001 May 25
Neuropharmacological analysis of the role of the serotoninergic system in forming hyperalgesia in neurotic rats.
2001 May-Jun
Small platform stress increases exploratory activity of mice in staircase test.
2001 Oct
Effectiveness of pharmacotherapy for body dysmorphic disorder: a chart-review study.
2001 Sep
Tandospirone potentiates the fluoxetine-induced increases in extracellular dopamine via 5-HT(1A) receptors in the rat medial frontal cortex.
2002 Apr
The stimulus effect of 5,6,7,8-tetrahydro-1,3-dioxolo[4,5-g]isoquinoline is similar to that of cocaine but different from that of amphetamine.
2002 Jan-Feb
Contact leukoderma caused by buspirone patches.
2002 Mar
Patents

Sample Use Guides

The recommended initial dose is 15 mg daily (7.5 mg b.i.d.). To achieve an optimal therapeutic response, at intervals of 2 to 3 days the dosage may be increased 5 mg per day, as needed. The maximum daily dosage should not exceed 60 mg per day. In clinical trials allowing dose titration, divided doses of 20 mg to 30 mg per day were commonly employed.
Route of Administration: Oral
In Vitro Use Guide
Buspiron was incubated with hippocampal pyramidal cells at concentration of 50 uM. Buspirone was shown to attenuate the synaptic activation of cells.
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:01:11 UTC 2021
Edited
by admin
on Fri Jun 25 21:01:11 UTC 2021
Record UNII
207LT9J9OC
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BUSPIRONE HYDROCHLORIDE
EP   MART.   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD  
USAN  
Official Name English
8-AZASPIRO(4,5)DECANE-7,9-DIONE, 8-(4-(4-(2-PYRIMIDINYL)-1-PIPERAZINYL)BUTYL)-, MONOHYDROCHLORIDE
Common Name English
BUSPAR
Brand Name English
BUSPIRONE HYDROCHLORIDE [MART.]
Common Name English
MJ 9022-1
Code English
BUSPIRONE HYDROCHLORIDE [VANDF]
Common Name English
BUSPIRONE HYDROCHLORIDE [USP-RS]
Common Name English
BUSPIRONE HYDROCHLORIDE [ORANGE BOOK]
Common Name English
BUSPIRONE HYDROCHLORIDE [EP MONOGRAPH]
Common Name English
N-(4-(4-(2-PYRIMIDINYL)-1-PIPERAZINYL)BUTYL)-1,1-CYCLOPENTANEDIACETAMIDE MONOHYDROCHLORIDE
Systematic Name English
APD-405
Code English
BUSPIRONE HCL
Common Name English
APD405
Code English
BUSPIRONE HYDROCHLORIDE [USAN]
Common Name English
NSC-759571
Code English
BUSPIRONE HYDROCHLORIDE [WHO-DD]
Common Name English
BUSPIRONE HYDROCHLORIDE [MI]
Common Name English
BUSPIRONE HYDROCHLORIDE [USP MONOGRAPH]
Common Name English
NSC-751138
Code English
MJ-9022-1
Code English
BUSPIRONE HYDROCHLORIDE [JAN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C28197
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
Code System Code Type Description
MERCK INDEX
M2777
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY Merck Index
USP_CATALOG
1078802
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY USP-RS
ECHA (EC/EINECS)
251-489-4
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
FDA UNII
207LT9J9OC
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
RXCUI
203116
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY RxNorm
EPA CompTox
33386-08-2
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
EVMPD
SUB00906MIG
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
ChEMBL
CHEMBL49
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
CAS
33386-08-2
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
PUBCHEM
36431
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
NCI_THESAURUS
C26641
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
DRUG BANK
DBSALT000313
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
impurity detected at UV 210 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Related Record Type Details
ACTIVE MOIETY