Identification

Name
Buspirone
Accession Number
DB00490  (APRD00222)
Type
Small Molecule
Groups
Approved, Investigational
Description

An anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to diazepam. [PubChem]

Structure
Thumb
Synonyms
  • 8-(4-(4-(2-Pyrimidinyl)-1-piperizinyl)butyl)-8-azaspiro(4,5)decane-7,9-dione
  • Buspiron
  • Buspirona
  • Buspirone
  • Buspironum
External IDs
BCI-024 / MJ 90221-1
Product Ingredients
IngredientUNIICASInChI Key
Buspirone Hydrochloride207LT9J9OC33386-08-2RICLFGYGYQXUFH-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BusparTablet15 mg/1OralPhysicians Total Care, Inc.2001-08-312011-05-31Us
BusparTablet5 mg/1OralPhysicians Total Care, Inc.1995-07-312011-05-31Us
BusparTablet10 mg/1OralBristol Myers Squibb2009-06-012011-03-31Us
BusparTablet30 mg/1OralBristol Myers Squibb2009-06-012011-05-31Us
BusparTablet5 mg/1OralBristol Myers Squibb2009-06-012012-01-31Us
BusparTablet10 mg/1OralPhysicians Total Care, Inc.1995-02-142011-05-31Us
BusparTablet15 mg/1OralBristol Myers Squibb2009-06-012011-05-31Us
Buspar Tab 10mgTablet10 mgOralBristol Myers Squibb1989-12-312010-11-12Canada
BuspironeTablet10 mgOralSanis Health Inc2016-02-17Not applicableCanada
BusPIRone HydrochlorideTablet15 mg/1OralPar Pharmaceutical Inc2007-03-232007-03-23Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-buspirone - Tab 10mgTablet10 mgOralApotex Corporation1996-12-31Not applicableCanada
BusparTablet5 mg/1OralDirectrx2016-05-03Not applicableUs
BuspironeTablet10 mg/1OralStat Rx USA2002-03-01Not applicableUs
Buspirone HClTablet15 mg/1OralRebel Distributors2001-03-28Not applicableUs
Buspirone HClTablet10 mg/1OralActavis Pharma Company2001-03-282019-03-31Us
Buspirone HClTablet10 mg/1OralImpax Generics2016-11-01Not applicableUs
Buspirone HClTablet10 mg/1OralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Buspirone HClTablet5 mg/1OralMc Kesson Packaging Services A Buisness Unit Of Mc Kesson Corporation2004-12-142010-04-24Us
Buspirone HClTablet10 mg/1OralAmerincan Health Packaging2005-09-192015-07-01Us
Buspirone HClTablet10 mg/1OralClinical Solutions Wholsesale2001-03-282017-06-22Us58118 065720180913 8702 s8cink
International/Other Brands
Ansial (Rontag) / Anxiron (Valeant) / Anxut (Eisai) / Bespar / Buscalm (Wockhardt) / Busp (Hexal) / Buspar (Bristol-Myers Squibb) / Buspon (Deva) / Dalpas (Biotech) / Epsilat (Coup) / Pasrin (Aspen Pharmacare) / Spamilan (Anpharm)
Categories
UNII
TK65WKS8HL
CAS number
36505-84-7
Weight
Average: 385.5031
Monoisotopic: 385.247775261
Chemical Formula
C21H31N5O2
InChI Key
QWCRAEMEVRGPNT-UHFFFAOYSA-N
InChI
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
IUPAC Name
8-{4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl}-8-azaspiro[4.5]decane-7,9-dione
SMILES
O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)C1=NC=CC=N1

Pharmacology

Indication

For the management of anxiety disorders or the short-term relief of the symptoms of anxiety, and also as an augmention of SSRI-treatment against depression.

Associated Conditions
Pharmacodynamics

Buspirone is used in the treatment of generalized anxiety where it has advantages over other antianxiety drugs because it does not cause sedation (drowsiness) and does not cause tolerance or physical dependence. 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. in vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding in vitro or in vivo when tested in preclinical models. Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems.

Mechanism of action

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.

