◎ Sugi Atlas

Atlas / Drug / Buspirone

Buspirone

drug
On this page

Also known as BCI-024BuspironaGen-buspironeSID11110857SID11112732SID11113821SID26751994SID90340780SID104171117BuspironBuspinoneSID144203643SID144212688SID170464909

Summary

Buspirone (CHEMBL49) is an approved small-molecule anxiolytic drug (ATC N05BE01) targeting HTR7 and HTR1A; indicated across 20 conditions including anxiety and dementia.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N05BE01
  • Targets: 2 (HTR7, HTR1A)
  • Indications: 20 conditions
  • Clinical trials: 54
  • Chemistry: 385.5 Da · C21H31N5O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL49
NameBuspirone
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID2477
ChEBICHEBI:3223
ATCN05BE01
Molecular formulaC21H31N5O2
Molecular weight385.5
InChIKeyQWCRAEMEVRGPNT-UHFFFAOYSA-N

SMILES: C1CCC2(C1)CC(=O)N(C(=O)C2)CCCCN3CCN(CC3)C4=NC=CC=N4

IUPAC name: 8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-8-azaspiro[4.5]decane-7,9-dione

ChEBI definition: An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N4 position.

Pharmacological roles (ChEBI): anxiolytic drug, sedative, serotonergic agonist, EC 3.4.21.26 (prolyl oligopeptidase) inhibitor.

Also known as: BCI-024, Buspirona, Buspirone, Gen-buspirone, buspirone, SID11110857, SID11112732, SID11113821, SID26751994, SID90340780, SID104171117, Buspiron

Parent form; salt/anhydrous children: CHEMBL1200399

Patent coverage: 6,273 distinct patent families (23,063 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
HTR75-HT7 receptorAntagonist6.40.8%P34969
HTR1A5-HT1A receptorPartial agonist80%P08908

Broader ChEMBL bioactivity targets: 41 (assay-derived). Sample: Solute carrier family 22 member 2, Multidrug and toxin extrusion protein 1, Multidrug and toxin extrusion protein 2, 5-hydroxytryptamine receptor 2B, Adrenergic receptor alpha-1, Alpha-2C adrenergic receptor, Adrenergic receptor alpha-2, Dopamine receptor, Serotonin 2 (5-HT2) receptor, Adrenergic receptor alpha-1.

Bioactivity

ChEMBL activities: 171 potent at pChembl ≥ 5 of 194 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
HTR1A8.51Ki3.1nMCHEMBL_ACT_159622
P193278.42Ki3.8nMCHEMBL_ACT_2287026
HTR1A8.4Ki4nMCHEMBL_ACT_18858923
HTR1A8.32Ki4.78nMCHEMBL_ACT_18168816
HTR1A8.3Ki5.01nMCHEMBL_ACT_22404436
HTR1A8.3Ki5.01nMCHEMBL_ACT_22781486
HTR1A8.3Ki5.01nMCHEMBL_ACT_24845262
HTR1A8.3Ki5nMCHEMBL_ACT_27894149
P193278.3Ki5nMCHEMBL_ACT_307664
P193278.3Ki5nMCHEMBL_ACT_340294
HTR1A8.18Ki6.6nMCHEMBL_ACT_328488
P193278.15IC507.13nMCHEMBL_ACT_1307834
P193278.15Ki7nMCHEMBL_ACT_749624
HTR1A8.07Ki8.6nMCHEMBL_ACT_749639
HTR1A8.05Ki8.9nMCHEMBL_ACT_18700518
P193278.03Ki9.3nMCHEMBL_ACT_749633
P193278.03Ki9.31nMCHEMBL_ACT_7607088
P193278Ki10nMCHEMBL_ACT_1134306
HTR1A8Kd10nMCHEMBL_ACT_2930079
P193278Ki10nMCHEMBL_ACT_792400
P193278Ki10nMCHEMBL_ACT_896540
P193277.96IC5011nMCHEMBL_ACT_102327
P193277.96IC5011nMCHEMBL_ACT_1521984
HTR1A7.92Ki12nMCHEMBL_ACT_13375491
P193277.91Ki12.3nMCHEMBL_ACT_889350
DRD27.89Ki13nMCHEMBL_ACT_159623
DRD27.89Ki13nMCHEMBL_ACT_1718526
P193277.89IC5012.8nMCHEMBL_ACT_53362
P193277.89IC5012.8nMCHEMBL_ACT_742814
P193277.86Ki13.8nMCHEMBL_ACT_1250634

Target pathways

Aggregated over 2 target gene(s): HTR7, HTR1A.

