SB-242084

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SB-242084 is a selective antagonist of the serotonin 5-HT2C receptor which is used in scientific research.[1]

It has anxiolytic effects-like effects in rodents,[2] and enhances dopamine signalling in the limbic system,[3] as well as having complex effects on the dopamine release produced by cocaine, increasing it in some brain regions[4][5] but reducing it in others.[6][7] In animal studies, SB-242084 produced stimulant-type activity and reinforcing effects, somewhat similar to but much weaker than cocaine or amphetamines.[8][9] It is self-administered by monkeys.[9] It has been found to increase dopamine levels in the striatum in rats and in the nucleus accumbens in monkeys by about 200%.[10]

The drug has been shown to increase the effectiveness of the selective serotonin reuptake inhibitor (SSRI) class of antidepressants in animals, and may also reduce their side effects.[11][12] SSRIs acutely reduce social interaction in rodents, thought to be an anxiogenic response, and this effect can be reversed by SB-242084.[13][14] In addition, SSRIs have been found to acutely induce hypolocomotion, which can be reversed by SB-242084.[13][15][16]

SB-242084 was under development by GlaxoSmithKline for the treatment of anxiety disorders in the late 1990s.[17] However, its development looks to have been abandoned.[17]

See also

References

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