TargetActionsOrganism
A5-hydroxytryptamine receptor 1A
partial agonist
Human
AD(2) dopamine receptor
antagonist
Human
Absorption

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

Volume of distribution
Not Available
Protein binding

95% (approximately 70% bound to albumin, 30% bound to alpha 1 -acid glycoprotein)

Metabolism

Metabolized hepatically, primarily by oxidation by cytochrome P450 3A4 producing several hydroxylated derivatives and a pharmacologically active metabolite, 1-pyrimidinylpiperazine (1-PP)

Route of elimination

In a single-dose study using 14C-labeled buspirone, 29% to 63% of the dose was excreted in the urine within 24 hours, primarily as metabolites; fecal excretion accounted for 18% to 38% of the dose.

Half life

2-3 hours (although the action of a single dose is much longer than the short halflife indicates).

Clearance
Not Available
Toxicity

Oral, rat LD50 = 136 mg/kg. Symptoms of overdose include dizziness, drowsiness, nausea or vomiting, severe stomach upset, and unusually small pupils.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of Buspirone can be decreased when combined with (R)-warfarin.
(S)-WarfarinThe metabolism of Buspirone can be decreased when combined with (S)-Warfarin.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of serotonin syndrome can be increased when Buspirone is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of serotonin syndrome can be increased when Buspirone is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineThe risk or severity of serotonin syndrome can be increased when Buspirone is combined with 3,4-Methylenedioxyamphetamine.
3,5-diiodothyropropionic acidThe metabolism of Buspirone can be decreased when combined with 3,5-diiodothyropropionic acid.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of serotonin syndrome can be increased when Buspirone is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Buspirone.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Buspirone is combined with 4-Methoxyamphetamine.
5-androstenedioneThe metabolism of Buspirone can be decreased when combined with 5-androstenedione.
Food Interactions
  • Always take at the same time with respect to meals.
  • Avoid alcohol.
  • Avoid taking grapefruit or grapefruit juice throughout treatment.
  • Take with food.

References

Synthesis Reference
US3717634
General References
Not Available
External Links
Human Metabolome Database
HMDB0014633
KEGG Compound
C06861
PubChem Compound
2477
PubChem Substance
46508113
ChemSpider
2383
BindingDB
50001859
ChEBI
3223
ChEMBL
CHEMBL49
Therapeutic Targets Database
DAP000031
PharmGKB
PA448689
IUPHAR
36
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Buspirone
ATC Codes
N05BE01 — Buspirone
AHFS Codes
  • 28:24.92 — Miscellaneous Anxiolytics Sedatives and Hypnotics
FDA label
Download (275 KB)
MSDS
