1-Methylmedmain

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.^{[1] [2] [3]} It is the 1-methyl derivative of medmain.^{[1] [2] [3]} The drug has low-potency serotonin antagonist or partial agonist activity, with low affinity for serotonin 5-HT₁ and 5-HT₂ receptors (IC₅₀ Tooltip half-maximal inhibitory concentration =>1,000nM) but greater activity against the serotonin receptors in the rat stomach fundus strip (K_B = 48nM) (thought to represent the serotonin 5-HT_2B receptor).^{[3] [4] [1]} It has similar potency as medmain, but lacks medmain's convulsant activity.^{[2] [3]} 1-Methylmedmain was described and studied by E. Shaw and Dilworth Woolley in the 1950s.^{[3] [1] [2]} Other analogues of medmain have also been explored, but none had improved activity at the rat fundus strip serotonin 5-HT_2B receptor compared to medmain and 1-methylmedmain.^{[3] [4]}