Positive Allosteric Modulator of the Human 5-HT2C Receptor

Positive Allosteric Modulator of the Human 5-HT2C Receptor

The human 5-hydroxytryptamine-2C (5-HT2C) receptor has been the target of potential anxiolytics and antiobesity drugs, and its positive allosteric modulator was discovered to be L-threo-α-D-galacto-octopyranoside, methyl-7-chloro-6,7,8-trideoxy-6-[[(4-undecyl-2-piperidinyl)carbonyl]amino]-1-thiomono...

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Veröffentlicht in:Molecular pharmacology 2003-07, Vol.64 (1), p.78-84
Hauptverfasser: Im, Wha Bin, Chio, Christopher L, Alberts, Glen L, Dinh, Dac M
Format: Artikel
Sprache:eng
Schlagworte:
Allosteric Regulation
Animals
Cells, Cultured
Galactosides - pharmacology
Humans
Piperidines - pharmacology
Receptor, Serotonin, 5-HT2C
Receptors, Serotonin - drug effects
Receptors, Serotonin - metabolism
Serotonin Agents - pharmacology
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Beschreibung
Zusammenfassung:The human 5-hydroxytryptamine-2C (5-HT2C) receptor has been the target of potential anxiolytics and antiobesity drugs, and its positive allosteric modulator was discovered to be L-threo-α-D-galacto-octopyranoside, methyl-7-chloro-6,7,8-trideoxy-6-[[(4-undecyl-2-piperidinyl)carbonyl]amino]-1-thiomonohydrochloride (2S-cis) (PNU-69176E). The drug at low micromolar concentrations (
ISSN:0026-895X
1521-0111
DOI:10.1124/mol.64.1.78