Identification
- Summary
Buspirone is an anxiolytic agent used for short-term treatment of generalized anxiety and second-line treatment of depression.
- Brand Names
- Buspar
- Generic Name
- Buspirone
- DrugBank Accession Number
- DB00490
- Background
Buspirone is a novel anxiolytic agent with a unique structure and a pharmacological profile. Belonging to the azaspirodecanedione drug class,2 buspirone is a serotonin 5-HT1A receptor agonist that is not chemically or pharmacologically related to benzodiazepines, barbiturates, and other sedative/anxiolytic drugs.13 Unlike many drugs used to treat anxiety, buspirone does not exhibit anticonvulsant, sedative, hypnotic, and muscle-relaxant properties. Due to these characteristics, buspirone been termed 'anxioselective'.1 First synthesized in 1968 then patented in 1975,10 it is commonly marketed under the brand name Buspar®. Buspirone was first approved in 1986 by the FDA 4 and has been used to treat anxiety disorders, such as generalized anxiety disorder (GAD), and relieve symptoms of anxiety. It has also been used as a second-line therapy for unipolar depression when the use of selective serotonin reuptake inhibitors (SSRIs) is deemed clinically inadequate or inappropriate.10 The potential use of buspirone in combination with melatonin in depression and cognitive impairment via promoting neurogenesis has also been investigated.4
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Buspirone (DB00490)
- Weight
- Average: 385.5031
Monoisotopic: 385.247775261 - Chemical Formula
- C21H31N5O2
- 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
Pharmacology
- Indication
Indicated for the management of anxiety disorders or the short-term relief of the symptoms of anxiety.13
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Anxiety disorders •••••••••••• •••••• Adjunct therapy in treatment of Depression ••• ••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
The clinical effect of buspirone in alleviating the symptoms of generalized anxiety disorders typically takes 2 to 4 weeks to achieve.10 The delayed onset of action of buspirone suggests that the therapeutic effectiveness in generalized anxiety may involved more than its molecular mechanism of action at the 5-HT1A receptors,9 or buspirone may induce adaptations of 5-HT1A receptors.10 Buspirone was not shown to alter the psychomotor or cognitive function in healthy volunteers, and the risk of developing sedation is relatively low compared to other anxiolytics, such as benzodiazepines.1 Unlike benzodiazepines and barbiturates used in anxiety disorders, buspirone is not associated with a risk for developing physical dependence or withdrawal, or any significant interaction with central nervous system depressants such as ethanol. This is due to the lack of effects on GABA receptors.1,10 Buspirone also does not exhibit any anticonvulsant or muscle-relaxing properties,5 but may interfere with arousal reactions due to its inhibitory action on the aactivity of noradrenergic locus coerulus neurons.9
Despite its clinical effectiveness in generalized anxiety, buspirone demonstrated limited clinical effectiveness on panic disorders, severe anxiety, phobias, and obsessive compulsive disorders.4,9 The clinical effectiveness of the long-term use of buspirone, for more than 3 to 4 weeks, has not demonstrated in controlled trials but there were no observable significant adverse events in patients receiving buspirone for a year in a study of long-term use.13
- Mechanism of action
The therapeutic action of buspirone in generalized anxiety disorders is thought to be mainly derived from its interaction with two major 5-HT1A receptor subtypes that are involved in the brain's anxiety and fear circuitry to enhance the serotonergic activity in these brain areas.10 Buspirone acts as a full agonist at presynaptic 5-HT1A receptors, or 5-HT1A autoreceptors, expressed at dorsal raphe while acting as a partial agonist at the postsynaptic 5-HT1A receptors expressed on hippocampus and cortex.7,8 5-HT1A receptors function as inhibitory autoreceptors by being expressed on the soma or dendrites of serotonergic neurons or mediate postsynaptic actions of 5-HT by being highly expressed on the corticolimbic circuits.9 They are inhibitory G-protein coupled receptors that couple to Gi/Go proteins. When activated, presynaptic 5-HT1A autoreceptors causes neuron hyperpolarization and reduces the firing rate of the serotonergic neuron, thereby decreasing extracellular 5-HT levels in the neuron's projection areas. Activated postsynaptic 5-HT1A receptors promote hyperpolarization to released 5-HT on pyramidal neurons.8