Top Reactome pathways

9 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction2HTR1A, HTR7
Signaling by GPCR2HTR1A, HTR7
Class A/1 (Rhodopsin-like receptors)2HTR1A, HTR7
Amine ligand-binding receptors2HTR1A, HTR7
Serotonin receptors2HTR1A, HTR7
GPCR ligand binding2HTR1A, HTR7
GPCR downstream signalling1HTR7
G alpha (s) signalling events1HTR7
RHOBTB3 ATPase cycle1HTR7

Dominant GO biological processes

GO termTargets
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger2
chemical synaptic transmission2
signal transduction2
G protein-coupled receptor signaling pathway2
G protein-coupled serotonin receptor signaling pathway2
smooth muscle contraction1
adenylate cyclase-activating serotonin receptor signaling pathway1
circadian rhythm1
blood circulation1
vasoconstriction1
behavioral fear response1
adenylate cyclase-inhibiting serotonin receptor signaling pathway1
serotonin receptor signaling pathway1
gamma-aminobutyric acid signaling pathway1
positive regulation of cell population proliferation1

Indications & clinical

Indications

20 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
anxiety4MONDO:0011918EFO:0005230
dementia3MONDO:0001627HP:0000726
depressive disorder3MONDO:0002050MONDO:0002050
Parkinson disease3MONDO:0005180MONDO:0005180
generalized anxiety disorder3MONDO:0001942EFO:1001892
cocaine dependence2MONDO:0005186EFO:0002610
autism spectrum disorder2MONDO:0005258EFO:0003756
autism2MONDO:0005260EFO:0003758
attention deficit-hyperactivity disorder2MONDO:0007743EFO:0003888
physiological sexual disorder2MONDO:0002134EFO:0004714
spinal cord injury2MONDO:0043797EFO:1001919
cannabis dependence2MONDO:0005689EFO:0007191
gastroparesis2MONDO:0006769EFO:1000948
major depressive disorder2MONDO:0002009MONDO:0002009
dyspepsia1MONDO:0002268EFO:0008533
systemic sclerosis0MONDO:0005100EFO:0000717

4 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 54.

