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

General Information of Drug (ID: DMGFB0E)

• Drug Name: MOXONIDINE Drug Info
• Synonyms: BDF-5895; BE-5895; Normoxin; AC1OCENE; SCHEMBL1230620; Moxonidine hydrochloride hydrate; moxonidine hydrochloride monohydrate; LY-326869; 4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methylpyrimidin-5-amine hydrate hydrochloride

Indication

Disease Entry	ICD 11	Status	REF
Alcohol dependence	6C40.2	Approved	[1]

• Cross-matching ID:
  PubChem CID: 4810
  ChEBI ID: CHEBI:7009
  CAS Number: CAS 75438-57-2
  TTD Drug ID: DMGFB0E

Molecule-Related Drug Atlas

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dihydroergocristine	DM5SQ1G	Alcohol dependence	6C40.2	Approved	[4]
Brimonidine	DMQLT4N	Ocular hypertension	9C61.01	Approved	[5]
Amosulalol	DML8QSZ	Hypertension	BA00-BA04	Approved	[6]
Amezinium	DM6I2WQ	Hypotension	BA20-BA21	Approved	[7]
Propylhexedrine	DMTBW2O	Obesity	5B81	Approved	[8]
Tetrahydrozoline	DMT57WC	Ocular disease	1F00.1Z	Approved	[9]
Rilmenidine	DM13PQW	Hypertension	BA00-BA04	Approved	[10]
Xylometazoline	DMKV32D	Allergic rhinitis	CA08.0	Phase 4	[11]
TNX-102	DMO1234	Fibromyalgia	MG30.01	Phase 3	[12]
IDAZOXAN HYDROCHLORIDE	DMSP0X8	Neurological disorder	6B60	Phase 3	[13]

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	[14]
Connexyn	DMF29Q5	Attention deficit hyperactivity disorder	6A05.Z	Approved	[15]
Guanfacine	DMPN5IH	Attention deficit hyperactivity disorder	6A05.Z	Phase 4	[16]
A295	DM55GO2	Aggressive cancer	2A00-2F9Z	IND submitted	[17]
MEDETOMIDINE	DMX9Y7V	Pain	MG30-MG3Z	Phase 2	[18]
DSP-1200	DM4WSHG	Depression	6A70-6A7Z	Phase 1	[19]
MAZAPERTINE	DMRHYAU	N. A.	N. A.	Discontinued in Phase 2	[20]
NMI-870	DMU596F	Sexual dysfunction	HA00-HA01	Discontinued in Phase 2	[21]
SNAP-5089	DMROJEN	Heart arrhythmia	BC65	Terminated	[22]
A-80426	DMBC3DG	N. A.	N. A.	Terminated	[23]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MEDETOMIDINE	DMX9Y7V	Pain	MG30-MG3Z	Phase 2	[18]
AGN-199981	DMP5Y1A	Neuropathic pain	8E43.0	Phase 2	[24]
INDORAMIN	DMNSJFD	Hypertension	BA00-BA04	Withdrawn from market	[25]
MAZAPERTINE	DMRHYAU	N. A.	N. A.	Discontinued in Phase 2	[20]
SNAP-5089	DMROJEN	Heart arrhythmia	BC65	Terminated	[22]
A-80426	DMBC3DG	N. A.	N. A.	Terminated	[23]
WB-4101	DMQU8B1	N. A.	N. A.	Terminated	[26]
SK&F-104078	DMRADBU	N. A.	N. A.	Terminated	[25]
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[27]
R-226161	DM4BP7S	Discovery agent	N.A.	Investigative	[28]

Drug(s) Affected By Insulin (INS)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tolbutamide	DM02AWV	Advanced cancer	2A00-2F9Z	Approved	[29]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[30]
Epinephrine	DM3KJBC	Acute asthma	CA23	Approved	[31]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[32]
Fructose	DM43AN2	Vomiting	MD90	Approved	[33]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[34]
Glimepiride	DM5FSJA	Diabetic complication	5A2Y	Approved	[35]
Clonidine	DM6RZ9Q	Attention deficit hyperactivity disorder	6A05.Z	Approved	[36]
Propranolol	DM79NTF	Angina pectoris	BA40	Approved	[37]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[38]

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	[2]
Adrenergic receptor alpha-2B (ADRA2B)	TTWM4TY	ADA2B_HUMAN	Inhibitor	[2]
Adrenergic receptor alpha-2C (ADRA2C)	TT2NUT5	ADA2C_HUMAN	Inhibitor	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Insulin (INS)	OTZ85PDU	INS_HUMAN	Gene/Protein Processing	[3]