The anxiolytic action of buspirone is mainly thought to arise from the interaction at presynaptic 5-HT1A autoreceptors. Acting as a potent agonist in these receptors, buspirone initially causes activation of these autoreceptors and inhibition of 5-HT release. It is proposed that buspirone induces desensitization of somatodendritic autoreceptors over time, which may explain the delayed onset of action of the drug. Desensitization of the autoreceptors ultimately results in heightened excitation of serotonergic neurons and enhanced 5-HT release.9 Buspirone also displays a weak affinity for serotonin 5HT2 receptors and acts as a weak antagonist on dopamine D2 autoreceptors,10 although there is not much evidence that the action at these receptors contribute to the anxiolytic effect of buspirone.6 It acts as an antagonist at presynaptic dopamine D3 and D4 receptors and may bind to alpha-1 adrenergic receptors as a partial agonist.4
Target Actions Organism A5-hydroxytryptamine receptor 1A partial agonistHumans ADopamine D2 receptor antagonistHumans UDopamine D3 receptor antagonistHumans UDopamine D4 receptor antagonistHumans UAlpha-1 adrenergic receptors partial agonistHumans - Absorption
Buspirone is rapidly absorbed following oral administration.13 Bioavailability is low and variable (approximately 5%) due to extensive first pass metabolism. While absorption of buspirone is decreased with concomitant food intake, the first-pass metabolism of the drug is also decreased, resulting in an increased bioavailability 10 as well as increased Cmax and AUC.13 Following oral administration of single oral doses of 20 mg, the Cmax ranged from 1 to 6 ng/mL and the Tmax ranged from 40 to 90 minutes.13
- Volume of distribution
In a pharmacokinetic study assessing buspirone over the dose range of 10 to 40 mg, the volume of distribution was 5.3 L/kg.3
- Protein binding
Based on the findings of an in vitro protein binding study, approximately 86% of buspirone is bound to plasma proteins.13 It is mainly bound to serum albumin and alpha-1-acid glycoprotein.2
- Metabolism
Buspirone is extensively metabolized upon administration, where it primarily undergoes hepatic oxidation mediated by the CYP3A4 enzyme. Hydroxylated derivatives are produced, including a pharmacologically active metabolite 1-pyrimidinylpiperazine (1-PP). In animal studies, 1-PP possessed about one quarter of the pharmacological activity of buspirone.13
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- Route of elimination
A single-dose pharmacokinetic studies using 14C-labeled buspirone demonstrated that about 29-63% of the dose administered was excreted in the urine within 24 hours, primarily in the form of metabolites. About 18% to 38% of the dose was eliminated via fecal excretion.13
- Half-life
In a single-dose pharmacokinetic study of 14C-labeled buspirone, the average elimination half-life of unchanged buspirone following administration of single doses ranging from 10 to 40 mg was about 2 to 3 hours.13
- Clearance
In a pharmacokinetic study assessing buspirone over the dose range of 10 to 40 mg, the systemic clearance was 1.7 L/h/kg.3
- Adverse Effects
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The oral LD50 of buspirone is 196 mg/kg in rat, 655 mg/kg in mouse, 586 mg/kg in dog, and 356 mg/kg in monkey. The intraperitoneal LD50 is 136 mg/kg in rat and 146 mg/kg in mouse.13,11
In clinical pharmacology trials, administration of buspirone at the dose of 375 mg/day resulted in symptoms of nausea, vomiting, dizziness, drowsiness, miosis, and gastric distress. Few cases of overdosage that have been reported usually resulted in complete recovery. In case of overdose, the use of general symptomatic and supportive treatment is recommended along with immediate gastric lavage and monitoring of respiration, pulse, and blood pressure.13
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Buspirone is combined with 1,2-Benzodiazepine. Abacavir Buspirone may decrease the excretion rate of Abacavir which could result in a higher serum level. Abametapir The serum concentration of Buspirone can be increased when it is combined with Abametapir. Abatacept The metabolism of Buspirone can be increased when combined with Abatacept. Abiraterone The metabolism of Buspirone can be decreased when combined with Abiraterone. - Food Interactions
- Avoid alcohol. Alcohol may cause additive CNS depressant effects.
- Avoid grapefruit products. Grapefruit increases the plasma concentrations of the drug.
- Take at the same time every day. Take consistently at the same time in regard to meals.
- Take with or without food. Take drug always with or always without food in a consistent manner.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Buspirone hydrochloride 207LT9J9OC 33386-08-2 RICLFGYGYQXUFH-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Ansial (Rontag) / Anxiron (Valeant) / Anxut (Eisai) / Bespar / Buscalm (Wockhardt) / Busp (Hexal) / Buspon (Deva) / Dalpas (Biotech) / Epsilat (Coup) / Pasrin (Aspen Pharmacare) / Spamilan (Anpharm)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Buspar Tablet 15 mg/1 Oral Physicians Total Care, Inc. 2001-08-31 2011-05-31 US 
Buspar Tablet 30 mg/1 Oral Bristol Myers Squibb 2009-06-01 2011-05-31 US Buspar Tablet 5 mg/1 Oral Bristol Myers Squibb 2009-06-01 2012-01-31 US Buspar Tablet 10 mg/1 Oral Physicians Total Care, Inc. 1995-02-14 2011-05-31 US Buspar Tablet 15 mg/1 Oral Bristol Myers Squibb 2009-06-01 2011-05-31 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-buspirone Tablet 10 mg Oral Apotex Corporation 1996-12-31 Not applicable Canada 
Auro-buspirone Tablet 10 mg Oral Auro Pharma Inc 2020-10-30 Not applicable Canada Buspar Tablet 5 mg/1 Oral Directrx 2016-05-03 Not applicable US Buspirone Tablet 10 mg/1 Oral Stat Rx USA 2002-03-01 Not applicable US Buspirone HCl Tablet 5 mg/1 Oral Actavis Pharma Company 2001-03-28 2018-12-31 US 
Categories
- ATC Codes
- N05BE01 — Buspirone
- Drug Categories
- Agents that produce hypertension
- Antidepressive Agents
- Azaspirodecanedione Derivatives
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Substrates
- Dopamine Antagonists
- Dopamine D2 Receptor Antagonists
- Drugs that are Mainly Renally Excreted
- Miscellaneous Anxiolytics Sedatives and Hypnotics
- Nervous System
- Neurotransmitter Agents
- P-glycoprotein inhibitors
- Piperazines
- Psycholeptics
- Pyrimidines
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin Agents
- Spiro Compounds
- Tranquilizing Agents
- Chemical TaxonomyProvided by Classyfire
- 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
- Amine / Amino acid or derivatives / Aminopyrimidine / Aromatic heteropolycyclic compound / Azacycle / Azaspirodecane / Azaspirodecanedione / Carbonyl group / Carboxylic acid derivative / Carboxylic acid imide show 21 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- N-arylpiperazine, pyrimidines, N-alkylpiperazine, piperidones, azaspiro compound (CHEBI:3223)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- TK65WKS8HL
- CAS number
- 36505-84-7
- 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
References
- Synthesis Reference
- US3717634
- General References
- Goa KL, Ward A: Buspirone. A preliminary review of its pharmacological properties and therapeutic efficacy as an anxiolytic. Drugs. 1986 Aug;32(2):114-29. doi: 10.2165/00003495-198632020-00002. [Article]
- Jann MW: Buspirone: an update on a unique anxiolytic agent. Pharmacotherapy. 1988;8(2):100-16. [Article]
- Mahmood I, Sahajwalla C: Clinical pharmacokinetics and pharmacodynamics of buspirone, an anxiolytic drug. Clin Pharmacokinet. 1999 Apr;36(4):277-87. doi: 10.2165/00003088-199936040-00003. [Article]
- Howland RH: Buspirone: Back to the Future. J Psychosoc Nurs Ment Health Serv. 2015 Nov;53(11):21-4. doi: 10.3928/02793695-20151022-01. [Article]
- Eison AS, Temple DL Jr: Buspirone: review of its pharmacology and current perspectives on its mechanism of action. Am J Med. 1986 Mar 31;80(3B):1-9. doi: 10.1016/0002-9343(86)90325-6. [Article]
