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

General Information of Drug (ID: DM31CVR)

• Drug Name: 1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine Drug Info
• Synonyms: CHEMBL160344; ZINC27714862; BDBM50226210

Indication

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

• Cross-matching ID:
  PubChem CID: 13599004
  TTD Drug ID: DM31CVR

Molecule-Related Drug Atlas

Drug(s) Targeting 5-HT 1D receptor (HTR1D)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[2]
Eletriptan	DMW649X	Migraine	8A80	Approved	[3]
Zolmitriptan	DM1IB4Q	Migraine	8A80	Approved	[3]
Frovatriptan	DM7RE8P	Migraine	8A80	Approved	[3]
Sumatriptan	DMVYXR8	Cluster headache	8A81.0	Approved	[4]
Rizatriptan	DMDJMA3	Migraine	8A80	Approved	[5]
Almogran	DM7I64Z	Migraine	8A80	Approved	[6]
Neu-P11	DMIQDFW	Alzheimer disease	8A20	Phase 2	[7]
FKB01MD	DM2O7NM	N. A.	N. A.	Phase 2	[8]
NXN-188	DMMBAIH	Migraine	8A80	Phase 2	[9]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[10]
ZOTEPINE	DMF3VXA	Anxiety disorder	6B00-6B0Z	Approved	[11]
Iloperidone	DM6AUFY	Schizophrenia	6A20	Approved	[12]
Flibanserin	DM70DTN	Depression	6A70-6A7Z	Approved	[13]
Lurasidone hydrochloride	DMCVPXO	Schizophrenia	6A20	Approved	[14]
Aniracetam	DMOIFW0	Cerebrovascular ischaemia	8B1Z	Approved	[15]
lumateperone tosylate	DMQ8HOJ	Schizophrenia	6A20	Approved	[16]
Sarpogrelate	DMGLP6S	Diabetic complication	5A2Y	Approved	[17]
Pimavanserin	DMR7IVC	Parkinson disease	8A00.0	Approved	[18]
Zicronapine	DMP8ESD	Schizophrenia	6A20	Phase 3	[19]

Drug(s) Targeting 5-HT 1A receptor (HTR1A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Trazodone	DMK1GBJ	Depression	6A70-6A7Z	Approved	[3]
Buspirone	DMBS632	Anxiety disorder	6B00-6B0Z	Approved	[20]
OPC-34712	DMHG57U	Major depressive disorder	6A70.3	Approved	[21]
Vilazodone	DM4LECQ	Major depressive disorder	6A70.3	Approved	[22]
Flibanserin	DM70DTN	Depression	6A70-6A7Z	Approved	[13]
Gepirone	DMGX5Q0	Major depressive disorder	6A70.3	Approved	[23]
TERTATOLOL	DM2L3D5	Hypertension	BA00-BA04	Approved	[24]
Urapidil	DMD59GI	Hypertension	BA00-BA04	Approved	[25]
Treximet	DMU54QB	Migraine	8A80	Approved	[26]
CM-2395	DMASPWR	Schizophrenia	6A20	Phase 3	[27]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 1A receptor (HTR1A)	TTSQIFT	5HT1A_HUMAN	Inhibitor	[1]
5-HT 1D receptor (HTR1D)	TT6MSOK	5HT1D_HUMAN	Inhibitor	[1]
5-HT 2A receptor (HTR2A)	TTJQOD7	5HT2A_HUMAN	Inhibitor	[1]

References

• [1] Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents. J Med Chem. 1986 May;29(5):630-4.
• [2] Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. Mol Pharmacol. 1991 Aug;40(2):143-8.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [4] Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32.
• [5] An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210.
• [6] Efficacy and tolerability of subcutaneous almotriptan for the treatment of acute migraine: a randomized, double-blind, parallel-group, dose-finding study. Clin Ther. 2001 Nov;23(11):1867-75.
• [7] Clinical pipeline report, company report or official report of Neurim Pharmaceuticals.
• [8] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [9] Company report (NeurAxon)
• [10] 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.
• [11] Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
• [12] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [13] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [14] Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
• [15] 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.
• [16] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [17] 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.
• [18] 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.
• [19] Clinical pipeline report, company report or official report of Lundbeck.
• [20] Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
• [21] 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.
• [22] 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
• [23] Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
• [24] 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).
• [25] Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
• [26] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [27] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)