McN-5292 is a stimulant drug which acts as a triple reuptake inhibitor, producing potent inhibition of the reuptake of all three monoamines, but around 10x selectivity for noradrenaline reuptake compared to dopamine and serotonin.[1][2]
Compound 22b in the table had Ki(nM): DA=1.7, NE=0.16, SER=1.5.
In terms of the SAR, it would be useful to compare for RTI-31 or RTI-113 for example.
See also
References
- ↑ "Prevention of the nigrostriatal toxicity of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine by inhibitors of 3,4-dihydroxyphenylethylamine transport". Journal of Neurochemistry 47 (4): 1073–1079. October 1986. doi:10.1111/j.1471-4159.1986.tb00722.x. PMID 3489072.
- ↑ "Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships". Journal of Medicinal Chemistry 30 (8): 1433–1454. August 1987. doi:10.1021/jm00391a028. PMID 3039136.
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 | Original source: https://en.wikipedia.org/wiki/McN-5292. Read more |