Phase distribution

PhaseTrials
PHASE218
PHASE415
PHASE36
Not specified5
PHASE1/PHASE24
PHASE13
EARLY_PHASE12
PHASE2/PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04118387PHASE4RECRUITINGCentral Sleep Apnea : Physiologic Mechanisms to Inform Treatment
NCT04400266PHASE4RECRUITINGBuspirone and Melatonin for Depression Following Traumatic Brain Injury
NCT05629325PHASE4RECRUITINGBuspirone for Weak or Absent Esophageal Peristalsis
NCT07439042PHASE4NOT_YET_RECRUITINGBuspirone for Anxiety in Autistic Youth
NCT00021528PHASE4COMPLETEDSequenced Treatment Alternatives to Relieve Depression (STAR*D)
NCT00326235PHASE4COMPLETEDEffects of Buspirone in Opiate Withdrawal
NCT00334360PHASE4COMPLETEDDexmed/Buspirone Synergism on Shivering
NCT00875836PHASE4COMPLETEDBuspirone Treatment for Marijuana Dependence
NCT01546896PHASE4WITHDRAWNEffects of Buspar on Depressive Symptom Improvement and Neuroprotection in Patients With Anxiety Disorder
NCT01821690PHASE4COMPLETEDBuspirone for the Treatment of Traumatic Brain Injury (TBI) Irritability and Aggression
NCT02273154PHASE4UNKNOWNRandomized，Controlled and Open-label Study of Buspirone add-on Treatment in Patients With Major Depression Disorder
NCT02483598PHASE4TERMINATEDMechanistic Investigation Of Intestinal Cytochrome p450 3A4 Following Roux-en-Y Surgery And Its Effect on Plasma Concentrations of Buspirone
NCT03444831PHASE4COMPLETEDBuspirone Plus Omeprazole for Functional Dyspepsia
NCT03538431PHASE4COMPLETEDImproving Driving in Young People With Autism Spectrum Disorders
NCT04807517PHASE4COMPLETEDBuspirone Treatment of Anxiety in Williams Syndrome
NCT00178971PHASE3COMPLETEDSerotonin 1A Agonists and Cognition in Schizophrenia
NCT00746954PHASE3TERMINATEDBuspirone as a Potential Treatment for Recurrent Central Apnea
NCT00873509PHASE2/PHASE3COMPLETEDBuspirone in the Treatment of 2-6 Year Old Children With Autistic Disorder
NCT01833312PHASE3TERMINATEDCooling Plus Best Medical Treatment Versus Best Medical Treatment Alone for Acute Ischaemic Stroke
NCT02374567PHASE3TERMINATEDPharmacovigilance in Gerontopsychiatric Patients
NCT02617017PHASE3COMPLETEDBuspirone Treatment of Iatrogenic Dyskinesias in Advanced Parkinson’ Disease
NCT05430217PHASE3COMPLETEDEfficacy and Safety of Buspirone, Sustained-release Tablets, 15 mg in Patients With Autonomic Dysfunction Syndrome Accompanied by Vertigo
NCT02313194PHASE1/PHASE2ACTIVE_NOT_RECRUITINGSpinal Cord Neuromodulation for Spinal Cord Injury
NCT04458324PHASE2ACTIVE_NOT_RECRUITINGHybrid Functional Electrical Stimulation Exercise to Prevent Cardiopulmonary Declines in High-level Spinal Cord Injury
NCT05511909PHASE2RECRUITINGEvaluating Buspirone to Treat Opioid Withdrawal
NCT00149617PHASE2COMPLETEDEffectiveness of Buspirone and Motivational Enhancement Therapy for the Treatment of Marijuana Dependence - 1
NCT00166621PHASE1/PHASE2COMPLETEDEarly Pharmacotherapy Aimed at Neuroplasticity in Autism : Safety and Efficacy
NCT00174226PHASE2COMPLETEDTreatment of Adult ADHD With Atomoxetine or Atomoxetine and Buspar
NCT00360191PHASE2COMPLETEDA Placebo-Controlled Trial of Buspirone for Treatment of Marijuana Dependence
NCT00705003PHASE2COMPLETEDEfficacy and Safety Study of a Combination Product [Drug:BCI-024 (Buspirone) and Drug:BCI-049 (Melatonin)] to Treat Major Depressive Disorder (MDD)
NCT01267292PHASE2COMPLETEDPsychopharmacology for Cocaine Dependence - Buspirone
NCT01395953PHASE2WITHDRAWNDouble-blind Trial of Buspirone for the Treatment of Anxiety in Youth With Autism Spectrum Disorders
NCT01496612PHASE2TERMINATEDBuspirone Therapy for Localized Epilepsy
NCT01641159PHASE2COMPLETEDStudy of Buspirone for Relapse-Prevention in Adults With Cocaine Dependence
NCT01699828PHASE1/PHASE2COMPLETEDExploring Occupancy of Dopamine D3 Receptor by Buspirone in Humans Using PET
NCT02101203PHASE2COMPLETEDLybridos in Pre-and Postmenopausal Women With Hypoactive Sexual Desire Disorder
NCT02132832PHASE2COMPLETEDBuspirone, Stress, and Attentional Bias to Marijuana Cues
NCT02458469PHASE2COMPLETEDRole of Enhancing Serotonin Receptors Activity for Sleep Apnea Treatment in Patients With SCI
NCT02803749PHASE2COMPLETEDBuspirone in Parkinson’s Disease
NCT03432065PHASE2WITHDRAWNA Pilot Study of Buspirone for the Treatment of Anxiety in Youth with Autism Spectrum Disorders

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 1 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