References

• [1] The role of I(1)-imidazoline and alpha(2)-adrenergic receptors in the modulation of glucose metabolism in the spontaneously hypertensive obese rat ... J Pharmacol Exp Ther. 2003 Aug;306(2):646-57.
• [2] Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent. J Med Chem. 1996 Mar 15;39(6):1193-5.
• [3] Selective imidazoline agonist moxonidine in obese hypertensive patients. Int J Clin Pract. 2006 May;60(5):621-9. doi: 10.1111/j.1368-5031.2006.00951.x.
• [4] Effect of dihydroergocristine on blood pressure and activity at peripheral alpha-adrenoceptors in pithed rats. Eur J Pharmacol. 1984 Jan 13;97(1-2):21-7.
• [5] 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: 520).
• [6] Effects of amosulalol, a combined alpha 1- and beta-adrenoceptor-blocking agent, on ischemic myocardial energy metabolism in dogs. J Pharm Sci. 1993 Mar;82(3):291-5.
• [7] Pharmacology of amezinium, a novel antihypotensive drug. III. Studies on the mechanism of action. Arzneimittelforschung. 1981;31(9a):1558-65.
• [8] Airway compromise and delayed death following attempted central vein injection of propylhexedrine. J Emerg Med. 1994 Nov-Dec;12(6):795-7.
• [9] Prolonged cardiovascular effects after unintentional ingestion of tetrahydrozoline. Clin Toxicol (Phila). 2008 Feb;46(2):171-2.
• [10] Rilmenidine-induced ocular hypotension: role of imidazoline1 and alpha 2 receptors. Curr Eye Res. 1996 Sep;15(9):943-50.
• [11] Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2010 Dec;24(6):729-39.
• [12] Clinical pipeline report, company report or official report of Tonix Pharmaceuticals.
• [13] Different sites of action for alpha 2-adrenoceptor antagonists in the modulation of noradrenaline release and contraction response in the vas deferens of the rat. J Pharm Pharmacol. 1992 Mar;44(3):231-4.
• [14] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [15] alpha2A-adrenergic receptors heterosynaptically regulate glutamatergic transmission in the bed nucleus of the stria terminalis. Neuroscience. 2009 Sep 29;163(1):339-51.
• [16] Scientific rationale for the use of alpha2A-adrenoceptor agonists in treating neuroinflammatory cognitive disorders. Mol Psychiatry. 2023 Apr 7:1-13.
• [17] Clinical pipeline report, company report or official report of Klus Pharma
• [18] 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.
• [19] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [20] 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.
• [21] Female Sexual Dysfunction: Therapeutic Options and Experimental Challenges. Cardiovasc Hematol Agents Med Chem. 2009 October; 7(4): 260-269.
• [22] Design and synthesis of novel dihydropyridine alpha-1a antagonists. Bioorg Med Chem Lett. 1999 Oct 4;9(19):2843-8.
• [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] Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
• [25] 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.
• [26] alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs. J Med Chem. 1982 Dec;25(12):1389-401.
• [27] Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
• [28] Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-a... Bioorg Med Chem. 2007 Jun 1;15(11):3649-60.
• [29] Amino acid polymorphisms in the ATP-regulatable inward rectifier Kir6.2 and their relationships to glucose- and tolbutamide-induced insulin secretion, the insulin sensitivity index, and NIDDM. Diabetes. 1997 Mar;46(3):508-12. doi: 10.2337/diab.46.3.508.
• [30] The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
• [31] A receptor mechanism for the inhibition of insulin release by epinephrine in man. J Clin Invest. 1967 Jan;46(1):86-94. doi: 10.1172/JCI105514.
• [32] Vasodilatory effects of troglitazone improve blood pressure at rest and during mental stress in type 2 diabetes mellitus. Hypertension. 1999 Jul;34(1):83-8. doi: 10.1161/01.hyp.34.1.83.
• [33] Quinapril treatment restores the vasodilator action of insulin in fructose-hypertensive rats. Clin Exp Pharmacol Physiol. 2002 May-Jun;29(5-6):381-5. doi: 10.1046/j.1440-1681.2002.03668.x.
• [34] Retinoic acid can induce markers of endocrine transdifferentiation in pancreatic ductal adenocarcinoma: preliminary observations from an in vitro cell line model. J Clin Pathol. 2006 Jun;59(6):603-10. doi: 10.1136/jcp.2005.032003. Epub 2006 Feb 10.
• [35] Effects of prolonged in vitro exposure to sulphonylureas on the function and survival of human islets. J Diabetes Complications. 2005 Jan-Feb;19(1):60-4. doi: 10.1016/j.jdiacomp.2004.05.001.
• [36] Clonidine effect on insulin secretion and lipolysis in man. Acta Diabetol Lat. 1978 May-Aug;15(3-4):192-7. doi: 10.1007/BF02581064.
• [37] Beta-adrenergic contribution to glucagon-induced glucose production and insulin secretion in uremia. Am J Physiol. 1986 Sep;251(3 Pt 1):E322-7. doi: 10.1152/ajpendo.1986.251.3.E322.
• [38] Effect of testosterone replacement on whole body glucose utilisation and other cardiovascular risk factors in males with idiopathic hypogonadotrophic hypogonadism. Horm Metab Res. 1998 Oct;30(10):642-5. doi: 10.1055/s-2007-978950.