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

General Information of Drug (ID: DMTLNGV)

• Drug Name: Umespirone Drug Info
• Synonyms: KC-7218; KC-9172

Indication

Disease Entry	ICD 11	Status	REF
Anxiety disorder	6B00-6B0Z	Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 65902
  CAS Number: CAS 107736-98-1
  TTD Drug ID: DMTLNGV

Molecule-Related Drug Atlas

Drug(s) Targeting Dopamine D2 receptor (D2R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dopamine	DMPGUCF	Acromegaly	5A60.0	Approved	[3]
Haloperidol	DM96SE0	Delirium		Approved	[4]
Perphenazine	DMA4MRX	Schizophrenia	6A20	Approved	[5]
Perazine	DM2AOTZ	Psychotic disorder	6A20-6A25	Approved	[6]
Domperidone	DMBDPY0	Gastrointestinal disease	DE2Z	Approved	[7]
Levodopa	DMN3E57	Parkinson disease	8A00.0	Approved	[8]
Quetiapine	DM1N62C	Anorexia nervosa cachexia	6B80	Approved	[9]
Pimozide	DMW83TP	Schizophrenia	6A20	Approved	[10]
Chlorpromazine	DMBGZI3	Acute intermittent hepatic porphyria	5C58.11	Approved	[11]
Iloperidone	DM6AUFY	Schizophrenia	6A20	Approved	[12]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Trazodone	DMK1GBJ	Depression	6A70-6A7Z	Approved	[13]
Buspirone	DMBS632	Anxiety disorder	6B00-6B0Z	Approved	[14]
OPC-34712	DMHG57U	Major depressive disorder	6A70.3	Approved	[15]
Vilazodone	DM4LECQ	Major depressive disorder	6A70.3	Approved	[16]
Flibanserin	DM70DTN	Depression	6A70-6A7Z	Approved	[17]
Gepirone	DMGX5Q0	Major depressive disorder	6A70.3	Approved	[18]
TERTATOLOL	DM2L3D5	Hypertension	BA00-BA04	Approved	[19]
Urapidil	DMD59GI	Hypertension	BA00-BA04	Approved	[20]
Treximet	DMU54QB	Migraine	8A80	Approved	[21]
CM-2395	DMASPWR	Schizophrenia	6A20	Phase 3	[22]

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	Antagonist	[2]
Dopamine D2 receptor (D2R)	TTEX248	DRD2_HUMAN	Antagonist	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000698)
• [2] The effects of umespirone as a potential anxiolytic and antipsychotic agent. Pharmacol Biochem Behav. 1991 Sep;40(1):89-96.
• [3] 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.
• [4] Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
• [5] CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
• [6] 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.
• [7] Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
• [8] 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).
• [9] Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
• [10] [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
• [11] 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.
• [12] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [13] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [14] Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
• [15] 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.
• [16] 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
• [17] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [18] Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
• [19] 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).
• [20] Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
• [21] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [22] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)