N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.

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Tsai Y, Dukat M, Slassi A, MacLean N, Demchyshyn L, Savage JE, Roth BL, Hufesein S, Lee M, Glennon RA

N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.

Bioorg Med Chem Lett. 2000 Oct 16;10(20):2295-9.

PubMed ID

11055342 [ View in PubMed

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Abstract

N-Benzenesulfonyl-5-methoxy-N,N-dimethyltryptamine (BS/5-OMe DMT; 5) was shown to bind at human 5-HT6 serotonin receptors with high affinity (Ki = 2.3 nM) relative to serotonin (Ki = 78 nM). Structural variation failed to result in significantly enhanced affinity. BS/5-OMe DMT acts as an antagonist of 5-HT-stimulated adenylate cyclase (pA2 = 8.88 nM) and may represent the first member of a novel class of 5-HT6 antagonists.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clozapine	5-hydroxytryptamine receptor 6	Ki (nM)	4.8	N/A	N/A	Details