- Tunnicliff G: Molecular basis of buspirone's anxiolytic action. Pharmacol Toxicol. 1991 Sep;69(3):149-56. [Article]
- Yocca FD: Neurochemistry and neurophysiology of buspirone and gepirone: interactions at presynaptic and postsynaptic 5-HT1A receptors. J Clin Psychopharmacol. 1990 Jun;10(3 Suppl):6S-12S. [Article]
- Garcia-Garcia AL, Newman-Tancredi A, Leonardo ED: 5-HT(1A) [corrected] receptors in mood and anxiety: recent insights into autoreceptor versus heteroreceptor function. Psychopharmacology (Berl). 2014 Feb;231(4):623-36. doi: 10.1007/s00213-013-3389-x. Epub 2013 Dec 12. [Article]
- 43. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 538-539). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
- Buspirone - StatPearls - NCBI Bookshelf [Link]
- Buspirone (hydrochloride) Safety Data Sheet - Cayman Chemical [Link]
- Buspirone hydrochloride (B7148) - Sigma Aldrich Product Information Sheet [Link]
- BuSpar® (buspirone HCl) FDA Label [Link]
- External Links
- Human Metabolome Database
- HMDB0014633
- KEGG Drug
- D07593
- KEGG Compound
- C06861
- PubChem Compound
- 2477
- PubChem Substance
- 46508113
- ChemSpider
- 2383
- BindingDB
- 50001859
- 1827
- ChEBI
- 3223
- ChEMBL
- CHEMBL49
- ZINC
- ZINC000001530571
- Therapeutic Targets Database
- DAP000031
- PharmGKB
- PA448689
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Buspirone
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Other Autism Disorder 1 4 Completed Treatment Anxiety / Williams Syndrome 1 4 Completed Treatment Depression 1 4 Completed Treatment Dyspepsia 1 4 Completed Treatment Heroin Dependence 1
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
Form Route Strength Tablet Oral 10 mg/1 Tablet Oral 15 mg/1 Tablet Oral 30 mg/1 Tablet Oral 5 mg/1 Powder Not applicable 1 g/1g Tablet Oral 10 1/1 Tablet Oral 15 1/1 Tablet Oral 5 1/1 Tablet Oral 7.5 mg/1 Capsule Capsule 5 mg Tablet Oral 10 mg / tab Tablet Oral Tablet Oral 10 mg Tablet Oral 5 mg - Prices
Unit description Cost Unit Wellbutrin xl 300 mg tablet 8.68USD tablet Wellbutrin xl 150 mg tablet 6.58USD tablet Buspar 30 mg tablet 5.52USD tablet Buspirone hcl powder 4.74USD g Buspirone hcl 30 mg tablet 3.71USD tablet Buspar 15 mg tablet 3.07USD tablet Buspirone hcl 15 mg tablet 2.16USD tablet Buspar 10 mg tablet 2.05USD tablet Buspirone hcl 7.5 mg tablet 1.62USD tablet Buspirone hcl 10 mg tablet 1.42USD tablet Buspar 5 mg tablet 1.18USD tablet Vanspar 7.5 mg tablet 1.18USD tablet Buspar 10 mg Tablet 1.12USD tablet Buspirone hcl 5 mg tablet 0.79USD tablet Apo-Buspirone 10 mg Tablet 0.62USD tablet Novo-Buspirone 10 mg Tablet 0.62USD tablet Nu-Buspirone 10 mg Tablet 0.62USD tablet Pms-Buspirone 10 mg Tablet 0.62USD tablet Ratio-Buspirone 10 mg Tablet 0.62USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 201.5-202.5 Buspirone hydrochloride (B7148) - Sigma Aldrich Product Information Sheet logP 2.63 TAKACS-NOVAK,K 1995 (IN PRESS) - Predicted Properties
Property Value Source Water Solubility 0.588 mg/mL ALOGPS logP 1.95 ALOGPS logP 1.78 Chemaxon logS -2.8 ALOGPS pKa (Strongest Basic) 7.62 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 69.64 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 108.89 m3·mol-1 Chemaxon Polarizability 44.02 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9935 Blood Brain Barrier + 0.9839 Caco-2 permeable - 0.538 P-glycoprotein substrate Substrate 0.5726 P-glycoprotein inhibitor I Inhibitor 0.8563 P-glycoprotein inhibitor II Non-inhibitor 0.8282 Renal organic cation transporter Inhibitor 0.598 CYP450 2C9 substrate Non-substrate 0.8703 CYP450 2D6 substrate Substrate 0.8918 CYP450 3A4 substrate Substrate 0.6728 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Inhibitor 0.8948 CYP450 2D6 inhibitor Inhibitor 0.7186 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8681 Ames test Non AMES toxic 0.6277 Carcinogenicity Non-carcinogens 0.8959 Biodegradation Not ready biodegradable 0.987 Rat acute toxicity 2.8167 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7042 hERG inhibition (predictor II) Inhibitor 0.6914
