Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMBS632)

Drug Name
Buspirone Drug Info
Synonyms
Ansial; Ansiced; Anxiron; Axoren; Bespar; Buspirona; Buspironum; Buspisal; Ansial (TN); Ansiced (TN); Anxiron (TN); Axoren (TN); Bespar (TN); BuSpar (TN); Buspimen (TN); Buspinol (TN); Buspiron (TN); Buspirona [INN-Spanish]; Buspirone (INN); Buspirone [INN:BAN]; Buspirone-MDTS; Buspironum [INN-Latin]; Buspisal (TN); Gen-Buspirone; Narol (TN); Sorbon (TN); Spamilan (TN); Spitomin (TN); Gen-Buspirone (TN); MJ-9022-1; N-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-1-cyclopentanediacetamide; 8-(4-(4-(2-Pyrimidinyl)-1-piperizinyl)butyl)-8-azaspiro(4,5)decane-7,9-dione; 8-[4-(4-Pyrimidin-2-yl-piperazin-1-yl)-butyl]-8-aza-spiro[4.5]decane-7,9-dione; 8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-8-azaspiro[4.5]decane-7,9-dione; 8-{4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl}-8-azaspiro[4.5]decane-7,9-dione
Indication
Disease Entry ICD 11 Status REF
Anxiety disorder 6B00-6B0Z Approved [1]
Therapeutic Class
Antianxiety Agents
Cross-matching ID
PubChem CID
2477
ChEBI ID
CHEMBL49
CAS Number
CAS 36505-84-7
TTD Drug ID
DMBS632
VARIDT Drug ID
DR00683
INTEDE Drug ID
DR0248
ACDINA Drug ID
D00084

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting 5-HT 1A receptor (HTR1A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Trazodone DMK1GBJ Depression 6A70-6A7Z Approved [9]
OPC-34712 DMHG57U Major depressive disorder 6A70.3 Approved [10]
Vilazodone DM4LECQ Major depressive disorder 6A70.3 Approved [11]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [12]
Gepirone DMGX5Q0 Major depressive disorder 6A70.3 Approved [13]
TERTATOLOL DM2L3D5 Hypertension BA00-BA04 Approved [14]
Urapidil DMD59GI Hypertension BA00-BA04 Approved [15]
Treximet DMU54QB Migraine 8A80 Approved [16]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [17]
Eltoprazine DMW6C81 Attention deficit hyperactivity disorder 6A05.Z Phase 3 [18]
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Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [19]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [20]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [21]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [22]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [23]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [24]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [25]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [26]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [20]
Verapamil DMA7PEW Angina pectoris BA40 Approved [27]
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Drug(s) Metabolized By Cytochrome P450 2D6 (CYP2D6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [28]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [29]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [30]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [23]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [27]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [31]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [32]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [33]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [34]
Propranolol DM79NTF Angina pectoris BA40 Approved [35]
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Drug(s) Metabolized By Cytochrome P450 3A5 (CYP3A5)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [36]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [37]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [38]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [5]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [39]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [40]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [41]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [42]
Verapamil DMA7PEW Angina pectoris BA40 Approved [43]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [5]
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Drug(s) Metabolized By Cytochrome P450 3A7 (CYP3A7)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Progesterone DMUY35B Amenorrhea GA20.0 Approved [44]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [5]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [5]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [5]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [45]
Verapamil DMA7PEW Angina pectoris BA40 Approved [46]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [5]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [5]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [5]
Metronidazole DMTIVEN Abscess Approved [47]
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Drug(s) Metabolized By Cytochrome P450 102A1 (cyp102)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [6]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [48]
Propranolol DM79NTF Angina pectoris BA40 Approved [7]
Dextromethorphan DMUDJZM Allergic rhinitis CA08.0 Approved [6]
Nifedipine DMSVOZT Angina pectoris BA40 Approved [49]
Chlorzoxazone DMCYVDT Acute pain MG31 Approved [49]
Amodiaquine DME4RA8 Malaria 1F40-1F45 Approved [6]
Mefenamic acid DMK7HFI Dysmenorrhea GA34.3 Approved [48]
Meclofenamic acid DM05FXR Ankylosing spondylitis FA92.0 Approved [48]
GEA-6414 DM8J0MK N. A. N. A. Phase 1/2 [48]
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Drug(s) Affected By Pro-opiomelanocortin (POMC)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [50]
Prednisone DM2HG4X Acute asthma CA23 Approved [51]
Naloxone DM3FXMA Narcotic depression 6A7Z Approved [52]
Clonidine DM6RZ9Q Attention deficit hyperactivity disorder 6A05.Z Approved [53]
Fentanyl DM8WAHT Analgesia MB40.8 Approved [54]
Cyproheptadine DM92AH3 Allergic rhinitis CA08.0 Approved [55]
Triamcinolone DM98IXF Acute adrenal insufficiency Approved [56]
Ethanol DMDRQZU Chronic pain MG30 Approved [57]
Metyrapone DMI7FVQ Cushing disease 5A70 Approved [58]
Melatonin DMKWFBT Depression 6A70-6A7Z Approved [59]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 1A receptor (HTR1A) TTSQIFT 5HT1A_HUMAN Agonist [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [3]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [4]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [4]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Substrate [5]
Cytochrome P450 102A1 (cyp102) DE4OGUF CPXB_BACMB Substrate [6] , [7]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Pro-opiomelanocortin (POMC) OTV41F7T COLI_HUMAN Gene/Protein Processing [8]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 36).
