1-Methylmedmain, also known as 1,2-dimethyl-3-ethyl-5-dimethylaminoindole, is a serotonin receptor modulator and indole derivative related to the neurotransmitter serotonin. It is the 1-methyl derivative of medmain. The drug has low-potency serotonin antagonist or partial agonist activity, with low affinity for serotonin 5-HT1 and 5-HT2 receptors ( = >1,000nM) but greater activity against the serotonin receptors in the rat stomach fundus strip (KB = 48nM) (thought to represent the serotonin 5-HT2B receptor). It has similar potency as medmain, but lacks medmain's convulsant activity. 1-Methylmedmain was described and studied by E. Shaw and Dilworth Woolley in the 1950s. Other analogues of medmain have also been explored, but none had improved activity at the rat fundus strip serotonin 5-HT2B receptor compared to medmain and 1-methylmedmain.
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