Download (75.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedTreatmentSclerosis, Progressive Systemic1
1CompletedNot AvailableHealthy Volunteers2
1CompletedNot AvailableTo Determine Bioequivalence Under Fasting Conditions1
1CompletedOtherTo Determine Bioequivalence Under Fed Conditions1
1RecruitingTreatmentDependency (Psychology) / Opiate Withdrawal Syndrome / Opioid-Related Disorders / Pain, Chronic1
1RecruitingTreatmentDyskinesias / Movement Disorders / Parkinson's Disease (PD)1
1, 2CompletedBasic ScienceCessation, Smoking / Tobacco Use Cessation1
1, 2CompletedTreatmentAutism, Early Infantile1
1, 2CompletedTreatmentSpinal Cord Injuries (SCI)1
2CompletedBasic ScienceCannabis Use Disorders1
2CompletedBasic ScienceDependence, Cocaine1
2CompletedTreatmentAttention Deficit Disorder With Hyperactivity1
2CompletedTreatmentDependence, Cocaine1
2CompletedTreatmentHypoactive Sexual Desire Disorder (HSDD)2
2CompletedTreatmentMajor Depressive Disorder (MDD)1
2CompletedTreatmentMarijuana Abuse1
2CompletedTreatmentMarijuana Abuse / Moods Disorders1
2Not Yet RecruitingTreatmentGastroparesis1
2RecruitingBasic ScienceSleep Disordered Breathing (SDB) / Spinal Cord Injuries (SCI)1
2RecruitingTreatmentAutism Spectrum Conditions/Disorders / Feeling Anxious1
2RecruitingTreatmentFeeling Anxious / Parkinson's Disease (PD)1
2TerminatedTreatmentAnxiety Disorders / Depression / Epilepsies / Epilepsy, Localization Related / Seizures1
2WithdrawnTreatmentAutism Spectrum Conditions/Disorders1
2, 3CompletedSupportive CareDyspnea / Pulmonary Complications / Unspecified Adult Solid Tumor, Protocol Specific1
2, 3CompletedTreatmentAutistic Disorder1
3RecruitingTreatmentAcute Ischemic Stroke (AIS)1
3RecruitingTreatmentParkinson1
3TerminatedBasic ScienceCentral Apnea / Heart Failure, Unspecified1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
4CompletedTreatmentDepression1
4CompletedTreatmentHeroin Dependence1
4CompletedTreatmentHypothermia1
4CompletedTreatmentIndigestion1
4CompletedTreatmentMarijuana Dependence1
4RecruitingDiagnosticAsthma Bronchial / Asthma: [Nos] or [Attack] / Major Depressive Disorder (MDD)1
4RecruitingOtherAutism Spectrum Conditions/Disorders1
4TerminatedOtherBypass, Gastric1
4Unknown StatusTreatmentMajor Depression Disorder1
4WithdrawnTreatmentAnxiety Disorders1
Not AvailableCompletedBasic ScienceCocaine Use Disorders1
Not AvailableCompletedTreatmentFunctional Dysphagia / Ineffective Esophageal Motility1
Not AvailableEnrolling by InvitationNot AvailableCardiovascular Disease (CVD) / Cardiovascular Risk Factors / High Blood Pressure (Hypertension) / Mental status changes / Sleep Apnea Syndrome / Sleep Bruxism / Sleep disorders and disturbances / Temporomandibular Disorders / Thyroid Dysfunction1
Not AvailableRecruitingTreatmentAutism Spectrum Conditions/Disorders / Feeling Anxious1
Not AvailableRecruitingTreatmentTraumatic Brain Injury (TBI)1
Not AvailableUnknown StatusTreatmentAnxiety Disorders1