2 Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
3 Effects of cytochrome P450 (CYP) 3A4 inhibitors on the anxiolytic action of tandospirone in rat contextual conditioned fear. Prog Neuropsychopharmacol Biol Psychiatry. 2007 May 9;31(4):926-31.
4 Cytochrome P450 3A-mediated metabolism of buspirone in human liver microsomes. Drug Metab Dispos. 2005 Apr;33(4):500-7.
5 Drug Interactions Flockhart Table
6 The bacterial P450 BM3: a prototype for a biocatalyst with human P450 activities. Trends Biotechnol. 2007 Jul;25(7):289-98.
7 acillus megaterium SF185 spores exert protective effects against oxidative stress in vivo and in vitro. Sci Rep. 2019 Aug 19;9(1):12082.
8 Hormonal responses to the 5-HT1A agonist buspirone in remitted endogenous depressive patients after long-term imipramine treatment. Psychoneuroendocrinology. 2010 May;35(4):481-9. doi: 10.1016/j.psyneuen.2009.08.012. Epub 2009 Sep 16.
9 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
10 Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors.Pharmacol Biochem Behav.2014 Sep;124:245-9.
11 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
12 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
13 Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
14 Synthesis of new derivatives of 8-OH-DPAT: Influence of substitution on the aromatic ring on the pharmacological profile, Bioorg. Med. Chem. Lett. 3(10):2035-2038 (1993).
15 Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
16 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
17 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
18 Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
19 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
20 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
21 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
22 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
23 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
24 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
25 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
26 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
27 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
28 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
29 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
30 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
31 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
32 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
33 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
34 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
35 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
36 Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
37 Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
38 Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
39 Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
40 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
41 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
42 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
43 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
44 The role of cytochrome P450 3A (CYP3A) isoform(s) in oxidative metabolism of testosterone and benzphetamine in human adult and fetal liver. J Steroid Biochem Mol Biol. 1993 Jan;44(1):61-7.
45 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
46 Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites. Drug Metab Dispos. 2004 Feb;32(2):259-66.
47 The role of human cytochrome P450 enzymes in the formation of 2-hydroxymetronidazole: CYP2A6 is the high affinity (low Km) catalyst. Drug Metab Dispos. 2013 Sep;41(9):1686-94.
48 Both reactivity and accessibility are important in cytochrome P450 metabolism: a combined DFT and MD study of fenamic acids in BM3 mutants. J Chem Inf Model. 2019 Feb 25;59(2):743-753.
49 Wild-type CYP102A1 as a biocatalyst: turnover of drugs usually metabolised by human liver enzymes. J Biol Inorg Chem. 2007 Mar;12(3):313-23.
50 Neuroendocrine effects of citalopram, a selective serotonin re-uptake inhibitor, during lifespan in humans. J Endocrinol Invest. 2010 Oct;33(9):657-62. doi: 10.1007/BF03346666. Epub 2010 Apr 22.
51 Prednisone effects on neurochemistry and behavior. Preliminary findings. Arch Gen Psychiatry. 1990 Oct;47(10):963-8. doi: 10.1001/archpsyc.1990.01810220079010.
52 Endogenous opioids modulate the cardiovascular response to mental stress. Psychoneuroendocrinology. 1990;15(3):185-92. doi: 10.1016/0306-4530(90)90029-9.
53 Normalization of blood pressure and plasma concentrations of beta-endorphin and leucine-enkephalin in patients with primary hypertension after treatment with clonidine. J Cardiovasc Pharmacol. 1987;10 Suppl 12:S147-51.
54 Serum beta-endorphin response to stress before and after operation under fentanyl anesthesia in neonates, infants and preschool children. Eur J Pediatr Surg. 2010 Mar;20(2):106-10. doi: 10.1055/s-0029-1243620. Epub 2010 Jan 18.
55 [Toxicity of cyproheptadine. Side effects and accidental overdosage (author's transl)]. Monatsschr Kinderheilkd (1902). 1978 Mar;126(3):123-6.
56 Steroid myopathy induced by epidural triamcinolone injection. Br J Rheumatol. 1995 Apr;34(4):385-6. doi: 10.1093/rheumatology/34.4.385.
57 The role of acetaldehyde in mediating effects of alcohol on expression of endogenous opioid system genes in a neuroblastoma cell line. FASEB J. 2008 Mar;22(3):662-70. doi: 10.1096/fj.07-8346com. Epub 2007 Oct 12.
58 Mineralocorticoid receptor function in posttraumatic stress disorder after pretreatment with metyrapone. Biol Psychiatry. 2006 Oct 1;60(7):784-7. doi: 10.1016/j.biopsych.2006.01.014. Epub 2006 Mar 29.
59 [Melatonin reduces cortisol response to ACTH in humans]. Rev Med Chil. 2008 Nov;136(11):1390-7. doi: 10.4067/s0034-98872008001100004.