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 218.3608619 predictedDarkChem Lite v0.1.0 [M-H]- 201.4435315 predictedDarkChem Lite v0.1.0 [M-H]- 184.05379 predictedDeepCCS 1.0 (2019) [M+H]+ 218.5471619 predictedDarkChem Lite v0.1.0 [M+H]+ 200.139181 predictedDarkChem Lite v0.1.0 [M+H]+ 186.41182 predictedDeepCCS 1.0 (2019) [M+Na]+ 218.4445619 predictedDarkChem Lite v0.1.0 [M+Na]+ 208.2484561 predictedDarkChem Lite v0.1.0 [M+Na]+ 192.66591 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
- Gene Name
- DRD3
- Uniprot ID
- P35462
- Uniprot Name
- D(3) dopamine receptor
- Molecular Weight
- 44224.335 Da
References
- Howland RH: Buspirone: Back to the Future. J Psychosoc Nurs Ment Health Serv. 2015 Nov;53(11):21-4. doi: 10.3928/02793695-20151022-01. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Sh3 domain binding
- Specific Function
- Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins ...
- Gene Name
- DRD4
- Uniprot ID
- P21917
- Uniprot Name
- D(4) dopamine receptor
- Molecular Weight
- 48359.86 Da
References
- Howland RH: Buspirone: Back to the Future. J Psychosoc Nurs Ment Health Serv. 2015 Nov;53(11):21-4. doi: 10.3928/02793695-20151022-01. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Partial agonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Components:
| Name | UniProt ID |
|---|---|
| Alpha-1A adrenergic receptor | P35348 |
| Alpha-1B adrenergic receptor | P35368 |
| Alpha-1D adrenergic receptor | P25100 |
References
- Howland RH: Buspirone: Back to the Future. J Psychosoc Nurs Ment Health Serv. 2015 Nov;53(11):21-4. doi: 10.3928/02793695-20151022-01. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Lamberg TS, Kivisto KT, Neuvonen PJ: Concentrations and effects of buspirone are considerably reduced by rifampicin. Br J Clin Pharmacol. 1998 Apr;45(4):381-5. doi: 10.1046/j.1365-2125.1998.t01-1-00698.x. [Article]
- Flockhart Table of Drug Interactions [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- Kind
- Protein
- Organism
- Humans
- 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
- Flockhart Table of Drug Interactions [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Jagestedt M, von Bahr C: [Combination of serotonergic agents resulted in severe adverse effects]. Lakartidningen. 2004 Apr 29;101(18):1618-9. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Jann MW: Buspirone: an update on a unique anxiolytic agent. Pharmacotherapy. 1988;8(2):100-16. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
- Gene Name
- ORM1
- Uniprot ID
- P02763
- Uniprot Name
- Alpha-1-acid glycoprotein 1
- Molecular Weight
- 23511.38 Da
References
- Jann MW: Buspirone: an update on a unique anxiolytic agent. Pharmacotherapy. 1988;8(2):100-16. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Feng B, Mills JB, Davidson RE, Mireles RJ, Janiszewski JS, Troutman MD, de Morais SM: In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system. Drug Metab Dispos. 2008 Feb;36(2):268-75. doi: 10.1124/dmd.107.017434. Epub 2007 Oct 25. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55