Pharmacoeconomics

Manufacturers
  • Bristol myers squibb co pharmaceutical research institute
  • Actavis totowa llc
  • Apotex inc
  • Dr reddys laboratories ltd
  • Egis pharmaceuticals
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Kv pharmaceutical co
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
Packagers
  • Advanced Pharmaceutical Services Inc.
  • Amerisource Health Services Corp.
  • Apotex Inc.
  • Apotheca Inc.
  • Apothecon
  • AQ Pharmaceuticals Inc.
  • A-S Medication Solutions LLC
  • Bristol-Myers Squibb Co.
  • Bryant Ranch Prepack
  • BTA Pharmaceuticals
  • Cardinal Health
  • Comprehensive Consultant Services Inc.
  • Corepharma LLC
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Doctor Reddys Laboratories Ltd.
  • Egis Pharmaceuticals Public Ltd. Co.
  • Ethex Corp.
  • H.E. Butt Grocery Co.
  • Heartland Repack Services LLC
  • Innoviant Pharmacy Inc.
  • Ivax Pharmaceuticals
  • KV Pharmaceutical Co.
  • Lake Erie Medical and Surgical Supply
  • Major Pharmaceuticals
  • Mckesson Corp.
  • Medisca Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Neuman Distributors Inc.
  • Nucare Pharmaceuticals Inc.
  • Palmetto Pharmaceuticals Inc.
  • Par Pharmaceuticals
  • Patheon Inc.
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Pharmaceutical Utilization Management Program VA Inc.
  • Pharmedix
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Prx Pharmaceuticals
  • Ranbaxy Laboratories
  • Rebel Distributors Corp.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Sandhills Packaging Inc.
  • Southwood Pharmaceuticals
  • Stat Rx Usa
  • Teva Pharmaceutical Industries Ltd.
  • Torpharm Inc.
  • UDL Laboratories
  • Va Cmop Dallas
  • Vangard Labs Inc.
  • Watson Pharmaceuticals
Dosage forms
FormRouteStrength
TabletOral10 mg
TabletOral10 mg/1
TabletOral15 mg/1
TabletOral30 mg/1
TabletOral5 mg/1
TabletOral10 1/1
TabletOral15 1/1
TabletOral5 1/1
TabletOral7.5 mg/1
TabletOral5 mg
Prices
Unit descriptionCostUnit
Wellbutrin xl 300 mg tablet8.68USD tablet
Wellbutrin xl 150 mg tablet6.58USD tablet
Buspar 30 mg tablet5.52USD tablet
Buspirone hcl powder4.74USD g
Buspirone hcl 30 mg tablet3.71USD tablet
Buspar 15 mg tablet3.07USD tablet
Buspirone hcl 15 mg tablet2.16USD tablet
Buspar 10 mg tablet2.05USD tablet
Buspirone hcl 7.5 mg tablet1.62USD tablet
Buspirone hcl 10 mg tablet1.42USD tablet
Buspar 5 mg tablet1.18USD tablet
Vanspar 7.5 mg tablet1.18USD tablet
Buspar 10 mg Tablet1.12USD tablet
Buspirone hcl 5 mg tablet0.79USD tablet
Apo-Buspirone 10 mg Tablet0.62USD tablet
Novo-Buspirone 10 mg Tablet0.62USD tablet
Nu-Buspirone 10 mg Tablet0.62USD tablet
Pms-Buspirone 10 mg Tablet0.62USD tablet
Ratio-Buspirone 10 mg Tablet0.62USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)201.5-202.5 °CNot Available
water solubility21.4 mg/LNot Available
logP2.63TAKACS-NOVAK,K 1995 (IN PRESS)
Predicted Properties
PropertyValueSource
Water Solubility0.588 mg/mLALOGPS
logP1.95ALOGPS
logP1.78ChemAxon
logS-2.8ALOGPS
pKa (Strongest Basic)7.62ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area69.64 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity108.89 m3·mol-1ChemAxon
Polarizability44.12 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9935
Blood Brain Barrier+0.9839
Caco-2 permeable-0.538
P-glycoprotein substrateSubstrate0.5726
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IINon-inhibitor0.8282
Renal organic cation transporterInhibitor0.598
CYP450 2C9 substrateNon-substrate0.8703
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.6728
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorInhibitor0.8948
CYP450 2D6 inhibitorInhibitor0.7186
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8681
Ames testNon AMES toxic0.6277
CarcinogenicityNon-carcinogens0.8959
BiodegradationNot ready biodegradable0.987
Rat acute toxicity2.8167 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7042
hERG inhibition (predictor II)Inhibitor0.6914
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-004i-6940000000-197b8ea9ac79cbda753b
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-000i-0009000000-429c277f63eb2ab52f57
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-000i-0009000000-170a03c9244dada2609b
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00di-0922000000-80c9aa9ae15b661116ad
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00di-1900000000-fafa91d49f01314afdf1
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00dj-4900000000-460409b07d20201af414
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000f-0930000000-081eac0a05abab8fc5fa

