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Details

Stereochemistry ACHIRAL
Molecular Formula C21H31N5O2
Molecular Weight 385.5039
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BUSPIRONE

SMILES

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

InChI

InChIKey=QWCRAEMEVRGPNT-UHFFFAOYSA-N
InChI=1S/C21H31N5O2/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

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

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
Controversies in dyspepsia.
2001
Overview of different pharmacotherapies for attaining remission in generalized anxiety disorder.
2001
Separation anxiety disorder in children and adolescents: epidemiology, diagnosis and management.
2001
Effect of anxiolytics on blood sugar level in rabbits.
2001 Apr
Switching from benzodiazepines to buspirone using a tapered overlap method in generalized anxiety disorder.
2001 Aug
Review of pharmacokinetic and pharmacodynamic interaction studies with citalopram.
2001 Aug
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
Serotonergic regulation of inhibitory avoidance and one-way escape in the rat elevated T-maze.
2001 Dec
The impact of impulsivity on cocaine use and retention in treatment.
2001 Dec
Effect of nonnicotine pharmacotherapy on smoking behavior.
2001 Dec
Pharmacokinetics and tolerability of buspirone during oral administration to children and adolescents with anxiety disorder and normal healthy adults.
2001 Dec
Effects of cholecystokinin tetrapeptide (CCK(4)) and anxiolytic drugs on the electrically evoked [(3)H]5-hydroxytryptamine outflow from rat cortical slices.
2001 Dec 13
Treatment of the agitation of late-life psychosis and Alzheimer's disease.
2001 Jan
An open trial of divalproex sodium in autism spectrum disorders.
2001 Jul
Pharmacokinetics of buspirone extended-release tablets: a single-dose study.
2001 Jul
Characterization of alpha1-adrenoceptor-mediated contraction in the mouse thoracic aorta.
2001 Jul 20
Effect of citalopram and buspirone on the antinociceptive action of analgesic drugs.
2001 Jul-Aug
Behavioral and biochemical effects of L-tryptophan and buspirone in a model of cerebellar atrophy.
2001 Jul-Aug
[New drugs for the treatment of functional dyspepsia].
2001 Jul-Sep
An investigation of the mechanisms responsible for acute fluoxetine-induced anxiogenic-like effects in mice.
2001 Jun
Patients with severe depression may benefit from buspirone augmentation of selective serotonin reuptake inhibitors: results from a placebo-controlled, randomized, double-blind, placebo wash-in study.
2001 Jun
Conformational analysis and pharmacophore design for selected 1-(2-pyrimidinyl)piperazine derivatives with sedative-hypnotic activity.
2001 Mar-Apr
Pattern of symptom improvement following treatment with venlafaxine XR in patients with generalized anxiety disorder.
2001 Nov
Acoustic startle, conditioned startle potentiation and the effects of 8-OH-DPAT and buspirone in rats selectively bred for differences in 8-OH-DPAT-induced hypothermia.
2001 Nov
Quantifying the 5-HT1A agonist action of buspirone in man.
2001 Nov
Buspirone and meperidine synergistically reduce the shivering threshold.
2001 Nov
Astrocyte-mediated trophic support of developing serotonin neurons: effects of ethanol, buspirone, and S100B.
2001 Nov 26
Venlafaxine and generalised anxiety disorder: new preparation. Minimise recourse to drugs.
2001 Oct
The effect of glucocorticoids on the anxiolytic efficacy of buspirone.
2001 Oct
A double-blind placebo-controlled study of buspirone-stimulated prolactin release in non-ulcer dyspepsia--are central serotoninergic responses enhanced?
2001 Oct
Small platform stress increases exploratory activity of mice in staircase test.
2001 Oct
Impact of cortisol on buspirone stimulated prolactin release: a double-blind placebo-controlled study.
2001 Oct
Effectiveness of pharmacotherapy for body dysmorphic disorder: a chart-review study.
2001 Sep
Diazepam, but not buspirone, induces similar anxiolytic-like actions in lactating and ovariectomized Wistar rats.
2001 Sep
[The role of neuropeptide Y in anxiety].
2001 Sep-Oct
Hypomania induced by herbal and pharmaceutical psychotropic medicines following mild traumatic brain injury.
2002 Apr
Tandospirone potentiates the fluoxetine-induced increases in extracellular dopamine via 5-HT(1A) receptors in the rat medial frontal cortex.
2002 Apr
Olfactory-mediated fear-potentiated startle.
2002 Feb
Bupropion-induced acute dystonia.
2002 Feb
Benzodiazepine discontinuation in generalized anxiety disorder.
2002 Feb
Light-enhanced startle: further pharmacological and behavioral characterization.
2002 Jan
Atypical kinetics for a series of putative dopamine antagonists to reverse the low-magnitude Ca2+ phase in the dopamine-bound D2short receptor state.
2002 Jan
Effect of drug proportion and mixing time on the content uniformity of a low dose drug in a high shear mixer.
2002 Jan
Short term aerobic exercise training in young males does not alter sensitivity to a central serotonin agonist.
2002 Jan
Pharmacological and endocrinological characterisation of stress-induced hyperthermia in singly housed mice using classical and candidate anxiolytics (LY314582, MPEP and NKP608).
2002 Jan 25
Anxiogenic activity of Myristica fragrans seeds.
2002 Jan-Feb
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 Sat Jun 26 04:35:17 UTC 2021
Edited
by admin
on Sat Jun 26 04:35:17 UTC 2021
Record UNII
TK65WKS8HL
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BUSPIRONE
INN   MI   VANDF   WHO-DD  
INN  
Official Name English
BUSPIRONE [VANDF]
Common Name English
BUSPIRONE [INN]
Common Name English
8-(4-(4-(2-PYRIMIDINYL)-1-PIPERIZINYL)BUTYL)-8-AZASPIRO(4,5)DECANE-7,9-DIONE
Systematic Name English
BUSPIRONE [MI]
Common Name English
BCI-024
Code English
BUSPIRONE [WHO-DD]
Common Name English
GEN-BUSPIRONE
Brand Name English
Classification Tree Code System Code
WHO-VATC QN05BE01
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
LIVERTOX 129
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
WHO-ATC N05BE01
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
NCI_THESAURUS C28197
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
Code System Code Type Description
CAS
36505-84-7
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
MERCK INDEX
M2777
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY Merck Index
ChEMBL
CHEMBL49
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
PUBCHEM
2477
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
EVMPD
SUB05992MIG
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
IUPHAR
36
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
RXCUI
1827
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY RxNorm
DRUG CENTRAL
437
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
MESH
D002065
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
ECHA (EC/EINECS)
253-072-2
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
WIKIPEDIA
BUSPIRONE
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
NCI_THESAURUS
C62013
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
INN
3456
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
FDA UNII
TK65WKS8HL
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
DRUG BANK
DB00490
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
EPA CompTox
36505-84-7
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
LACTMED
Buspirone
Created by admin on Sat Jun 26 04:35:17 UTC 2021 , Edited by admin on Sat Jun 26 04:35:17 UTC 2021
PRIMARY
Related Record Type Details
TARGET->PARTIAL AGONIST
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE ACTIVE -> PARENT
METABOLITE ACTIVE -> PARENT
Related Record Type Details
IMPURITY -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC