Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00031

Target Information
NameAlpha-2 adrenergic receptor    
Type of targetSuccessful target    
SynonymsAlpha(2)-adrenoceptor    
DiseaseAlzheimer's disease
[ICD9: 331.0   ICD10: G30]
[1]
Analgesics
[ICD9: 338   ICD10: R52]
[2]
Diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[3]
Erectile dysfunction
[ICD9: 302.72, 607.84   ICD10: F52.2, N48.4]
[4]
Gastrointestinal disturbances[5]
Heart failure
[ICD9: 428   ICD10: I50]
[6]
Hypertension
[ICD9: 401   ICD10: I10, I11, I12, I13, I15]
[7][6]
Ischemic heart disease
[ICD9: 410-414   ICD10: I20-I25]
[6]
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]
[2]
Nasal congestion
[ICD9: 478.19   ICD10: J34.89]
[8]
Open-angle glaucoma
[ICD9: 365   ICD10: H40-H42]
[9]
Peri-operative ischemia
[ICD9: 459.89   ICD10: I99.8]
[10]
Prefrontal cognitive deficits[11]
Spasticity associated with cerebral or spinal damage[12]
Systemic sclerosis
[ICD9: 710.1   ICD10: M34]
[13]
Tachycardia, unspecified
[ICD9: 427, 785.0   ICD10: I47-I49, R00.0]
[7]
Vasospastic attacks associated with idiopathic Raynaud's disease
[ICD9: 443.0   ICD10: I73.0]
[14]
Drug(s)ApraclonidineApprovedAdditional Intra Ocular Pressure (IOP) reduction[15][16]
ClonidineApprovedHypertension[11][6][2]
DexamfetamineApprovedAttention-deficit hyperactivity disorder[17]
DexmedetomidineApprovedSedation[7][10]
Ergoloid mesylateApprovedAlzheimer's Disease[18]
GuanabenzApprovedHigh blood pressure[19]
GuanfacineApprovedHypertension[20]
Guanfacine extended releaseApprovedAttention-defi cit/hyperactivity disorder[21]
LofexidineApprovedHeroin and opiate withdrawal[22][23]
MeperidineApprovedAnesthetic[24][25]
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
6,391,878
6,426,350
6,436,978
6,486,202
6,495,555
6,544,927
6,576,640
Target ValidationClick to Find Target Validation Information.    
AgonistApraclonidine[15][16]
BHT-920[8]
Brominide tartrate[34][28][9]
Clonidine[11][6][2]
Dexamfetamine[17]
Dexmedetomidine[7][10]
Guanabenz[19]
Guanfacine[20]
Guanfacine extended release[21]
Lofexidine[22][23]
Meperidine[24][25]
Mivazerol[10]
Oxymetazoline[28]
Saline[11]
Tizanidine[12]
UK 14,304[13]
AntagonistADX415[32]
Atipamezole[35]
Ergoloid mesylate[18]
Fipamezole[36]
Idazoxan[33]
Nicergoline[26][27]
Rauwolscine[5]
Yohimbine[29][30][31]
MultitargetDexamfetamine[17]
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



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543