Target Information
Target General Information | Top | |||||
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Target ID |
T31424
(Former ID: TTDS00031)
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Target Name |
Adrenergic receptor Alpha-2 (ADRA2)
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Synonyms |
Alpha-2 adrenergic receptor; Alpha(2)-adrenoceptor
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Gene Name |
NO-GeName
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 16 Target-related Diseases | + | ||||
1 | Attention deficit hyperactivity disorder [ICD-11: 6A05] | |||||
2 | Breathing abnormality [ICD-11: MD11] | |||||
3 | Cerebral ischaemia [ICD-11: 8B1Z] | |||||
4 | Dementia [ICD-11: 6D80-6D8Z] | |||||
5 | Essential hypertension [ICD-11: BA00] | |||||
6 | Eyelid inflammatory disorder [ICD-11: 9A02] | |||||
7 | Glaucoma [ICD-11: 9C61] | |||||
8 | Hypertension [ICD-11: BA00-BA04] | |||||
9 | Mood/affect symptom [ICD-11: MB24] | |||||
10 | Muscle disorder [ICD-11: FB32-FB3Z] | |||||
11 | Opioid use disorder [ICD-11: 6C43] | |||||
12 | Optic nerve disorder [ICD-11: 9C40] | |||||
13 | Pain [ICD-11: MG30-MG3Z] | |||||
14 | Sexual dysfunction [ICD-11: HA00-HA01] | |||||
15 | Skin sensation disturbance [ICD-11: ME65] | |||||
16 | Tonus and reflex abnormality [ICD-11: MB47] | |||||
BioChemical Class |
GPCR rhodopsin
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UniProt ID |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 15 Approved Drugs | + | ||||
1 | Apraclonidine | Drug Info | Approved | Intra ocular pressure reduction | [2], [3] | |
2 | Brimonidine | Drug Info | Approved | Ocular hypertension | [4], [5] | |
3 | Clonidine | Drug Info | Approved | Hypertension | [6], [7] | |
4 | Dexmedetomidine | Drug Info | Approved | Irritability | [3], [8] | |
5 | Guanabenz | Drug Info | Approved | High blood pressure | [9], [10] | |
6 | Guanfacine extended release | Drug Info | Approved | Attention deficit hyperactivity disorder | [11] | |
7 | Guanidine Hydrochloride | Drug Info | Approved | Muscle fatigue | [12] | |
8 | Lofexidine | Drug Info | Approved | Opioid dependence | [13] | |
9 | Meperidine | Drug Info | Approved | Pain | [12] | |
10 | Methyldopate Hydrochloride | Drug Info | Approved | Hypertension | [12] | |
11 | Nicergoline | Drug Info | Approved | Brain ischaemia | [12], [14] | |
12 | Oxymetazoline | Drug Info | Approved | Eye inflammation | [12] | |
13 | Sodium chloride | Drug Info | Approved | Skin burns | [12] | |
14 | Tizanidine | Drug Info | Approved | Spasm | [3], [15] | |
15 | Yohimbine | Drug Info | Approved | Erectile dysfunction | [16], [17] | |
Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
1 | Fadolmidine | Drug Info | Phase 2 | Neuropathic pain | [18] | |
2 | Fipamezole | Drug Info | Phase 2 | Acute myeloid leukaemia | [19] | |
Discontinued Drug(s) | [+] 3 Discontinued Drugs | + | ||||
1 | Mivazerol | Drug Info | Discontinued in Phase 3 | Angina pectoris | [20] | |
2 | Atipamezole | Drug Info | Discontinued in Phase 2 | Male sexual disorder | [21] | |
3 | ADX415 | Drug Info | Terminated | Hypertension | [22] | |
Mode of Action | [+] 3 Modes of Action | + | ||||
Agonist | [+] 14 Agonist drugs | + | ||||
1 | Apraclonidine | Drug Info | [23], [24] | |||
2 | Brimonidine | Drug Info | [25] | |||
3 | Clonidine | Drug Info | [26], [27], [28] | |||
4 | Dexmedetomidine | Drug Info | [29], [30] | |||
5 | Guanabenz | Drug Info | [31] | |||
6 | Guanfacine extended release | Drug Info | [11] | |||
7 | Lofexidine | Drug Info | [1], [33] | |||
8 | Meperidine | Drug Info | [34], [35] | |||
9 | Oxymetazoline | Drug Info | [39] | |||
10 | Sodium chloride | Drug Info | [26] | |||
11 | Tizanidine | Drug Info | [40] | |||
12 | Fadolmidine | Drug Info | [18] | |||
13 | Mivazerol | Drug Info | [30] | |||
14 | Brominide tartrate | Drug Info | [39], [45], [46] | |||
Modulator | [+] 2 Modulator drugs | + | ||||
1 | Guanidine Hydrochloride | Drug Info | [32] | |||
2 | Methyldopate Hydrochloride | Drug Info | [36] | |||
Antagonist | [+] 6 Antagonist drugs | + | ||||
1 | Nicergoline | Drug Info | [37], [38] | |||
2 | Yohimbine | Drug Info | [17], [41], [42] | |||
3 | Fipamezole | Drug Info | [43] | |||
4 | Atipamezole | Drug Info | [44] | |||
5 | ADX415 | Drug Info | [22] | |||
6 | [3H]rauwolscine | Drug Info | [47] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | Clinical 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 DrugAlcohol Abuse. 2008;34(5):611-6. | |||||
REF 2 | 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: 7117). | |||||
REF 3 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
REF 4 | 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). | |||||
REF 5 | ClinicalTrials.gov (NCT00675207) Comparison of Brimonidine Purite, Dorzolamide, and Brinzolamide as Adjunctive Therapy to Prostaglandin Analogs. U.S. National Institutes of Health. | |||||
REF 6 | 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: 516). | |||||
REF 7 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070315. | |||||
REF 8 | 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: 521). | |||||
REF 9 | 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: 5443). | |||||
REF 10 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074149. | |||||
REF 11 | Emerging drugs for attention-deficit/hyperactivity disorder. Expert Opin Emerg Drugs. 2007 Sep;12(3):423-34. | |||||
REF 12 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 13 | 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89. | |||||
REF 14 | Drug information of Nicergoline, 2008. eduDrugs. | |||||
REF 15 | 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: 7308). | |||||
REF 16 | 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: 102). | |||||
REF 17 | Interest of alpha2-adrenergic agonists and antagonists in clinical practice: background, facts and perspectives. Curr Top Med Chem. 2007;7(2):187-94. | |||||
REF 18 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 19 | ClinicalTrials.gov (NCT00559871) Safety and Efficacy Study of Fipamezole in Treatment of Motor Dysfunctions in Parkinson's Disease. U.S. National Institutes of Health. | |||||
REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002725) | |||||
REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000275) | |||||
REF 22 | Clinical pipeline report, company report or official report of Shionogi (2011). | |||||
REF 23 | Apraclonidine 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. | |||||
REF 24 | Topically 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. | |||||
REF 25 | Increased alpha2-adrenergic constriction of isolated arterioles in diffuse scleroderma. Arthritis Rheum. 2000 Aug;43(8):1886-90. | |||||
REF 26 | Noradrenergic 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. | |||||
REF 27 | The alpha2 -adrenergic receptors in hypertension and heart failure: experimental and clinical studies. J Hypertens. 2001 Dec;19(12):2115-24. | |||||
REF 28 | Effects 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. | |||||
REF 29 | Dexmedetomidine in intensive care unit: a study of hemodynamic changes. Middle East J Anesthesiol. 2002 Oct;16(6):587-95. | |||||
REF 30 | Alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role. Anaesthesia. 1999 Feb;54(2):146-65. | |||||
REF 31 | Centrally acting sympathetic inhibitors for therapy of patients with hypertension. Nippon Rinsho. 1997 Aug;55(8):2081-5. | |||||
REF 32 | Guanidine-based 2-adrenoceptor ligands: Towards selective antagonist activity.Eur J Med Chem.2014 Jul 23;82:242-54. | |||||
REF 33 | A 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. | |||||
REF 34 | Meperidine, remifentanil and tramadol but not sufentanil interact with alpha(2)-adrenoceptors in alpha(2A)-, alpha(2B)- and alpha(2C)-adrenoceptor ... Eur J Pharmacol. 2008 Mar 17;582(1-3):70-7. | |||||
REF 35 | Meperidine exerts agonist activity at the alpha(2B)-adrenoceptor subtype. Anesthesiology. 2002 Jun;96(6):1420-6. | |||||
REF 36 | Effect of Antihypertensive Therapy with Alpha Methyldopa on Levels of Angiogenic Factors in Pregnancies with Hypertensive Disorders | |||||
REF 37 | Effect 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. | |||||
REF 38 | Nicergoline 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. | |||||
REF 39 | Potent alpha(2A)-adrenoceptor-mediated vasoconstriction by brimonidine in porcine ciliary arteries. Invest Ophthalmol Vis Sci. 2001 Aug;42(9):2049-55. | |||||
REF 40 | Tizanidine. 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. | |||||
REF 41 | Acute neurotoxicity after yohimbine ingestion by a body builder. Clin Toxicol (Phila). 2009 Sep;47(8):827-9. | |||||
REF 42 | Alpha2-adrenergic receptors attenuate secretagogue-induced endocytosis and promote exocytosis of intestinal NHE2 and NHE3. J Pharmacol Exp Ther. 2009 Sep;330(3):818-25. | |||||
REF 43 | Emerging drugs for Parkinson's disease. Expert Opin Emerg Drugs. 2006 Sep;11(3):403-17. | |||||
REF 44 | Low 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. | |||||
REF 45 | Alpha(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. | |||||
REF 46 | Brimonidine. 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. | |||||
REF 47 | Characterization of alpha-adrenoceptor subtypes in smooth muscle of equine ileum. Am J Vet Res. 2001 Sep;62(9):1370-4. |
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