Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTK8CXU)

• DTT Name: 5-HT 1B receptor (HTR1B)
• Synonyms: Serotonin receptor 1B; Serotonin 1D beta receptor; S12; HTR1DB; 5-hydroxytryptamine receptor 1B; 5-HT1B receptor; 5-HT1B; 5-HT-1D-beta; 5-HT-1B
• Gene Name: HTR1B
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: 5HT1B_HUMAN
• TTD ID: T07806
• Sequence:
  MEEPGAQCAPPPPAGSETWVPQANLSSAPSQNCSAKDYIYQDSISLPWKVLLVMLLALIT
  LATTLSNAFVIATVYRTRKLHTPANYLIASLAVTDLLVSILVMPISTMYTVTGRWTLGQV
  VCDFWLSSDITCCTASILHLCVIALDRYWAITDAVEYSAKRTPKRAAVMIALVWVFSISI
  SLPPFFWRQAKAEEEVSECVVNTDHILYTVYSTVGAFYFPTLLLIALYGRIYVEARSRIL
  KQTPNRTGKRLTRAQLITDSPGSTSSVTSINSRVPDVPSESGSPVYVNQVKVRVSDALLE
  KKKLMAARERKATKTLGIILGAFIVCWLPFFIISLVMPICKDACWFHLAIFDFFTWLGYL
  NSLINPIIYTMSNEDFKQAFHKLIRFKCTS
• Function: Functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Regulates the release of 5-hydroxytryptamine, dopamine and acetylcholine in the brain, and thereby affects neural activity, nociceptive processing, pain perception, mood and behavior. Besides, plays a role in vasoconstriction of cerebral arteries. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).
• KEGG Pathway:
  cAMP signaling pathway (hsa04024)
  Neuroactive ligand-receptor interaction (hsa04080)
  Serotonergic synapse (hsa04726)
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Serotonin receptors (R-HSA-390666)

Molecular Interaction Atlas (MIA) of This DTT

7 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Eletriptan	DMW649X	Migraine	8A80	Approved	[2]
Fluphenazine	DMIT8LX	Psychotic disorder	6A20-6A25	Approved	[2]
Frovatriptan	DM7RE8P	Migraine	8A80	Approved	[2]
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[3]
Naratriptan	DMO50U2	Headache	8A80-8A84	Approved	[1]
Prolixin decanoate	DMMJ1IS	Schizophrenia	6A20	Approved	[2]
Zolmitriptan	DM1IB4Q	Migraine	8A80	Approved	[2]

3 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Eltoprazine	DMW6C81	Attention deficit hyperactivity disorder	6A05.Z	Phase 3	[4]
NXN-188	DMMBAIH	Migraine	8A80	Phase 2	[5]
[N-methyl-3H(3)]AZ-10419369	DMSCV02	Mood disorder	6A60-6E23	Phase 1	[6]

10 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Alniditan	DMFE3CT	Migraine	8A80	Discontinued in Phase 3	[7]
Elzasonan hydrochloride	DM1EOC3	Mood disorder	6A60-6E23	Discontinued in Phase 2	[8]
IS-159	DMLQWFA	Migraine	8A80	Discontinued in Phase 2	[9]
Anpirtoline	DM35LJC	Pain	MG30-MG3Z	Terminated	[11]
AZD-1134	DMPCFRN	Anxiety disorder	6B00-6B0Z	Terminated	[12]
CGS-12066B	DM6MEX4	Anxiety disorder	6B00-6B0Z	Terminated	[13]
F-12682	DM23OHW	Major depressive disorder	6A70.3	Terminated	[14]
GR-127935	DM01HLX	Major depressive disorder	6A70.3	Terminated	[15]
L-775606	DMJ37IX	N. A.	N. A.	Terminated	[16]
VR-147	DMLWQOP	Migraine	8A80	Terminated	[17]

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Donitriptan	DMA2K7C	Migraine	8A80	Preclinical	[10]

41 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[18]
(R)-flurocarazolol	DM2KBOU	Discovery agent	N.A.	Investigative	[19]
(S)-flurocarazolol	DM715AS	Discovery agent	N.A.	Investigative	[19]
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine	DMX5N3V	Discovery agent	N.A.	Investigative	[20]
1-(7-Methoxy-naphthalen-2-yl)-piperazine	DM1MJCE	Discovery agent	N.A.	Investigative	[21]
1-Naphthalen-2-yl-piperazine	DMJK0MF	Discovery agent	N.A.	Investigative	[21]
1-naphthylpiperazine	DM6BIWK	Discovery agent	N.A.	Investigative	[3]
2-(5-Nonyloxy-1H-indol-3-yl)-ethylamine	DM2TU6W	Discovery agent	N.A.	Investigative	[22]
2-(5-Thiophen-2-yl-1H-indol-3-yl)-ethylamine	DM1AEK4	Discovery agent	N.A.	Investigative	[23]
2-methyl-5-HT	DM1S5CB	N. A.	N. A.	Investigative	[24]
5-amino-3-(N-methylpiperidin-4-yl)-1H-indole	DMJKQ5I	Discovery agent	N.A.	Investigative	[25]
5-CT	DM260KD	Discovery agent	N.A.	Investigative	[26]
5-Ethyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole	DMK57W2	Discovery agent	N.A.	Investigative	[27]
5-Isopropyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole	DMXGRMB	Discovery agent	N.A.	Investigative	[27]
5-OH-DPAT	DMZT6JR	Discovery agent	N.A.	Investigative	[26]
7-methoxy-1-naphthylpiperazine	DM3MXI5	Discovery agent	N.A.	Investigative	[21]
9-OH-risperidone	DMGORXQ	Discovery agent	N.A.	Investigative	[28]
A-987306	DMU34BK	Discovery agent	N.A.	Investigative	[29]
BRL-15572	DMM61Y2	Discovery agent	N.A.	Investigative	[30]
CP-94,253	DMHN2LT	Discovery agent	N.A.	Investigative	[31]
dipropyl-5-CT	DM9VKXC	Discovery agent	N.A.	Investigative	[24]
GR55562	DM8L1Z2	Discovery agent	N.A.	Investigative	[32]
L-747201	DMBPWSJ	Discovery agent	N.A.	Investigative	[16]
L-772,405	DM5O0CM	Discovery agent	N.A.	Investigative	[33]
lysergol	DM1OHF8	Discovery agent	N.A.	Investigative	[3]
SB 216641	DMB3R4Z	Discovery agent	N.A.	Investigative	[30]
SB 224289	DMIS8JQ	Discovery agent	N.A.	Investigative	[32]
SB 272183	DMOLNQX	Discovery agent	N.A.	Investigative	[34]
SB 649915	DM21Z6H	Discovery agent	N.A.	Investigative	[35]
SB 714786	DMGHRY0	Discovery agent	N.A.	Investigative	[35]
SB236057	DMYQDPM	Discovery agent	N.A.	Investigative	[36]
SEROTONIN	DMOFCRY	Discovery agent	N.A.	Investigative	[29]
TFMPP	DMAC8TP	Discovery agent	N.A.	Investigative	[3]
WAY-466	DMMOH51	Discovery agent	N.A.	Investigative	[37]
[11C]AZ10419369	DMMZUPX	Discovery agent	N.A.	Investigative	[38]
[125I]GTI	DMSYT5P	Discovery agent	N.A.	Investigative	[39]
[2-(5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amine	DMOZ73L	Discovery agent	N.A.	Investigative	[27]
[3H]8-OH-DPAT	DM4KCYU	Discovery agent	N.A.	Investigative	[40]
[3H]eletriptan	DMDTYRV	Discovery agent	N.A.	Investigative	[41]
[3H]GR 125,743	DM4URBO	Discovery agent	N.A.	Investigative	[42]
[3H]sumatriptan	DM3MBGV	Discovery agent	N.A.	Investigative	[41]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Major depressive disorder	6A20	Pre-frontal cortex	3.68E-03	0.16	0.92

References

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