It hasanxiolytic effects-like effects in rodents,[2] and enhancesdopamine signalling in thelimbic system,[3] as well as having complex effects on the dopamine release produced bycocaine, increasing it in some brain regions[4][5] but reducing it in others.[6][7] In animal studies, SB-242084 producedstimulant-type activity andreinforcing effects, somewhat similar to but much weaker than cocaine oramphetamines.[8][9] It isself-administered by monkeys.[9] It has been found to increase dopamine levels in thestriatum in rats and in thenucleus accumbens in monkeys by about 200%.[10]
SB-242084 was under development byGlaxoSmithKline for the treatment ofanxiety disorders in the late 1990s.[17] However, its development looks to have been abandoned.[17]
^Kennett GA, Wood MD, Bright F, Trail B, Riley G, Holland V, et al. (1997). "SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist".Neuropharmacology.36 (4–5):609–20.doi:10.1016/S0028-3908(97)00038-5.PMID9225286.S2CID23032157.
^Martin JR, Ballard TM, Higgins GA (April 2002). "Influence of the 5-HT2C receptor antagonist, SB-242084, in tests of anxiety".Pharmacology, Biochemistry, and Behavior.71 (4):615–625.doi:10.1016/S0091-3057(01)00713-4.PMID11888553.S2CID19142495.
^Di Matteo V, Di Giovanni G, Di Mascio M, Esposito E (August 1999). "SB 242084, a selective serotonin2C receptor antagonist, increases dopaminergic transmission in the mesolimbic system".Neuropharmacology.38 (8):1195–205.doi:10.1016/S0028-3908(99)00047-7.PMID10462132.S2CID39658512.
^Navailles S, Moison D, Ryczko D, Spampinato U (November 2006). "Region-dependent regulation of mesoaccumbens dopamine neurons in vivo by the constitutive activity of central serotonin2C receptors".Journal of Neurochemistry.99 (4):1311–9.doi:10.1111/j.1471-4159.2006.04188.x.PMID17018023.S2CID43833462.
^Banks ML, Bauer CT, Blough BE, Rothman RB, Partilla JS, Baumann MH, Negus SS (June 2014)."Abuse-related effects of dual dopamine/serotonin releasers with varying potency to release norepinephrine in male rats and rhesus monkeys".Exp Clin Psychopharmacol.22 (3):274–284.doi:10.1037/a0036595.PMC4067459.PMID24796848.A corollary of this proposition is that antagonists at 5-HT2C receptors may block endogenous serotonergic tone at these receptors and thereby disinhibit mesolimbic DA neurons. In support of this idea, 5-HT2C antagonists including SB 242,084 have been shown to increase firing rates of DA neurons and produce modest but significant (~200%) increases in DA levels in rat striatum and squirrel monkey nucleus accumbens (but not squirrel monkey caudate) (Alex et al. 2005; Di Giovanni et al. 1999; Manvich et al. 2012b).
^abBagdy G, Graf M, Anheuer ZE, Modos EA, Kantor S (December 2001). "Anxiety-like effects induced by acute fluoxetine, sertraline or m-CPP treatment are reversed by pretreatment with the 5-HT2C receptor antagonist SB-242084 but not the 5-HT1A receptor antagonist WAY-100635".Int J Neuropsychopharmacol.4 (4):399–408.doi:10.1017/S1461145701002632.PMID11806866.
^Dekeyne A, Denorme B, Monneyron S, Millan MJ (April 2000). "Citalopram reduces social interaction in rats by activation of serotonin (5-HT)(2C) receptors".Neuropharmacology.39 (6):1114–1117.doi:10.1016/s0028-3908(99)00268-3.PMID10727723.
^Yamauchi M, Tatebayashi T, Nagase K, Kojima M, Imanishi T (August 2004). "Chronic treatment with fluvoxamine desensitizes 5-HT2C receptor-mediated hypolocomotion in rats".Pharmacol Biochem Behav.78 (4):683–689.doi:10.1016/j.pbb.2004.05.003.PMID15301922.
^Shishkina GT, Iudina AM, Dygalo NN (2006). "[Effects of fluoxetine on locomotor activity: possible involvement of dopamine]".Zh Vyssh Nerv Deiat Im I P Pavlova (in Russian).56 (4):523–528.PMID17025197.
^ab"SB 242084".AdisInsight. 26 July 2002. Retrieved14 January 2025.
