TTD Target ID: TTDC00184

Target Information
Name	Beta-3 adrenergic receptor
Type of target	Clinical trial target
Synonyms	Beta-3 adrenoceptor
	Beta-3 adrenoreceptor
	Beta3-AR
	Beta3AR
Disease	Cardiac arrhythmias    [1]
	Erectile dysfunction    [2]
	Gain weight in patients with morbid obesity    [3]
	Hypertension    [4][1]
	Hypertonicity of bladder    [5]
	Noninsulin-dependent diabetes mellitus    [6][7]
	Obesity    [7][8][1]
	Overactive bladder disorder    [9]
Drug(s)	AZ-40140		Phase II	Obesity, Diabetes Type 2	[10]
	LY-362884		Phase II	Obesity, Diabetes Type 2	[10]
	N-5984		Phase II	Obesity, Diabetes Type 2	[10]
	Beta3-adrenoceptor agonist		Phase I	Eating disorder Obesity	[11]
	Amibegron		Discontined in Phase III	Major Depressive Disorders,Severe Mood Disorders	[12]
	GW-427353		Discontinued in Phase II	Irritable Bowel Syndrome (IBS), Obesity, Micturition disorder, Diabetes Type 2	[10]
	Amibegron		Preclinical	Major Depressive Disorders,Obesity, Diabetes Type 2	[12]
	CL-314698		Preclinical	Obesity, Diabetes Type 2	[10]
	CP-114271		Preclinical	Obesity	[10]
	GCR-1087		Preclinical	Obesity, Diabetes Type 2	[10]
	L-742791		Preclinical	Obesity	[10]
	L-751250		Preclinical	Obesity	[10]
BioChemical Class	G-protein coupled receptor (rhodopsin family)
Pathway	Calcium signaling pathway
	Neuroactive ligand-receptor interaction
UniProt ID	P13945
PDB Structure	2CDW.
Function	Beta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. Beta-3 is involved in the regulation of lipolysis and thermogenesis.
Sequence	MAPWPHENSSLAPWPDLPTLAPNTANTSGLPGVPWEAALAGALLALAVLATVGGNLLVIV AIAWTPRLQTMTNVFVTSLAAADLVMGLLVVPPAATLALTGHWPLGATGCELWTSVDVLC VTASIETLCALAVDRYLAVTNPLRYGALVTKRCARTAVVLVWVVSAAVSFAPIMSQWWRV GADAEAQRCHSNPRCCAFASNMPYVLLSSSVSFYLPLLVMLFVYARVFVVATRQLRLLRG ELGRFPPEESPPAPSRSLAPAPVGTCAPPEGVPACGRRPARLLPLREHRALCTLGLIMGT FTLCWLPFFLANVLRALGGPSLVPGPAFLALNWLGYANSAFNPLIYCRSPDFRSAFRRLL CRCGRRLPPEPCAAARPALFPSGVPAARSSPAQPRLCQRLDGASWGVS
Related US Patent	6,124,457
	6,232,337
	6,265,581
	6,291,491
	6,310,050
	6,395,762
	6,410,734
	6,413,991
	6,436,914
	6,444,685
	6,451,814
	6,458,817
	6,465,501
	6,498,170
	6,506,901
	6,509,358
	6,514,991
	6,525,202
	6,537,994
	6,566,377
	6,569,873
	6,583,140
	6,593,341
	6,596,734
	6,605,618
	6,649,603
	6,660,752
	6,689,800
	6,689,888
	6,706,743
Target Validation	Click to Find Target Validation Information.
QSAR Model	Click to Find Target QSAR Model.
