Therapeutic Targets Database
BIDD Pharmainformatics Databases


TTD Target ID: TTDS00031

Target Information
NameAlpha-2 adrenergic receptor    
Type of targetSuccessful target    
DiseaseAlzheimer's disease
[ICD9: 331.0   ICD10: G30]
[ICD9: 338   ICD10: R52]
Diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
Erectile dysfunction
[ICD9: 302.72, 607.84   ICD10: F52.2, N48.4]
Gastrointestinal disturbances[5]
Heart failure
[ICD9: 428   ICD10: I50]
[ICD9: 401   ICD10: I10, I11, I12, I13, I15]
Ischemic heart disease
[ICD9: 410-414   ICD10: I20-I25]
Mechanical allodynia associated with neuropathic pain of spinal origin
[ICD9: 204.0, 338, 356.0, 356.8,780   ICD10: C91.0, G64, G90.0, R52, G89]
Nasal congestion
[ICD9: 478.19   ICD10: J34.89]
Open-angle glaucoma
[ICD9: 365   ICD10: H40-H42]
Peri-operative ischemia
[ICD9: 459.89   ICD10: I99.8]
Prefrontal cognitive deficits[11]
Spasticity associated with cerebral or spinal damage[12]
Systemic sclerosis
[ICD9: 710.1   ICD10: M34]
Tachycardia, unspecified
[ICD9: 427, 785.0   ICD10: I47-I49, R00.0]
Vasospastic attacks associated with idiopathic Raynaud's disease
[ICD9: 443.0   ICD10: I73.0]
Drug(s)ApraclonidineApprovedAdditional Intra Ocular Pressure (IOP) reduction[15][16]
DexamfetamineApprovedAttention-deficit hyperactivity disorder[17]
Ergoloid mesylateApprovedAlzheimer's Disease[18]
GuanabenzApprovedHigh blood pressure[19]
Guanfacine extended releaseApprovedAttention-defi cit/hyperactivity disorder[21]
LofexidineApprovedHeroin and opiate withdrawal[22][23]
NicergolineApprovedSenile dementia[26][27]
OxymetazolineApprovedNasal congestion[28]
TizanidineApprovedSpasms, Pain[12]
YohimbineApprovedMale impotence[29][30][31]
ADX415Phase IIHypertension[32]
IdazoxanWithdrawn in Phase IIIMajor Depressive Disorder, Parkinsoní»s Disease[33]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
Related US Patent6,306,877
Target ValidationClick to Find Target Validation Information.    
Brominide tartrate[34][28][9]
Guanfacine extended release[21]
UK 14,304[13]
Ergoloid mesylate[18]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Protective effects of the alpha 2-adrenoceptor antagonist, dexefaroxan, against degeneration of the basalocortical cholinergic system induced by cortical devascularization in the adult rat. Neuroscience. 2002;115(1):41-53. To Reference
Ref 2Effects of intrathecal vs. systemic clonidine in treating chronic allodynia-like response in spinally injured rats. Brain Res. 1996 Oct 14;736(1-2):28-34. To Reference
Ref 3Investigation of alpha 2-adrenoceptors in humans. Am J Med. 1989 Sep 18;87(3C):6S-9S. To Reference
Ref 4Oral alpha adrenoceptor blockade as a treatment of erectile dysfunction. World J Urol. 2001 Feb;19(1):9-13. To Reference
Ref 5Characterization of alpha-adrenoceptor subtypes in smooth muscle of equine ileum. Am J Vet Res. 2001 Sep;62(9):1370-4. To Reference
Ref 6The alpha2 -adrenergic receptors in hypertension and heart failure: experimental and clinical studies. J Hypertens. 2001 Dec;19(12):2115-24. To Reference
Ref 7Dexmedetomidine in intensive care unit: a study of hemodynamic changes. Middle East J Anesthesiol. 2002 Oct;16(6):587-95. To Reference
Ref 8Intranasal application of the alpha2-adrenoceptor agonist BHT-920 produces decongestion in the cat. Am J Rhinol. 2001 Nov-Dec;15(6):407-15. To Reference
Ref 9Brimonidine. A review of its pharmacological properties and clinical potential in the management of open-angle glaucoma and ocular hypertension. Drugs Aging. 1998 Mar;12(3):225-41. To Reference
Ref 10alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role. Anaesthesia. 1999 Feb;54(2):146-65. To Reference
Ref 11Noradrenergic alpha-2 receptor agonists reverse working memory deficits induced by the anxiogenic drug, FG7142, in rats. Pharmacol Biochem Behav. 2000 Nov;67(3):397-403. To Reference
Ref 12Tizanidine. A review of its pharmacology, clinical efficacy and tolerability in the management of spasticity associated with cerebral and spinal disorders. Drugs. 1997 Mar;53(3):435-52. To Reference
