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

General Information of Drug (ID: DMALRU4)

• Drug Name: 8-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info
• Synonyms: 8-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline; CHEMBL6857; BDBM50136494; AKOS022804102

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 10467319
  TTD Drug ID: DMALRU4

Molecule-Related Drug Atlas

Drug(s) Targeting 5-HT 2A receptor (HTR2A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[3]
ZOTEPINE	DMF3VXA	Anxiety disorder	6B00-6B0Z	Approved	[4]
Iloperidone	DM6AUFY	Schizophrenia	6A20	Approved	[5]
Flibanserin	DM70DTN	Depression	6A70-6A7Z	Approved	[6]
Lurasidone hydrochloride	DMCVPXO	Schizophrenia	6A20	Approved	[7]
Aniracetam	DMOIFW0	Cerebrovascular ischaemia	8B1Z	Approved	[8]
lumateperone tosylate	DMQ8HOJ	Schizophrenia	6A20	Approved	[9]
Sarpogrelate	DMGLP6S	Diabetic complication	5A2Y	Approved	[10]
Pimavanserin	DMR7IVC	Parkinson disease	8A00.0	Approved	[11]
Zicronapine	DMP8ESD	Schizophrenia	6A20	Phase 3	[12]

Drug(s) Targeting Monoamine oxidase type B (MAO-B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Selegiline Hydrochloride	DM3VR1L	Parkinson disease	8A00.0	Approved	[13]
Phenelzine	DMHIDUE	Depression	6A70-6A7Z	Approved	[14]
Tranylcypromine	DMGB5RE	Major depressive disorder	6A70.3	Approved	[15]
Selegiline	DM6034S	Major depressive disorder	6A70.3	Approved	[16]
Safinamide mesylate	DM0J2ZT	Parkinson disease	8A00.0	Approved	[17]
Rasagiline	DM3WKQ4	Parkinson disease	8A00.0	Approved	[18]
Sulphadoxine	DMZI2UF	Malaria	1F40-1F45	Approved	[19]
Pargyline	DMM0HR1	Hypertension	BA00-BA04	Approved	[20]
Indeloxazine	DMWO3N6	Dementia	6D80-6D86	Approved	[21]
Budipine	DMODHQI	Migraine	8A80	Approved	[22]

Drug(s) Targeting Monoamine oxidase type A (MAO-A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Moclobemide	DMNZWL7	Depression	6A70-6A7Z	Approved	[23]
Tranylcypromine	DMGB5RE	Major depressive disorder	6A70.3	Approved	[24]
Clorgyline	DMCEUJD	Parkinson disease	8A00.0	Approved	[25]
Isocarboxazid	DMAF1NB	Depression	6A70-6A7Z	Approved	[26]
TRYPTAMINE	DMAFPHB	N. A.	N. A.	Phase 3	[1]
Psoralen	DMIZJ8M	N. A.	N. A.	Phase 3	[27]
CHF-3381	DMQ2O8V	Neuropathic pain	8E43.0	Phase 2	[28]
Ladostigil	DMJSY3Q	Alzheimer disease	8A20	Phase 2	[29]
CX157	DMS2WB5	Mood disorder	6A60-6E23	Phase 2	[30]
PIPERINE	DMYEAB1	Vitiligo	ED63.0	Phase 1/2	[31]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 2A receptor (HTR2A)	TTJQOD7	5HT2A_HUMAN	Inhibitor	[2]
Monoamine oxidase type A (MAO-A)	TT3WG5C	AOFA_HUMAN	Inhibitor	[1]
Monoamine oxidase type B (MAO-B)	TTGP7BY	AOFB_HUMAN	Inhibitor	[1]

References

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• [3] 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.
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• [6] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
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• [9] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [10] 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.
• [11] 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.
• [12] Clinical pipeline report, company report or official report of Lundbeck.
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• [14] Limitation of adipose tissue enlargement in rats chronically treated with semicarbazide-sensitive amine oxidase and monoamine oxidase inhibitors. Pharmacol Res. 2008 Jun;57(6):426-34.
• [15] Tranylcypromine: new perspectives on an "old" drug. Eur Arch Psychiatry Clin Neurosci. 2006 Aug;256(5):268-73.
• [16] 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. (Target id: 2490).
• [17] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [18] Glyceraldehyde-3-phosphate dehydrogenase-monoamine oxidase B-mediated cell death-induced by ethanol is prevented by rasagiline and 1-R-aminoindan. Neurotox Res. 2009 Aug;16(2):148-59.
• [19] Novel monoamine oxidase inhibitors, 3-(2-aminoethoxy)-1,2-benzisoxazole derivatives, and their differential reversibility. Jpn J Pharmacol. 2002 Feb;88(2):174-82.
• [20] Dose-dependent activation of distinct hypertrophic pathways by serotonin in cardiac cells. Am J Physiol Heart Circ Physiol. 2009 Aug;297(2):H821-8.
• [21] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [22] Multiple mechanisms of action: the pharmacological profile of budipine. J Neural Transm Suppl. 1999;56:83-105.
• [23] Efficacy of citalopram and moclobemide in patients with social phobia: some preliminary findings. Hum Psychopharmacol. 2002 Dec;17(8):401-5.
• [24] Tramadol and another atypical opioid meperidine have exaggerated serotonin syndrome behavioural effects, but decreased analgesic effects, in genetically deficient serotonin transporter (SERT) mice. Int J Neuropsychopharmacol. 2009 Mar 11:1-11.
• [25] Further investigation into the mechanism of tachykinin NK(2) receptor-triggered serotonin release from guinea-pig proximal colon. J Pharmacol Sci. 2009 May;110(1):122-6.
• [26] MAOIs in the contemporary treatment of depression. Neuropsychopharmacology. 1995 May;12(3):185-219.
• [27] Inhibition of rat brain monoamine oxidase activities by psoralen and isopsoralen: implications for the treatment of affective disorders. Pharmacol Toxicol. 2001 Feb;88(2):75-80.
• [28] Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
• [29] Ladostigil: a novel multimodal neuroprotective drug with cholinesterase and brain-selective monoamine oxidase inhibitory activities for Alzheimer's disease treatment. Curr Drug Targets. 2012 Apr;13(4):483-94.
• [30] Reversible inhibitors of monoamine oxidase-A (RIMAs): robust, reversible inhibition of human brain MAO-A by CX157. Neuropsychopharmacology. 2010 Feb;35(3):623-31.
• [31] Proposed structural basis of interaction of piperine and related compounds with monoamine oxidases. Bioorg Med Chem Lett. 2010 Jan 15;20(2):537-40.