Inhibitor	1- (1H-Indol-4-yloxy)-3-phenethylamino-propan-2-ol		[13]
	1- (2-allylphenoxy)-3-morpholinopropan-2-ol		[14]
	1- (2-isopropylphenoxy)-3-morpholinopropan-2-ol		[14]
	BMS-196085		[15]
	BRL-37344		[16]
	BUCINDOLOL		[17]
Agonist	AZ-40140		[10]
	Amibegron		[12]
	BRL 26830A		[18]
	BRL 37344		[19]
	Beta3-adrenoceptor agonist		[11]
	CGP 12177		[19]
	CL-314698		[10]
	CL-316,243		[7]
	CP-114271		[10]
	Carazolol		[1]
	FR149175		[20]
	GCR-1087		[10]
	GW-427353		[10]
	L-742791		[10]
	L-751250		[10]
	LY-362884		[10]
	N-5984		[10]
	SM 11044		[19]
	SWR-0342SA		[21]
	Trecadrine		[22]
	Trimetoquinol		[23]
	ZD2079		[24]
	ZD7114		[24]
Cross References	3D Structure Related Literature On-Line Medical Dictionary
Ref 1	Current therapeutic uses and potential of beta-adrenoceptor agonists and antagonists. Eur J Clin Pharmacol. 1998 Feb;53(6):389-404. To Reference
Ref 2	Involvement of beta 3-adrenergic receptor activation via cyclic GMP- but not NO-dependent mechanisms in human corpus cavernosum function. Proc Natl Acad Sci U S A. 2003 Apr 29;100(9):5531-6. Epub 2003 Apr 21. To Reference
Ref 3	Genetic variation in the beta 3-adrenergic receptor and an increased capacity to gain weight in patients with morbid obesity. N Engl J Med. 1995 Aug 10;333(6):352-4. To Reference
Ref 4	Association of Trp64Arg beta 3-adrenergic-receptor gene polymorphism with essential hypertension in the Sardinian population. J Hypertens. 1999 Jan;17(1):33-8. To Reference
Ref 5	Pathophysiology of the overactive bladder and its pharmacological treatment. Nippon Yakurigaku Zasshi. 2003 May;121(5):331-8. To Reference
Ref 6	Time of onset of non-insulin-dependent diabetes mellitus and genetic variation in the beta 3-adrenergic-receptor gene. N Engl J Med. 1995 Aug 10;333(6):343-7. To Reference
Ref 7	Beta 3-adrenoceptor agonists as anti-diabetic and anti-obesity drugs in humans. Curr Pharm Des. 2001 Sep;7(14):1433-49. To Reference
Ref 8	Desensitization of the beta-adrenergic response in human brown adipocytes. Endocrinology. 1998 Jun;139(6):2676-84. To Reference
Ref 9	Beta3-adrenoceptors in human detrusor muscle. Urology. 2002 May;59(5 Suppl 1):25-9. To Reference
Ref 10	Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. To Reference
Ref 11	Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36. To Reference
Ref 12	Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. To Reference
Ref 13	J Med Chem. 1986 Aug;29(8):1524-7.Synthesis and beta-adrenergic receptor blocking potency of 1-(substituted amino)-3-(4-indolyloxy)propan-2-ols. To Reference
Ref 14	Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404. Epub 2010 Apr 9.A vHTS approach for the identification of beta-adrenoceptor ligands. To Reference
Ref 15	Bioorg Med Chem Lett. 2007 Aug 1;17(15):4290-6. Epub 2007 May 16.Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations. To Reference
Ref 16	Bioorg. Med. Chem. Lett. 7(12):1583-1588 (1997) To Reference
Ref 17	J Med Chem. 1980 Mar;23(3):285-9.Antihypertensive indole derivatives of phenoxypropanolamines with beta-adrenergic receptor antagonist and vasodilating activity. To Reference
Ref 18	Anti-obesity and anti-diabetic actions of a beta 3-adrenoceptor agonist, BRL 26830A, in yellow KK mice. Endocrinol Jpn. 1991 Aug;38(4):397-403. To Reference
Ref 19	Effects of several putative beta 3-adrenoceptor agonists on lipolysis in human omental adipocytes. Int J Obes Relat Metab Disord. 1996 May;20(5):428-34. To Reference
Ref 20	FR149175, a beta 3-adrenoceptor-selective agonist, is a possible therapeutic agent for non-insulin-dependent diabetes mellitus. Jpn J Pharmacol. 1997 May;74(1):109-12. To Reference
Ref 21	Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21. To Reference
Ref 22	Potential anti-diabetic applications of a new molecule with affinity for beta 3-adrenoceptors. Life Sci. 1996;59(11):PL141-6. To Reference
Ref 23	Synthesis and human beta-adrenoceptor activity of 1-(3,5-diiodo-4- methoxybenzyl)-1,2,3,4-tetrahydroisoquinolin-6-ol derivatives in vitro. J Med Chem. 2000 Feb 24;43(4):591-8. To Reference
Ref 24	Urinary tract toxicity in rats following administration of beta 3-adrenoceptor agonists. Toxicol Pathol. 1999 Mar-Apr;27(2):165-70. To Reference

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Professor in Department of Pharmacy
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