423 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
BREXPIPRAZOLEChEMBL + PubChemPhase 4 (approved)HTR1A, HTR7
DihydroergotamineChEMBL + PubChemPhase 4 (approved)HTR1A, HTR7
PRAMIPEXOLEChEMBL + PubChemPhase 4 (approved)HTR1A, HTR7
AMOXAPINEChEMBLPhase 4 (approved)HTR1A, HTR7
ARIPIPRAZOLEChEMBLPhase 4 (approved)HTR1A, HTR7
ASTEMIZOLEChEMBLPhase 4 (approved)HTR1A, HTR7
CARIPRAZINEChEMBLPhase 4 (approved)HTR1A, HTR7
CARVEDILOLChEMBLPhase 4 (approved)HTR1A, HTR7
CHLORPROMAZINEChEMBLPhase 4 (approved)HTR1A, HTR7
CINACALCETChEMBLPhase 4 (approved)HTR1A, HTR7
CISAPRIDEChEMBLPhase 4 (approved)HTR1A, HTR7
CLONIDINEChEMBLPhase 4 (approved)HTR1A, HTR7
CLOZAPINEChEMBLPhase 4 (approved)HTR1A, HTR7
CYPROHEPTADINEChEMBLPhase 4 (approved)HTR1A, HTR7
DIBENZEPINChEMBLPhase 4 (approved)HTR1A, HTR7
DOXEPINChEMBLPhase 4 (approved)HTR1A, HTR7
FLUPHENAZINEChEMBLPhase 4 (approved)HTR1A, HTR7
FROVATRIPTANChEMBLPhase 4 (approved)HTR1A, HTR7
HALOPERIDOLChEMBLPhase 4 (approved)HTR1A, HTR7
IMIPRAMINEChEMBLPhase 4 (approved)HTR1A, HTR7
KETANSERINChEMBLPhase 4 (approved)HTR1A, HTR7
LOXAPINEChEMBLPhase 4 (approved)HTR1A, HTR7
LURASIDONEChEMBLPhase 4 (approved)HTR1A, HTR7
METHYSERGIDEChEMBLPhase 4 (approved)HTR1A, HTR7
MIANSERINChEMBLPhase 4 (approved)HTR1A, HTR7
MIRTAZAPINEChEMBLPhase 4 (approved)HTR1A, HTR7
NEFAZODONEChEMBLPhase 4 (approved)HTR1A, HTR7
OLANZAPINEChEMBLPhase 4 (approved)HTR1A, HTR7
PERPHENAZINEChEMBLPhase 4 (approved)HTR1A, HTR7
PHENYLEPHRINEChEMBLPhase 4 (approved)HTR1A, HTR7
PROMAZINEChEMBLPhase 4 (approved)HTR1A, HTR7
QUETIAPINEChEMBLPhase 4 (approved)HTR1A, HTR7
RISPERIDONEChEMBLPhase 4 (approved)HTR1A, HTR7
RITONAVIRChEMBLPhase 4 (approved)HTR1A, HTR7
SALMETEROLChEMBLPhase 4 (approved)HTR1A, HTR7
SILODOSINChEMBLPhase 4 (approved)HTR1A, HTR7
SORAFENIBChEMBLPhase 4 (approved)HTR1A, HTR7
SUMATRIPTANChEMBLPhase 4 (approved)HTR1A, HTR7
TAMSULOSINChEMBLPhase 4 (approved)HTR1A, HTR7
TEGASERODChEMBLPhase 4 (approved)HTR1A, HTR7
THIORIDAZINEChEMBLPhase 4 (approved)HTR1A, HTR7
THIOTHIXENEChEMBLPhase 4 (approved)HTR1A, HTR7
VILAZODONEChEMBLPhase 4 (approved)HTR1A, HTR7
VORTIOXETINEChEMBLPhase 4 (approved)HTR1A, HTR7
ZIPRASIDONEChEMBLPhase 4 (approved)HTR1A, HTR7
BRILAROXAZINEChEMBLPhase 3HTR1A, HTR7
IDALOPIRDINEChEMBLPhase 3HTR1A, HTR7
INTEPIRDINEChEMBLPhase 3HTR1A, HTR7
NALUZOTANChEMBLPhase 3HTR1A, HTR7
OXITRIPTANChEMBLPhase 3HTR1A, HTR7
SEROTONINChEMBLPhase 3HTR1A, HTR7
ULOTARONTChEMBLPhase 3HTR1A, HTR7
ADOPRAZINEChEMBLPhase 2HTR1A, HTR7
AZAPERONEChEMBLPhase 2HTR1A, HTR7
CHLOROPHENYLPIPERAZINEChEMBLPhase 2HTR1A, HTR7
FANANSERINChEMBLPhase 2HTR1A, HTR7
GSK163090ChEMBLPhase 2HTR1A, HTR7
IPSAPIRONEChEMBLPhase 2HTR1A, HTR7
JNJ-18038683 FREE BASEChEMBLPhase 2HTR1A, HTR7
LYSERGIDEChEMBLPhase 2HTR1A, HTR7

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot