Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: Adrenergic receptor alpha-1B (ADRA1B)
• Synonyms: Alpha-1B adrenoreceptor; Alpha-1B adrenoceptor; Alpha-1B adrenergic receptor; Alpha 1B-adrenoreceptor; Alpha 1B-adrenoceptor
• Gene Name: ADRA1B
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: ADA1B_HUMAN
• TTD ID: T29500
• Sequence:
  MNPDLDTGHNTSAPAHWGELKNANFTGPNQTSSNSTLPQLDITRAISVGLVLGAFILFAI
  VGNILVILSVACNRHLRTPTNYFIVNLAMADLLLSFTVLPFSAALEVLGYWVLGRIFCDI
  WAAVDVLCCTASILSLCAISIDRYIGVRYSLQYPTLVTRRKAILALLSVWVLSTVISIGP
  LLGWKEPAPNDDKECGVTEEPFYALFSSLGSFYIPLAVILVMYCRVYIVAKRTTKNLEAG
  VMKEMSNSKELTLRIHSKNFHEDTLSSTKAKGHNPRSSIAVKLFKFSREKKAAKTLGIVV
  GMFILCWLPFFIALPLGSLFSTLKPPDAVFKVVFWLGYFNSCLNPIIYPCSSKEFKRAFV
  RILGCQCRGRGRRRRRRRRRLGGCAYTYRPWTRGGSLERSQSRKDSLDDSGSCLSGSQRT
  LPSASPSPGYLGRGAPPPVELCAFPEWKAPGALLSLPAPEPPGRRGRHDSGPLFTFKLLT
  EPESPGTDGGASNGGCEAAADVANGQPGFKSNMPLAPGQF
• Function: Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes. This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  cGMP-PKG signaling pathway (hsa04022)
  Neuroactive ligand-receptor interaction (hsa04080)
  Adrenergic signaling in cardiomyocytes (hsa04261)
  Vascular smooth muscle contraction (hsa04270)
  Salivary secretion (hsa04970)
• Reactome Pathway:
  G alpha (q) signalling events (R-HSA-416476)
  G alpha (12/13) signalling events (R-HSA-416482)
  Adrenoceptors (R-HSA-390696)

Molecular Interaction Atlas (MIA) of This DTT

4 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methamphetamine	DMPM4SK	Anxiety		Approved	[2]
Methoxamine	DMF5XQH	Hypertension	BA00-BA04	Approved	[3]
Phendimetrazine	DM6TS1N	Obesity	5B81	Approved	[4]
Propericiazine	DME9JNL	Psychiatric disorder	6E8Z	Approved	[1]

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MEDETOMIDINE	DMX9Y7V	Pain	MG30-MG3Z	Phase 2	[5]

13 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sunepitron	DM6M8ZX	N. A.	N. A.	Discontinued in Phase 3	[6]
TIOSPIRONE	DME5QDP	N. A.	N. A.	Discontinued in Phase 3	[7]
MAZAPERTINE	DMRHYAU	N. A.	N. A.	Discontinued in Phase 2	[8]
SOU-001	DMPAEK5	Urinary incontinence	MF50.2	Discontinued in Phase 2	[9]
ABANOQUIL	DMDOQCV	N. A.	N. A.	Terminated	[10]
AGN-193080	DMVS6BN	N. A.	N. A.	Terminated	[11]
BMY-7378	DMRHCEG	N. A.	N. A.	Terminated	[12]
NIGULDIPINE	DMSPWMF	N. A.	N. A.	Terminated	[13]
Siramesine	DMB6T7K	N. A.	N. A.	Terminated	[14]
SK&F-104078	DMRADBU	N. A.	N. A.	Terminated	[13]
SK&F-104856	DMN91EK	N. A.	N. A.	Terminated	[13]
SNAP-5089	DMROJEN	Heart arrhythmia	BC65	Terminated	[13]
WB-4101	DMQU8B1	N. A.	N. A.	Terminated	[10]