Taxonomy

Description
This compound belongs to the class of organic compounds known as n-arylpiperazines. These are organic compounds containing a piperazine ring where the nitrogen ring atom carries an aryl group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazinanes
Sub Class
Piperazines
Direct Parent
N-arylpiperazines
Alternative Parents
Azaspirodecane derivatives / Piperidinediones / Dialkylarylamines / Aminopyrimidines and derivatives / N-alkylpiperazines / Delta lactams / N-substituted carboxylic acid imides / Heteroaromatic compounds / Dicarboximides / Trialkylamines
show 6 more
Substituents
Azaspirodecanedione / N-arylpiperazine / Azaspirodecane / Piperidinedione / Dialkylarylamine / Aminopyrimidine / N-alkylpiperazine / Piperidinone / Delta-lactam / Pyrimidine
show 21 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
N-arylpiperazine, pyrimidines, N-alkylpiperazine, piperidones, azaspiro compound (CHEBI:3223)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Partial agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. de Boer SF, Lesourd M, Mocaer E, Koolhaas JM: Selective antiaggressive effects of alnespirone in resident-intruder test are mediated via 5-hydroxytryptamine1A receptors: A comparative pharmacological study with 8-hydroxy-2-dipropylaminotetralin, ipsapirone, buspirone, eltoprazine, and WAY-100635. J Pharmacol Exp Ther. 1999 Mar;288(3):1125-33. [PubMed:10027850]
  2. Rehman J, Kaynan A, Christ G, Valcic M, Maayani S, Melman A: Modification of sexual behavior of Long-Evans male rats by drugs acting on the 5-HT1A receptor. Brain Res. 1999 Mar 13;821(2):414-25. [PubMed:10064829]
  3. Liang KC: Pre- or post-training injection of buspirone impaired retention in the inhibitory avoidance task: involvement of amygdala 5-HT1A receptors. Eur J Neurosci. 1999 May;11(5):1491-500. [PubMed:10215901]
  4. Becker C, Hamon M, Benoliel JJ: Prevention by 5-HT1A receptor agonists of restraint stress- and yohimbine-induced release of cholecystokinin in the frontal cortex of the freely moving rat. Neuropharmacology. 1999 Apr;38(4):525-32. [PubMed:10221756]
  5. Dupuis DS, Tardif S, Wurch T, Colpaert FC, Pauwels PJ: Modulation of 5-HT1A receptor signalling by point-mutation of cysteine351 in the rat Galpha(o) protein. Neuropharmacology. 1999 Jul;38(7):1035-41. [PubMed:10428422]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  7. Osei-Owusu P, Scrogin KE: Buspirone raises blood pressure through activation of sympathetic nervous system and by direct activation of alpha1-adrenergic receptors after severe hemorrhage. J Pharmacol Exp Ther. 2004 Jun;309(3):1132-40. Epub 2004 Feb 9. [PubMed:14769835]
Details
2. D(2) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Malt EA, Olafsson S, Aakvaag A, Lund A, Ursin H: Altered dopamine D2 receptor function in fibromyalgia patients: a neuroendocrine study with buspirone in women with fibromyalgia compared to female population based controls. J Affect Disord. 2003 Jun;75(1):77-82. [PubMed:12781354]
  2. Boido A, Boido CC, Sparatore F: Synthesis and pharmacological evaluation of aryl/heteroaryl piperazinyl alkyl benzotriazoles as ligands for some serotonin and dopamine receptor subtypes. Farmaco. 2001 Apr;56(4):263-75. [PubMed:11421254]
  3. Nader MA, Hannemann M: Interactions of buspirone or gepirone with nicotine on schedule-controlled behavior of pigeons. Behav Pharmacol. 1993 Jun;4(3):263-268. [PubMed:11224194]
  4. Pache DM, Fernandez-Perez S, Sewell RD: Buspirone differentially modifies short-term memory function in a combined delayed matching/non-matching to position task. Eur J Pharmacol. 2003 Sep 23;477(3):205-11. [PubMed:14522358]
  5. Fernandez-Perez S, Pache DM, Sewell RD: Co-administration of fluoxetine and WAY100635 improves short-term memory function. Eur J Pharmacol. 2005 Oct 17;522(1-3):78-83. Epub 2005 Oct 7. [PubMed:16214127]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Zhu M, Zhao W, Jimenez H, Zhang D, Yeola S, Dai R, Vachharajani N, Mitroka J: Cytochrome P450 3A-mediated metabolism of buspirone in human liver microsomes. Drug Metab Dispos. 2005 Apr;33(4):500-7. Epub 2005 Jan 7. [PubMed:15640381]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Zhu M, Zhao W, Jimenez H, Zhang D, Yeola S, Dai R, Vachharajani N, Mitroka J: Cytochrome P450 3A-mediated metabolism of buspirone in human liver microsomes. Drug Metab Dispos. 2005 Apr;33(4):500-7. Epub 2005 Jan 7. [PubMed:15640381]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Zhu M, Zhao W, Jimenez H, Zhang D, Yeola S, Dai R, Vachharajani N, Mitroka J: Cytochrome P450 3A-mediated metabolism of buspirone in human liver microsomes. Drug Metab Dispos. 2005 Apr;33(4):500-7. Epub 2005 Jan 7. [PubMed:15640381]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [PubMed:12438524]

Drug created on June 13, 2005 07:24 / Updated on November 20, 2018 00:43