SB-242,084

Drugbox
IUPAC_name = 6-Chloro-2,3-dihydro-5-methyl-N- [6- [(2-methyl-3-pyridinyl)oxy] -3-pyridinyl] -1H-indole-1-carboxyamide

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CAS_number= 181632-25-7
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PubChem= 3644637
DrugBank=
C=21 | H=19 | Cl=1 | N=4 | O=2
molecular_weight = 394.853 g/mol
smiles = Cc1cc2CCN(c2cc1Cl)C(=O)Nc(cc4)cnc4Oc3cccnc3C
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SB-242,084 is a drug which acts as a selective antagonist for the 5HT_2C receptor. [Kennett GA, Wood MD, Bright F, Trail B, Riley G, Holland V, Avenell KY, Stean T, Upton N, Bromidge S, Forbes IT, Brown AM, Middlemiss DN, Blackburn TP. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. "Neuropharmacology". 1997 Apr-May;36(4-5):609-20. PMID 9225286] It has anxiolytic effects, [Martin JR, Ballard TM, Higgins GA. Influence of the 5-HT2C receptor antagonist, SB-242084, in tests of anxiety. "Pharmacology, Biochemistry and Behaviour". 2002 Apr;71(4):615-25. PMID 11888553] and enhances dopamine signalling in the limbic system. [Di Matteo V, Di Giovanni G, Di Mascio M, Esposito E. SB 242084, a selective serotonin2C receptor antagonist, increases dopaminergic transmission in the mesolimbic system. "Neuropharmacology". 1999 Aug;38(8):1195-205. PMID 10462132] It has been shown to increase the effectiveness of SSRI antidepressants, and may also reduce their side effects. [Cremers TI, Giorgetti M, Bosker FJ, Hogg S, Arnt J, Mørk A, Honig G, Bøgesø KP, Westerink BH, den Boer H, Wikstrom HV, Tecott LH. Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade. "Neuropsychopharmacology". 2004 Oct;29(10):1782-9. PMID 15138437] [Burghardt NS, Bush DE, McEwen BS, LeDoux JE. Acute selective serotonin reuptake inhibitors increase conditioned fear expression: blockade with a 5-HT(2C) receptor antagonist. "Biological Psychiatry". 2007 Nov 15;62(10):1111-8. PMID 17524369]

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