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

General Information of Drug (ID: DMVDO93)

• Drug Name: BL-1020 Drug Info
• Synonyms: BL 1020; Perphenazine 4-aminobutyrate; Butanoic acid, 4-amino-, 2-(4-(3-(2-chloro-10H-phenothiazin-10-yl)propyl)-1-piperazinyl)ethyl ester

Indication

Disease Entry	ICD 11	Status	REF
Schizophrenia	6A20	Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 11203271
  CAS Number: CAS 751477-01-7
  TTD Drug ID: DMVDO93

Molecule-Related Drug Atlas

Drug(s) Targeting Gamma-aminobutyric acid receptor (GAR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Phenobarbital	DMXZOCG	Cluster headache	8A81.0	Approved	[3]
Allopregnanolone	DMNLHAC	Depression	6A70-6A7Z	approved	[4]
THIOCOLCHICOSIDE	DMEPWYA	Muscle spasm	MB47.3	Approved	[5]
Clonazepam	DMTO13J	Absence epilepsy		Approved	[6]
Piperazine	DMTY9LU	Ascariasis	1F62	Approved	[7]
Alpidem	DMN7Y9K	Anxiety disorder	6B00-6B0Z	Approved	[8]
Moxidectin	DMYGHX5	Onchocerciasis	1F6A	Approved	[9]
DP-VPA	DMGOXPQ	Bipolar disorder	6A60	Approved	[10]
ANDROSTERONE	DMITJAK	N. A.	N. A.	Phase 3	[4]
ZK-93423	DMFWMKZ	Epileptic seizures	8A61-8A6Z	Phase 3	[11]

Drug(s) Targeting Dopamine D2 receptor (D2R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dopamine	DMPGUCF	Acromegaly	5A60.0	Approved	[12]
Haloperidol	DM96SE0	Delirium		Approved	[13]
Perphenazine	DMA4MRX	Schizophrenia	6A20	Approved	[14]
Perazine	DM2AOTZ	Psychotic disorder	6A20-6A25	Approved	[15]
Domperidone	DMBDPY0	Gastrointestinal disease	DE2Z	Approved	[16]
Levodopa	DMN3E57	Parkinson disease	8A00.0	Approved	[17]
Quetiapine	DM1N62C	Anorexia nervosa cachexia	6B80	Approved	[18]
Pimozide	DMW83TP	Schizophrenia	6A20	Approved	[19]
Chlorpromazine	DMBGZI3	Acute intermittent hepatic porphyria	5C58.11	Approved	[20]
Iloperidone	DM6AUFY	Schizophrenia	6A20	Approved	[21]

Drug(s) Affected By Prolactin (PRL)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[22]
Ranitidine	DM0GUSX	Gastric ulcer	DA60	Approved	[23]
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[24]
Citalopram	DM2G9AE	Acute coronary syndrome	BA41	Approved	[25]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[26]
Thioridazine	DM35M8J	Schizophrenia	6A20	Approved	[27]
Naloxone	DM3FXMA	Narcotic depression	6A7Z	Approved	[28]
Aripiprazole	DM3NUMH	Bipolar I disorder		Approved	[29]
Fluoxetine	DM3PD2C	Bipolar depression		Approved	[30]
Penicillamine	DM40EF6	Cystinuria	5C60.2	Approved	[31]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Dopamine D2 receptor (D2R)	TTEX248	DRD2_HUMAN	Antagonist	[1]
Gamma-aminobutyric acid receptor (GAR)	TTNJYV2	NOUNIPROTAC	Agonist	[1]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Prolactin (PRL)	OTWFQGX7	PRL_HUMAN	Gene/Protein Processing	[2]

References

• [1] The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
• [2] An open-label tolerability study of BL-1020 antipsychotic: a novel gamma aminobutyric acid ester of perphenazine. Clin Neuropharmacol. 2010 Nov-Dec;33(6):297-302. doi: 10.1097/WNF.0b013e3181f8d501.
• [3] DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.
• [4] Neurosteroid analogues. 11. Alternative ring system scaffolds: gamma-aminobutyric acid receptor modulation and anesthetic actions of benz[f]indenes. J Med Chem. 2006 Jul 27;49(15):4595-605.
• [5] 3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7.
• [6] Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
• [7] Cyclooctadepsipeptides--an anthelmintically active class of compounds exhibiting a novel mode of action. Int J Antimicrob Agents. 2003 Sep;22(3):318-31.
• [8] Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new se... J Med Chem. 1997 Sep 12;40(19):3109-18.
• [9] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [10] DP-VPA D-Pharm. Curr Opin Investig Drugs. 2002 Jun;3(6):921-3.
• [11] Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carbolin... J Med Chem. 1990 Mar;33(3):1062-9.
• [12] 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.
• [13] Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
• [14] CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
• [15] 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.
• [16] Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
• [17] 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).
• [18] Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
• [19] [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
• [20] 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.
• [21] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [22] Verapamil-induced hyperprolactinemia complicated by a pituitary incidentaloma. Ann Pharmacother. 1995 Oct;29(10):999-1001. doi: 10.1177/106002809502901009.
• [23] [Impotence and gynecomastia secondary to hyperprolactinemia induced by ranitidine]. Therapie. 1994 Jul-Aug;49(4):361-2.
• [24] Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin release. Mol Cell Endocrinol. 2005 Jul 15;239(1-2):27-36. doi: 10.1016/j.mce.2005.04.008.
• [25] Cholinergic modulation of the cerebral metabolic response to citalopram in Alzheimer's disease. Brain. 2009 Feb;132(Pt 2):392-401. doi: 10.1093/brain/awn326. Epub 2009 Jan 19.
• [26] The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
• [27] The effect of thioridazine on prolactinoma growth in a schizophrenic man: case report. Gen Hosp Psychiatry. 1985 Oct;7(4):364-6. doi: 10.1016/0163-8343(85)90053-2.
• [28] Influence of naloxone on muscle sympathetic nerve activity, systemic and calf haemodynamics and ambulatory blood pressure after exercise in mild essential hypertension. J Hypertens. 1995 Apr;13(4):447-61.
• [29] The efficacy, safety, and tolerability of aripiprazole for the treatment of schizoaffective disorder: results from a pooled analysis of a sub-population of subjects from two randomized, double-blind, placebo-controlled, pivotal trials. J Affect Disord. 2009 May;115(1-2):18-26. doi: 10.1016/j.jad.2008.12.017. Epub 2009 Feb 23.
• [30] Serum prolactin levels among outpatients with major depressive disorder during the acute phase of treatment with fluoxetine. J Clin Psychiatry. 2006 Jun;67(6):952-7. doi: 10.4088/jcp.v67n0612.
• [31] Massive breast enlargement in a patient receiving D-penicillamine for systemic sclerosis. J Rheumatol. 1985 Oct;12(5):990-1.