Ref 13Increased alpha2-adrenergic constriction of isolated arterioles in diffuse scleroderma. Arthritis Rheum. 2000 Aug;43(8):1886-90. To Reference
Ref 14Blockade of vasospastic attacks by alpha 2-adrenergic but not alpha 1-adrenergic antagonists in idiopathic Raynaud's disease. Circulation. 1995 Sep 15;92(6):1448-51. To Reference
Ref 15Apraclonidine attenuates the increases in spinal excitatory amino acid release in rats with adjuvant-induced inflammation. Anesth Analg. 2002 Mar;94(3):701-5; table of contents. To Reference
Ref 16Topically applied clonidine protects the rat retina from ischaemia/reperfusion by stimulating alpha(2)-adrenoceptors and not by an action on imidazoline receptors. Brain Res. 2001 Jun 15;904(1):126-36. To Reference
Ref 17Attention-deficit hyperactivity disorder: treatment discontinuation in adolescents and young adults. Br J Psychiatry. 2009 Mar;194(3):273-7. To Reference
Ref 18Hydergine: interaction with the neurotransmitter systems in the central nervous system. J Pharmacol. 1985;16 Suppl 3:1-17. To Reference
Ref 19Centrally acting sympathetic inhibitors for therapy of patients with hypertension. Nippon Rinsho. 1997 Aug;55(8):2081-5. To Reference
Ref 20Guanfacine in children with autism and/or intellectual disabilities. J Dev Behav Pediatr. 2008 Aug;29(4):303-8. To Reference
Ref 21Emerging drugs for attention-deficit/hyperactivity disorder. Expert Opin Emerg Drugs. 2007 Sep;12(3):423-34. To Reference
Ref 22Clinical pharmacokinetics of lofexidine, the alpha 2-adrenergic receptor agonist, in opiate addicts plasma using a highly sensitive liquid chromatography tandem mass spectrometric analysis. Am J Drug Alcohol Abuse. 2008;34(5):611-6. To Reference
Ref 23A Phase 3 placebo-controlled, double-blind, multi-site trial of the alpha-2-adrenergic agonist, lofexidine, for opioid withdrawal. Drug Alcohol Depend. 2008 Sep 1;97(1-2):158-68. Epub 2008 May 27. To Reference
Ref 24Meperidine, remifentanil and tramadol but not sufentanil interact with alpha(2)-adrenoceptors in alpha(2A)-, alpha(2B)- and alpha(2C)-adrenoceptor knock out mice brain. Eur J Pharmacol. 2008 Mar 17;582(1-3):70-7. Epub 2007 Dec 27. To Reference
Ref 25Meperidine exerts agonist activity at the alpha(2B)-adrenoceptor subtype. Anesthesiology. 2002 Jun;96(6):1420-6. To Reference
Ref 26Effect of non-selective alpha-adrenergic receptor antagonist nicergoline on the activity of neurons in the ventral lateral thalamic nucleus. Fiziol Zh. 2005;51(4):29-35. To Reference
Ref 27Nicergoline in senile dementia of Alzheimer type and multi-infarct dementia: a double-blind, placebo-controlled, clinical and EEG/ERP mapping study. Psychopharmacology (Berl). 1995 Feb;117(4):385-95. To Reference
Ref 28Potent alpha(2A)-adrenoceptor-mediated vasoconstriction by brimonidine in porcine ciliary arteries. Invest Ophthalmol Vis Sci. 2001 Aug;42(9):2049-55. To Reference
Ref 29Acute neurotoxicity after yohimbine ingestion by a body builder. Clin Toxicol (Phila). 2009 Jul 30. [Epub ahead of print] To Reference
Ref 30Alpha2-adrenergic receptors attenuate secretagogue-induced endocytosis and promote exocytosis of intestinal NHE2 and NHE3. J Pharmacol Exp Ther. 2009 Jun 25. [Epub ahead of print] To Reference
Ref 31Interest of alpha2-adrenergic agonists and antagonists in clinical practice: background, facts and perspectives. Curr Top Med Chem. 2007;7(2):187-94. To Reference
Ref 322011 Pipeline of Shionogi. To Reference
Ref 33Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42. To Reference
Ref 34alpha(2A)-adrenoceptor: G(alphai1) protein-mediated pertussis toxin-resistant attenuation of G(s) coupling to the cyclic AMP pathway. Biochem Pharmacol. 2000 Jun 15;59(12):1531-8. To Reference
Ref 35Low doses of alpha 2-adrenoceptor antagonists augment spinal morphine analgesia and inhibit development of acute and chronic tolerance. Br J Pharmacol. 2008 Dec;155(8):1264-78. Epub 2008 Sep 22. To Reference
Ref 36Emerging drugs for Parkinson's disease. Expert Opin Emerg Drugs. 2006 Sep;11(3):403-17. To Reference


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