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

General Information of Drug (ID: DM715AS)

• Drug Name: (S)-flurocarazolol Drug Info
• Synonyms: (S)-flurocarazolol; GTPL66; CHEMBL326418; SCHEMBL14155316; PDSP2_000794; PDSP1_000807

Indication

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

• Cross-matching ID:
  PubChem CID: 10358392
  TTD Drug ID: DM715AS

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	[3]
Eletriptan	DMW649X	Migraine	8A80	Approved	[4]
Zolmitriptan	DM1IB4Q	Migraine	8A80	Approved	[4]
Frovatriptan	DM7RE8P	Migraine	8A80	Approved	[4]
Fluphenazine	DMIT8LX	Psychotic disorder	6A20-6A25	Approved	[4]
Naratriptan	DMO50U2	Headache	8A80-8A84	Approved	[5]
Prolixin decanoate	DMMJ1IS	Schizophrenia	6A20	Approved	[4]
Eltoprazine	DMW6C81	Attention deficit hyperactivity disorder	6A05.Z	Phase 3	[6]
NXN-188	DMMBAIH	Migraine	8A80	Phase 2	[7]
[N-methyl-3H(3)]AZ-10419369	DMSCV02	Mood disorder	6A60-6E23	Phase 1	[8]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Trazodone	DMK1GBJ	Depression	6A70-6A7Z	Approved	[4]
Buspirone	DMBS632	Anxiety disorder	6B00-6B0Z	Approved	[9]
OPC-34712	DMHG57U	Major depressive disorder	6A70.3	Approved	[10]
Vilazodone	DM4LECQ	Major depressive disorder	6A70.3	Approved	[11]
Flibanserin	DM70DTN	Depression	6A70-6A7Z	Approved	[12]
Gepirone	DMGX5Q0	Major depressive disorder	6A70.3	Approved	[13]
TERTATOLOL	DM2L3D5	Hypertension	BA00-BA04	Approved	[14]
Urapidil	DMD59GI	Hypertension	BA00-BA04	Approved	[15]
Treximet	DMU54QB	Migraine	8A80	Approved	[16]
CM-2395	DMASPWR	Schizophrenia	6A20	Phase 3	[17]

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]
5-HT 1B receptor (HTR1B)	TTK8CXU	5HT1B_HUMAN	Antagonist	[2]

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: 66).
• [2] The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor. Psychopharmacology (Berl). 2001 Aug;157(1):111-4.
• [3] 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.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [5] Triptans in pregnancy. Ther Drug Monit. 2008 Feb;30(1):5-9.
• [6] Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
• [7] Company report (NeurAxon)
• [8] 5-HT1B and other related serotonergic proteins are altered in APPswe mutation. Neurosci Lett. 2015 May 6;594:137-43.
• [9] Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
• [10] 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.
• [11] 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
• [12] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [13] Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
• [14] 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).
• [15] Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
• [16] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [17] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)