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

General Information of Drug (ID: DM9IU21)

• Drug Name: LY 165,163 Drug Info
• Synonyms: PAPP; LY-165163

Indication

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

• Cross-matching ID:
  PubChem CID: 121930
  ChEBI ID: CHEBI:92250
  CAS Number: CAS 1814-64-8
  TTD Drug ID: DM9IU21

Molecule-Related Drug Atlas

Drug(s) Targeting 5-HT 6 receptor (HTR6)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LU AE58054	DMWGRQD	Schizophrenia	6A20	Phase 3	[4]
SB-742457	DM6L4ZT	Alzheimer disease	8A20	Phase 3	[5]
AVN 211	DMVB4OS	Schizophrenia	6A20	Phase 2/3	[6]
SYN120	DMDF7XB	Parkinson disease	8A00.0	Phase 2	[7]
AVN 101	DMJFLBC	Alzheimer disease	8A20	Phase 2	[6]
SYN-120	DMPW0UL	Alzheimer disease	8A20	Phase 2	[8]
PF-05212377	DMPVQYR	Alzheimer disease	8A20	Phase 2	[9]
AVN 322	DMK2LGM	Cognitive impairment	6D71	Phase 2	[5]
SAM-531	DMHVJZ6	Alzheimer disease	8A20	Phase 2	[10]
SUVN-502	DMQD753	Alzheimer disease	8A20	Phase 2	[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	[12]
Buspirone	DMBS632	Anxiety disorder	6B00-6B0Z	Approved	[13]
OPC-34712	DMHG57U	Major depressive disorder	6A70.3	Approved	[14]
Vilazodone	DM4LECQ	Major depressive disorder	6A70.3	Approved	[15]
Flibanserin	DM70DTN	Depression	6A70-6A7Z	Approved	[16]
Gepirone	DMGX5Q0	Major depressive disorder	6A70.3	Approved	[17]
TERTATOLOL	DM2L3D5	Hypertension	BA00-BA04	Approved	[18]
Urapidil	DMD59GI	Hypertension	BA00-BA04	Approved	[19]
Treximet	DMU54QB	Migraine	8A80	Approved	[20]
CM-2395	DMASPWR	Schizophrenia	6A20	Phase 3	[21]

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	[2]
5-HT 6 receptor (HTR6)	TTJS8PY	5HT6R_HUMAN	Agonist	[3]

References

• [1] 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: 18).
• [2] Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. Eur J Pharmacol. 1998 Aug 21;355(2-3):245-56.
• [3] Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol Pharmacol. 1993 Mar;43(3):320-7.
• [4] Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. Int J Neuropsychopharmacol. 2010 Sep;13(8):1021-33.
• [5] 5-HT6 receptors and Alzheimer's disease. Alzheimers Res Ther. 2013; 5(2): 15.
• [6] Latrepirdine, a potential novel treatment for Alzheimer's disease and Huntington's chorea. Curr Opin Investig Drugs. 2010 January; 11(1): 80-91.
• [7] Therapeutic strategies for Parkinson disease: beyond dopaminergic drugs. Nat Rev Drug Discov. 2018 Nov;17(11):804-822.
• [8] The Serotonin-6 Receptor as a Novel Therapeutic Target. Exp Neurobiol. 2011 December; 20(4): 159-168.
• [9] PF-05212377 Alzheimer's Disease (Phase 2). Pfizer.
• [10] Activation of 5-HT6 receptors modulates sleep-wake activity and hippocampal theta oscillation. ACS Chem Neurosci. 2013 Jan 16;4(1):191-9.
• [11] Novel and Potent 5-Piperazinyl Methyl-N1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands. ACS Med Chem Lett. 2010 October 14; 1(7): 340-344.
• [12] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [13] Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
• [14] 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.
• [15] 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
• [16] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [17] Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
• [18] 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).
• [19] Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
• [20] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [21] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)