44 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[15]
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine	DM27TH9	Discovery agent	N.A.	Investigative	[16]
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine	DM8N79M	Discovery agent	N.A.	Investigative	[16]
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline	DM5D09Q	Discovery agent	N.A.	Investigative	[17]
4-((E)-1-Naphthalen-1-yl-propenyl)-1H-imidazole	DMDOJ4E	Discovery agent	N.A.	Investigative	[18]
4-((Z)-1-Naphthalen-1-yl-propenyl)-1H-imidazole	DM1UK3G	Discovery agent	N.A.	Investigative	[18]
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole	DMFYBLH	Discovery agent	N.A.	Investigative	[5]
4-(1-Naphthalen-1-yl-propyl)-1H-imidazole	DM64THP	Discovery agent	N.A.	Investigative	[18]
4-(1-Naphthalen-1-yl-vinyl)-1H-imidazole	DM49PR1	Discovery agent	N.A.	Investigative	[18]
4-(2,3-Dihydro-1H-phenalen-1-yl)-1H-imidazole	DMVIQ7F	Discovery agent	N.A.	Investigative	[18]
4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline	DMCOJIL	Discovery agent	N.A.	Investigative	[17]
4-(3-Hydroxy-piperidin-3-yl)-benzene-1,2-diol	DMUQWJZ	Discovery agent	N.A.	Investigative	[19]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[20]
4-(4-Isopropyl-morpholin-2-yl)-benzene-1,2-diol	DMC9Z45	Discovery agent	N.A.	Investigative	[19]
4-(4-Methyl-indan-1-yl)-1H-imidazole	DMYZHXR	Discovery agent	N.A.	Investigative	[21]
4-Benzo[b]thiophen-4-yl-1H-imidazole	DM02Q8N	Discovery agent	N.A.	Investigative	[22]
4-Morpholin-2-yl-benzene-1,2-diol	DM049QO	Discovery agent	N.A.	Investigative	[19]
5-methylurapidil	DMCX9WN	Discovery agent	N.A.	Investigative	[23]
6-fluoronorepinehprine	DMPWXI8	Discovery agent	N.A.	Investigative	[24]
A-119637	DM1DWRN	Discovery agent	N.A.	Investigative	[25]
A-123189	DMZ51UJ	Discovery agent	N.A.	Investigative	[25]
AGN-192172	DM946RA	Discovery agent	N.A.	Investigative	[11]
AH 11110	DMF7ZYQ	Discovery agent	N.A.	Investigative	[26]
CORYNANTHEINE	DM18CUZ	Discovery agent	N.A.	Investigative	[13]
Cyclazosin	DMPXHO8	Discovery agent	N.A.	Investigative	[27]
FLUANISONE	DMQSDM7	Discovery agent	N.A.	Investigative	[28]
Imidazolidin-2-ylidene-o-tolyl-amine	DMTGRAF	Discovery agent	N.A.	Investigative	[11]
Imidazolidin-2-ylidene-quinoxalin-6-yl-amine	DMZ5ISH	Discovery agent	N.A.	Investigative	[11]
ISOCLOZAPINE	DM52CPU	Discovery agent	N.A.	Investigative	[29]
LEVONORDEFRIN	DMWDJ0H	Discovery agent	N.A.	Investigative	[18]
N-(5-Bromo-quinoxalin-6-yl)-guanidine	DMD5E8G	Discovery agent	N.A.	Investigative	[11]
OCTOCLOTHEPIN	DM0UADK	Discovery agent	N.A.	Investigative	[30]
Rec 15/2615	DM386JM	Discovery agent	N.A.	Investigative	[31]
RWJ-68157	DMUK7LX	Discovery agent	N.A.	Investigative	[32]
RWJ-69736	DM2EOBM	Discovery agent	N.A.	Investigative	[32]
SK&F-105854	DMYRKEJ	Discovery agent	N.A.	Investigative	[13]
SK&F-106686	DMHETY7	Discovery agent	N.A.	Investigative	[13]
SK&F-86466	DM4RHEZ	Discovery agent	N.A.	Investigative	[13]
SNAP-8719	DMCHPMA	Discovery agent	N.A.	Investigative	[12]
spiroxatrine	DMPHRXQ	Discovery agent	N.A.	Investigative	[23]
UH-301	DM5NYWV	N. A.	N. A.	Investigative	[33]
[125I]BE-2254	DM7GVYF	Discovery agent	N.A.	Investigative	[34]
[125I]HEAT	DMTFP5Q	Discovery agent	N.A.	Investigative	[35]
[3H]RX821002	DM6IRN4	Discovery agent	N.A.	Investigative	[36]

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