Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTWM4TY)

• DTT Name: Adrenergic receptor alpha-2B (ADRA2B)
• Synonyms: Subtype C2; Alpha-2BAR; Alpha-2B adrenoreceptor; Alpha-2B adrenoceptor; Alpha-2B adrenergic receptor; Alpha-2 adrenergic receptor subtype C2; ADRA2RL1; ADRA2L1
• Gene Name: ADRA2B
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: ADA2B_HUMAN
• TTD ID: T41580
• Sequence:
  MDHQDPYSVQATAAIAAAITFLILFTIFGNALVILAVLTSRSLRAPQNLFLVSLAAADIL
  VATLIIPFSLANELLGYWYFRRTWCEVYLALDVLFCTSSIVHLCAISLDRYWAVSRALEY
  NSKRTPRRIKCIILTVWLIAAVISLPPLIYKGDQGPQPRGRPQCKLNQEAWYILASSIGS
  FFAPCLIMILVYLRIYLIAKRSNRRGPRAKGGPGQGESKQPRPDHGGALASAKLPALASV
  ASAREVNGHSKSTGEKEEGETPEDTGTRALPPSWAALPNSGQGQKEGVCGASPEDEAEEE
  EEEEEEEEECEPQAVPVSPASACSPPLQQPQGSRVLATLRGQVLLGRGVGAIGGQWWRRR
  AQLTREKRFTFVLAVVIGVFVLCWFPFFFSYSLGAICPKHCKVPHGLFQFFFWIGYCNSS
  LNPVIYTIFNQDFRRAFRRILCRPWTQTAW
• Function: The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phentolamine > mianserine > spiperone > prazosin > alprenolol > propanolol > pindolol. Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
• KEGG Pathway:
  cGMP-PKG signaling pathway (hsa04022)
  Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway:
  Adrenaline signalling through Alpha-2 adrenergic receptor (R-HSA-392023)
  G alpha (i) signalling events (R-HSA-418594)
  G alpha (z) signalling events (R-HSA-418597)
  Adrenoceptors (R-HSA-390696)

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MOXONIDINE	DMGFB0E	Alcohol dependence	6C40.2	Approved	[1]

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AGN-199981	DMP5Y1A	Neuropathic pain	8E43.0	Phase 2	[2]
MEDETOMIDINE	DMX9Y7V	Pain	MG30-MG3Z	Phase 2	[3]

6 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
INDORAMIN	DMNSJFD	Hypertension	BA00-BA04	Withdrawn from market	[4]
MAZAPERTINE	DMRHYAU	N. A.	N. A.	Discontinued in Phase 2	[5]
A-80426	DMBC3DG	N. A.	N. A.	Terminated	[6]
SK&F-104078	DMRADBU	N. A.	N. A.	Terminated	[4]
SNAP-5089	DMROJEN	Heart arrhythmia	BC65	Terminated	[7]
WB-4101	DMQU8B1	N. A.	N. A.	Terminated	[8]

