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

General Information of Drug (ID: DM4EZOB)

• Drug Name: 2,3,4,5-Tetrahydro-1H-benzo[e][1,4]diazepine Drug Info
• Synonyms: 2,3,4,5-Tetrahydro-1H-benzo[e][1,4]diazepine; 5946-39-4; 2,3,4,5-tetrahydro-1H-1,4-benzodiazepine; CHEMBL323692; 1H-1,4-Benzodiazepine, 2,3,4,5-tetrahydro-; 2,3,4,5-tetrahydro-(1h)-1,4-benzodiazepine; 2,3,4,5-tetrahydro-1h benzo[e][1,4]diazepine; AC1MCKFZ; PubChem14772; ACMC-1ANOK; tetrahydrobenzo[1,4]diazepine; SCHEMBL379799; BEN206; BEN025; AC1Q1I93; KS-00001OTC; CTK1G9067; DTXSID20378071; MolPort-000-006-540; MLXBHOCKBUILHN-UHFFFAOYSA-N; ZINC2511438; STL554215; CT-889; BDBM50052888; MFCD03789577; BBL100421; AKOS005254212

Indication

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

• Cross-matching ID:
  PubChem CID: 2771762
  CAS Number: CAS 5946-39-4
  TTD Drug ID: DM4EZOB

Molecule-Related Drug Atlas

Drug(s) Targeting Adrenergic receptor alpha-2C (ADRA2C)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MOXONIDINE	DMGFB0E	Alcohol dependence	6C40.2	Approved	[2]
Dihydroergocristine	DM5SQ1G	Alcohol dependence	6C40.2	Approved	[3]
Brimonidine	DMQLT4N	Ocular hypertension	9C61.01	Approved	[4]
Amosulalol	DML8QSZ	Hypertension	BA00-BA04	Approved	[5]
Amezinium	DM6I2WQ	Hypotension	BA20-BA21	Approved	[6]
Propylhexedrine	DMTBW2O	Obesity	5B81	Approved	[7]
Tetrahydrozoline	DMT57WC	Ocular disease	1F00.1Z	Approved	[8]
Rilmenidine	DM13PQW	Hypertension	BA00-BA04	Approved	[9]
Xylometazoline	DMKV32D	Allergic rhinitis	CA08.0	Phase 4	[10]
TNX-102	DMO1234	Fibromyalgia	MG30.01	Phase 3	[11]

Drug(s) Targeting Adrenergic receptor alpha-2A (ADRA2A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lofexidine	DM1WXA6	Heroin and opiate withdrawal	6C43	Approved	[12]
MOXONIDINE	DMGFB0E	Alcohol dependence	6C40.2	Approved	[2]
Connexyn	DMF29Q5	Attention deficit hyperactivity disorder	6A05.Z	Approved	[13]
Guanfacine	DMPN5IH	Attention deficit hyperactivity disorder	6A05.Z	Phase 4	[14]
A295	DM55GO2	Aggressive cancer	2A00-2F9Z	IND submitted	[15]
MEDETOMIDINE	DMX9Y7V	Pain	MG30-MG3Z	Phase 2	[16]
DSP-1200	DM4WSHG	Depression	6A70-6A7Z	Phase 1	[17]
MAZAPERTINE	DMRHYAU	N. A.	N. A.	Discontinued in Phase 2	[18]
NMI-870	DMU596F	Sexual dysfunction	HA00-HA01	Discontinued in Phase 2	[19]
SNAP-5089	DMROJEN	Heart arrhythmia	BC65	Terminated	[20]

Drug(s) Targeting Adrenergic receptor alpha-2B (ADRA2B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MOXONIDINE	DMGFB0E	Alcohol dependence	6C40.2	Approved	[2]
MEDETOMIDINE	DMX9Y7V	Pain	MG30-MG3Z	Phase 2	[16]
AGN-199981	DMP5Y1A	Neuropathic pain	8E43.0	Phase 2	[21]
INDORAMIN	DMNSJFD	Hypertension	BA00-BA04	Withdrawn from market	[22]
MAZAPERTINE	DMRHYAU	N. A.	N. A.	Discontinued in Phase 2	[18]
SNAP-5089	DMROJEN	Heart arrhythmia	BC65	Terminated	[20]
A-80426	DMBC3DG	N. A.	N. A.	Terminated	[23]
WB-4101	DMQU8B1	N. A.	N. A.	Terminated	[24]
SK&F-104078	DMRADBU	N. A.	N. A.	Terminated	[22]
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[25]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Adrenergic receptor alpha-2A (ADRA2A)	TTWG9A4	ADA2A_HUMAN	Inhibitor	[1]
Adrenergic receptor alpha-2B (ADRA2B)	TTWM4TY	ADA2B_HUMAN	Inhibitor	[1]
Adrenergic receptor alpha-2C (ADRA2C)	TT2NUT5	ADA2C_HUMAN	Inhibitor	[1]

References

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• [9] Rilmenidine-induced ocular hypotension: role of imidazoline1 and alpha 2 receptors. Curr Eye Res. 1996 Sep;15(9):943-50.
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• [12] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [13] alpha2A-adrenergic receptors heterosynaptically regulate glutamatergic transmission in the bed nucleus of the stria terminalis. Neuroscience. 2009 Sep 29;163(1):339-51.
• [14] Scientific rationale for the use of alpha2A-adrenoceptor agonists in treating neuroinflammatory cognitive disorders. Mol Psychiatry. 2023 Apr 7:1-13.
• [15] Clinical pipeline report, company report or official report of Klus Pharma
• [16] A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic recep... J Med Chem. 1994 Jul 22;37(15):2328-33.
• [17] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [18] A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. J Med Chem. 1994 Apr 15;37(8):1060-2.
• [19] Female Sexual Dysfunction: Therapeutic Options and Experimental Challenges. Cardiovasc Hematol Agents Med Chem. 2009 October; 7(4): 260-269.
• [20] Design and synthesis of novel dihydropyridine alpha-1a antagonists. Bioorg Med Chem Lett. 1999 Oct 4;9(19):2843-8.
• [21] Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
• [22] Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. J Med Chem. 1995 Sep 1;38(18):3415-44.
• [23] Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking... J Med Chem. 2005 Mar 24;48(6):2054-71.
• [24] alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs. J Med Chem. 1982 Dec;25(12):1389-401.
• [25] Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.