TTD Target ID: TTDS00102

Target Information
Name	5-hydroxytryptamine 2 receptor
Type of target	Successful target
Synonyms	5-HT2 receptor
	5-HTB2
	Serotonin receptor 2
Disease	Acute respiratory distress syndrome    [1][2]
	Cocaine dependence    [3][4]
	Detrusor hyperreflexia    [5]
	Hypertension    [2][6][7]
	Skeletal muscle associated spasticity    [8]
	Urinary incontinence    [5]
Drug(s)	Cyclobenzaprine		Approved	Depression	[9]
	Ketanserin		Approved	Hypertension	[10]
	Mianserin		Approved	Depression	[11][12][13][3]
	Fluphenazine Decanoate		Phase II	Psoriasis	[14]
	E2101		Phase I	Cervical dystonia	[8]
BioChemical Class	G-protein coupled receptor (rhodopsin family)
Pathway	Calcium signaling pathway
	Gap junction
	Neuroactive ligand-receptor interaction
Related US Patent	6,469,011
	6,638,934
	6,664,286
Target Validation	Click to Find Target Validation Information.
Antagonist	Cyclobenzaprine		[9]
	E2101		[8]
	Fluphenazine Decanoate		[14]
	Ketanserin		[10]
	Metrenperone		[15][16][17][1]
	Mianserin		[11][12][13][3]
	Ritanserin		[18][19][20][6]
Binder	SB 206553 hydrochloride		[21]
Multitarget	Fluphenazine Decanoate		[14]
Cross References	3D Structure Related Literature On-Line Medical Dictionary
Ref 1	Efficiency of 5-hydroxytryptamine receptor blockade as therapeutic measure during acute respiratory distress syndrome in double-muscled cattle. Zentralbl Veterinarmed A. 1993 Apr;40(3):185-93. To Reference
Ref 2	The use of ketanserin, a 5-hydroxytryptamine receptor antagonist, for treatment of postoperative hypertension following coronary artery bypass surgery. Anesth Analg. 1983 Jan;62(1):63-9. To Reference
Ref 3	5-HT2 receptor antagonists given in the acute withdrawal from daily cocaine injections can reverse established sensitization. Eur J Pharmacol. 2002 Oct 25;453(2-3):255-63. To Reference
Ref 4	Antagonism of 5-hydroxytryptamine(2a) receptors attenuates the behavioral effects of cocaine in rats. J Pharmacol Exp Ther. 2001 Apr;297(1):357-63. To Reference
Ref 5	Influence of central serotonergic mechanisms on lower urinary tract function. Urology. 2002 May;59(5 Suppl 1):30-6. To Reference
Ref 6	Combined treatment of portal hypertension with ritanserin and propranolol in conscious and unrestrained cirrhotic rats. Hepatology. 1992 May;15(5):878-82. To Reference
Ref 7	5-Hydroxytryptamine receptor activity of the dopamine receptor agonist fenoldopam in canine tracheal smooth muscle. J Pharmacol Exp Ther. 1992 Feb;260(2):491-8. To Reference
Ref 8	In vitro interactions between a potential muscle relaxant E2101 and human cytochromes P450. Drug Metab Dispos. 2002 Jul;30(7):805-13. To Reference
Ref 9	Torticollis under Cyclobenzaprine. Pharmacology. 2009 Jul 8;84(2):91-92. [Epub ahead of print] To Reference
Ref 10	Nordexfenfluramine causes more severe pulmonary vasoconstriction than dexfenfluramine. Am J Physiol Lung Cell Mol Physiol. 2004 Mar;286(3):L531-8. Epub 2003 Nov 7. To Reference
Ref 11	5-HT reuptake and 5-HT2 receptors modulate capsaicin-evoked hypothermia in rats. Neurosci Lett. 2008 Jan 17;430(3):191-6. Epub 2007 Nov 5. To Reference
Ref 12	5-HT2 and 5-HT3 receptors in the lateral parabrachial nucleus mediate opposite effects on sodium intake. Neuroscience. 2007 Jun 8;146(4):1453-61. Epub 2007 Apr 16. To Reference
Ref 13	Lack of effect of some dopamine and non-dopamine receptor ligands on amphetamine-induced changes in the rat brain neuropeptide Y system. Pharmacol Rep. 2005 Nov-Dec;57(6):850-5. To Reference
Ref 14	Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63. To Reference
Ref 15	Cardiovascular response to intravenous administration of 5-hydroxytryptamine after type-2 receptor blockade, by metrenperone, in healthy calves. Vet J. 1999 Jan;157(1):31-7. To Reference
Ref 16	Pulmonary response to intravenous administration of 5-hydroxytryptamine after type-2 receptor blockade in healthy calves. Am J Vet Res. 1993 Jan;54(1):168-73. To Reference
Ref 17	Induction of serotonin-S2 receptor blockade during early or late stage of acute respiratory distress syndrome in double-muscled calves: a comparative study. Zentralbl Veterinarmed A. 1993 May;40(4):241-8. To Reference
Ref 18	Characterization of contractile 5-hydroxytryptamine receptor subtypes in the in situ autoperfused kidney in the anaesthetized rat. Eur J Pharmacol. 2008 Sep 11;592(1-3):133-7. Epub 2008 Jul 4. To Reference
Ref 19	Hypersensitivity of 5-HT2 receptors in OCD patients. An increased prolactin response after a challenge with meta-chlorophenylpiperazine and pre-treatment with ritanserin and placebo. J Psychiatr Res. 2008 Sep;42(11):894-901. Epub 2008 Jun 3. To Reference
Ref 20	Effects of antipsychotics and reference monoaminergic ligands on marble burying behavior in mice. Behav Pharmacol. 2008 Mar;19(2):145-52. To Reference
Ref 21	Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex. Neuropsychopharmacology. 2006 Feb;31(2):265-77. To Reference

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