57 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[9]
(1,2,3,4-Tetrahydro-isoquinolin-3-yl)-methanol	DMF6WHC	Discovery agent	N.A.	Investigative	[10]
(2-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine	DME6MYZ	Discovery agent	N.A.	Investigative	[11]
(3-Ethyl-indol-1-yl)-propyl-pyridin-4-yl-amine	DM5WJBH	Discovery agent	N.A.	Investigative	[11]
(3-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine	DMHED9G	Discovery agent	N.A.	Investigative	[11]
(R)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline	DM98L2X	Discovery agent	N.A.	Investigative	[12]
(S)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline	DMS4JAG	Discovery agent	N.A.	Investigative	[12]
1',2',3',6'-Tetrahydro-[2,4']bipyridinyl	DMFDK4N	Discovery agent	N.A.	Investigative	[13]
1,2,3,4,4a,5,10,10a-Octahydro-benzo[g]quinoline	DMDYX7P	Discovery agent	N.A.	Investigative	[14]
1,2,3,4,5,6-Hexahydro-benzo[c]azocine	DMTKYFE	Discovery agent	N.A.	Investigative	[12]
1,2,3,4-Tetrahydro-benzo[h]isoquinolin-8-ol	DMHKANE	Discovery agent	N.A.	Investigative	[15]
1,2,3,4-Tetrahydro-isoquinolin-7-ol	DM5VLIE	Discovery agent	N.A.	Investigative	[15]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole	DM3JGVF	Discovery agent	N.A.	Investigative	[16]
1,2,3,4-tetrahydroisoquinoline	DMZGCEQ	Discovery agent	N.A.	Investigative	[17]
1-(3-Fluoro-pyridin-2-yl)-4-methyl-piperazine	DMWFU3T	Discovery agent	N.A.	Investigative	[13]
1-(pyridin-2-yl)piperazine	DMKE7FG	Discovery agent	N.A.	Investigative	[13]
2,3,4,5-Tetrahydro-1H-benzo[c]azepine	DM1RE9Q	Discovery agent	N.A.	Investigative	[12]
2,3,4,5-Tetrahydro-1H-benzo[e][1,4]diazepine	DM4EZOB	Discovery agent	N.A.	Investigative	[12]
2,3,4,5-Tetrahydro-benzo[f][1,4]oxazepine	DMOFG4M	Discovery agent	N.A.	Investigative	[12]
2,3-Dihydro-1H-isoindole	DMWI9XS	Discovery agent	N.A.	Investigative	[12]
2-BFi	DMFAW4R	Discovery agent	N.A.	Investigative	[18]
3-Fluoromethyl-1,2,3,4-tetrahydro-isoquinoline	DMDPUC7	Discovery agent	N.A.	Investigative	[19]
3-Methoxymethyl-1,2,3,4-tetrahydro-isoquinoline	DMH1RX6	Discovery agent	N.A.	Investigative	[10]
3-Methyl-1,2,3,4-tetrahydro-isoquinoline	DMIWQ7G	Discovery agent	N.A.	Investigative	[12]
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole	DMFYBLH	Discovery agent	N.A.	Investigative	[3]
4-(4-Methyl-indan-1-yl)-1H-imidazole	DMYZHXR	Discovery agent	N.A.	Investigative	[20]
4-Benzo[b]thiophen-4-yl-1H-imidazole	DM02Q8N	Discovery agent	N.A.	Investigative	[21]
5-Aminomethyl-naphthalen-2-ol	DMTP9DB	Discovery agent	N.A.	Investigative	[15]
6,7,8,9-Tetrahydro-5-thia-8-aza-benzocycloheptene	DMNOI7B	Discovery agent	N.A.	Investigative	[12]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline	DMQ1BE8	Discovery agent	N.A.	Investigative	[22]
8-Methoxy-1,2,3,4-tetrahydro-benzo[h]isoquinoline	DMY50UR	Discovery agent	N.A.	Investigative	[15]
Butyl-indol-1-yl-pyridin-4-yl-amine	DM1CX9Y	Discovery agent	N.A.	Investigative	[11]
C-(6-Methoxy-naphthalen-1-yl)-methylamine	DMJ6SYI	Discovery agent	N.A.	Investigative	[15]
C-Naphthalen-1-yl-methylamine	DMFW1JC	Discovery agent	N.A.	Investigative	[15]
Ethyl-indol-1-yl-pyridin-4-yl-amine	DM3CWFR	Discovery agent	N.A.	Investigative	[11]
GNF-PF-2857	DML5QFZ	Discovery agent	N.A.	Investigative	[23]
GNF-PF-3878	DM7BXHQ	Discovery agent	N.A.	Investigative	[23]
imiloxan	DMS4D96	Discovery agent	N.A.	Investigative	[24]
Indol-1-yl-methyl-pyridin-4-yl-amine	DMJB876	Discovery agent	N.A.	Investigative	[11]
Indol-1-yl-prop-2-ynyl-pyridin-4-yl-amine	DMR9GNW	Discovery agent	N.A.	Investigative	[11]
Indol-1-yl-pyridin-4-yl-amine	DM1F53L	Discovery agent	N.A.	Investigative	[11]
JP1302	DMMVBK6	Discovery agent	N.A.	Investigative	[23]
METHYLNORADRENALINE	DMOWMPL	Discovery agent	N.A.	Investigative	[8]
MEZILAMINE	DMVYWJS	Discovery agent	N.A.	Investigative	[25]
PIPEROXAN	DMIHO0P	Discovery agent	N.A.	Investigative	[8]
R-226161	DM4BP7S	Discovery agent	N.A.	Investigative	[26]
S-34324	DMZLQ5W	Discovery agent	N.A.	Investigative	[6]
SK&F-64139	DM60Y3Q	Discovery agent	N.A.	Investigative	[17]
SNAP-5150	DM2OLGQ	Discovery agent	N.A.	Investigative	[7]
spiroxatrine	DMPHRXQ	Discovery agent	N.A.	Investigative	[27]
TRACIZOLINE	DM18CV3	Discovery agent	N.A.	Investigative	[22]
Tramazoline	DM3ML0N	Discovery agent	N.A.	Investigative	[8]
TRYPTOLINE	DMV19K7	Discovery agent	N.A.	Investigative	[22]
xylazine	DMSXJUW	Discovery agent	N.A.	Investigative	[28]
[3H]MK-912	DMO89N0	Discovery agent	N.A.	Investigative	[27]
[3H]rauwolscine	DMBQZ2H	Discovery agent	N.A.	Investigative	[29]
[3H]RX821002	DM6IRN4	Discovery agent	N.A.	Investigative	[30]

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