General Information of Drug (ID: DM36C17)

Drug Name
Blonanserin Drug Info
Synonyms
Lonasen; Blonanserin [INN]; AD 5423; AD-5423; Blonanserin (JAN/INN); 2-(4-Ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta(b)pyridine; 2-(4-Ethyl-1-piperazinyl)-4-(p-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta(b)pyridine; 2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
Indication
Disease Entry ICD 11 Status REF
Schizophrenia 6A20 Phase 3 [1]
Cross-matching ID
PubChem CID
125564
ChEBI ID
CHEBI:31296
CAS Number
CAS 132810-10-7
TTD Drug ID
DM36C17
INTEDE Drug ID
DR1902

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting 5-HT 2A receptor (HTR2A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [4]
ZOTEPINE DMF3VXA Anxiety disorder 6B00-6B0Z Approved [5]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [6]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [7]
Lurasidone hydrochloride DMCVPXO Schizophrenia 6A20 Approved [8]
Aniracetam DMOIFW0 Cerebrovascular ischaemia 8B1Z Approved [9]
lumateperone tosylate DMQ8HOJ Schizophrenia 6A20 Approved [10]
Sarpogrelate DMGLP6S Diabetic complication 5A2Y Approved [11]
Pimavanserin DMR7IVC Parkinson disease 8A00.0 Approved [12]
Zicronapine DMP8ESD Schizophrenia 6A20 Phase 3 [13]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Dopamine D2 receptor (D2R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [14]
Haloperidol DM96SE0 Delirium Approved [15]
Perphenazine DMA4MRX Schizophrenia 6A20 Approved [16]
Perazine DM2AOTZ Psychotic disorder 6A20-6A25 Approved [17]
Domperidone DMBDPY0 Gastrointestinal disease DE2Z Approved [18]
Levodopa DMN3E57 Parkinson disease 8A00.0 Approved [19]
Quetiapine DM1N62C Anorexia nervosa cachexia 6B80 Approved [20]
Pimozide DMW83TP Schizophrenia 6A20 Approved [21]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [22]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [6]
⏷ Show the Full List of 10 Drug(s)
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 [23]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [24]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [25]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [26]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [27]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [28]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [29]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [30]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [24]
Verapamil DMA7PEW Angina pectoris BA40 Approved [31]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 2A receptor (HTR2A) TTJQOD7 5HT2A_HUMAN Antagonist [2]
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Antagonist [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [3]

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: 7670).
2 The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
3 Profile of blonanserin for the treatment of schizophrenia. Neuropsychiatr Dis Treat. 2013;9:587-94.
4 Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23.
5 Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
6 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
7 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
8 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
9 Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism. Eur J Pharmacol. 2001 May 18;420(1):33-43.
10 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
11 Beneficial effects of sarpogrelate hydrochloride, a 5-HT2A receptor antagonist, supplemented with pioglitazone on diabetic model mice. Endocr Res. 2009;34(1-2):18-30.
12 Pimavanserin, a selective serotonin (5-HT)2A-inverse agonist, enhances the efficacy and safety of risperidone, 2mg/day, but does not enhance efficacy of haloperidol, 2mg/day: comparison with reference dose risperidone, 6mg/day.Schizophr Res.2012 Nov;141(2-3):144-52.
13 Clinical pipeline report, company report or official report of Lundbeck.
14 The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74.
15 Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
16 CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
17 Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.
18 Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
19 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: 3639).
20 Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
21 [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
22 Modulatory role of dopamine D2 receptors and fundamental role of L-type Ca2+ channels in the induction of long-term potentiation in the basolateral... Eur J Pharmacol. 2009 Mar 15;606(1-3):90-3.
23 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.
24 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
25 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.
26 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
27 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.
28 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.
29 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
30 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.
31 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.