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

General Information of Drug (ID: DMW6C81)

• Drug Name: Eltoprazine Drug Info
• Synonyms: Piperazine derivative (ADHD), PsychoGenics/ReqMed Company; 5-HT1A/5-HT1B agonist and 5-HT2C antagonist (ADHD), PsychoGenics/ReqMed Company

Indication

Disease Entry	ICD 11	Status	REF
Attention deficit hyperactivity disorder	6A05.Z	Phase 3	[1]
Alzheimer disease	8A20	Phase 2	[2]
Dyskinesia	MB47.4	Phase 2	[3]
Non-hodgkin lymphoma	2B33.5	Phase 2	[4]
Parkinson disease	8A00.0	Phase 2	[2]

• Cross-matching ID:
  PubChem CID: 65853
  CAS Number: CAS 98224-03-4
  TTD Drug ID: DMW6C81

Molecule-Related Drug Atlas

Drug(s) Targeting 5-HT 1B receptor (HTR1B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[6]
Eletriptan	DMW649X	Migraine	8A80	Approved	[7]
Zolmitriptan	DM1IB4Q	Migraine	8A80	Approved	[7]
Frovatriptan	DM7RE8P	Migraine	8A80	Approved	[7]
Fluphenazine	DMIT8LX	Psychotic disorder	6A20-6A25	Approved	[7]
Naratriptan	DMO50U2	Headache	8A80-8A84	Approved	[8]
Prolixin decanoate	DMMJ1IS	Schizophrenia	6A20	Approved	[7]
NXN-188	DMMBAIH	Migraine	8A80	Phase 2	[9]
[N-methyl-3H(3)]AZ-10419369	DMSCV02	Mood disorder	6A60-6E23	Phase 1	[10]
Alniditan	DMFE3CT	Migraine	8A80	Discontinued in Phase 3	[11]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Trazodone	DMK1GBJ	Depression	6A70-6A7Z	Approved	[7]
Buspirone	DMBS632	Anxiety disorder	6B00-6B0Z	Approved	[12]
OPC-34712	DMHG57U	Major depressive disorder	6A70.3	Approved	[13]
Vilazodone	DM4LECQ	Major depressive disorder	6A70.3	Approved	[14]
Flibanserin	DM70DTN	Depression	6A70-6A7Z	Approved	[15]
Gepirone	DMGX5Q0	Major depressive disorder	6A70.3	Approved	[16]
TERTATOLOL	DM2L3D5	Hypertension	BA00-BA04	Approved	[17]
Urapidil	DMD59GI	Hypertension	BA00-BA04	Approved	[18]
Treximet	DMU54QB	Migraine	8A80	Approved	[19]
CM-2395	DMASPWR	Schizophrenia	6A20	Phase 3	[20]

Drug(s) Targeting 5-HT 2C receptor (HTR2C)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[21]
Lorcaserin	DMG6OYJ	Obesity	5B81	Approved	[22]
Tramadol	DMRQD04	Osteoarthritis	FA00-FA05	Approved	[23]
Mirtazapine	DML53ZJ	Depression	6A70-6A7Z	Approved	[24]
Nefazodone	DM4ZS8M	Major depressive disorder	6A70.3	Approved	[25]
Methysergide	DM1EF73	Migraine	8A80	Approved	[26]
M100907	DM7ZFBA	Sleep-wake disorder	7A00-7B2Z	Phase 3	[27]
SR46349B	DM1ODMR	Primary insomnia	7A00	Phase 3	[28]
Vabicaserin	DM9GZW6	Psychotic disorder	6A20-6A25	Phase 2	[29]
Nuplazid	DMOJA5G	Alzheimer disease	8A20	Phase 2	[30]

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	Agonist	[5]
5-HT 1B receptor (HTR1B)	TTK8CXU	5HT1B_HUMAN	Agonist	[5]
5-HT 2C receptor (HTR2C)	TTWJBZ5	5HT2C_HUMAN	Antagonist	[5]

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [4] ClinicalTrials.gov (NCT01266174) Effects of Eltoprazine on Cognitive Impairment Associated With Schizophrenia (CIAS) in Adults. U.S. National Institutes of Health.
• [5] Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
• [6] Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors. J Neurochem. 1996 Nov;67(5):2096-103.
• [7] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [8] Triptans in pregnancy. Ther Drug Monit. 2008 Feb;30(1):5-9.
• [9] Company report (NeurAxon)
• [10] 5-HT1B and other related serotonergic proteins are altered in APPswe mutation. Neurosci Lett. 2015 May 6;594:137-43.
• [11] Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br J Pharmacol. 1998 Apr;123(8):1655-65.
• [12] Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
• [13] 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.
• [14] 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
• [15] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [16] Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
• [17] 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).
• [18] Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
• [19] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [20] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
• [21] 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.
• [22] Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
• [23] The inhibitory effects of tramadol on 5-hydroxytryptamine type 2C receptors expressed in Xenopus oocytes. Anesth Analg. 2004 May;98(5):1401-6, table of contents.
• [24] Inverse agonist and neutral antagonist actions of antidepressants at recombinant and native 5-hydroxytryptamine2C receptors: differential modulatio... Mol Pharmacol. 2008 Mar;73(3):748-57.
• [25] Serotonin 5-HT2C receptors as a target for the treatment of depressive and anxious states: focus on novel therapeutic strategies. Therapie. 2005 Sep-Oct;60(5):441-60.
• [26] Spinal serotonin receptor activation modulates the exercise ventilatory response with increased dead space in goats. Respir Physiol Neurobiol. 2008 May 31;161(3):230-8.
• [27] Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists ... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3708-12.
• [28] SR46349-B, a 5-HT(2A/2C) receptor antagonist, potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens. Neuropsychopharmacology. 2002 Sep;27(3):430-41.
• [29] Prediction of Efficacy of Vabicaserin, a 5-HT2C Agonist, for the Treatment of Schizophrenia Using a Quantitative Systems Pharmacology Model.CPT Pharmacometrics Syst Pharmacol.2014 Apr 23;3:e111.
• [30] The neuropharmacology of sleep paralysis hallucinations: serotonin 2A activation and a novel therapeutic drug. Psychopharmacology (Berl). 2018 Nov;235(11):3083-3091.