In Search of Potent 5‐HT6 Receptor Inverse Agonists | Zendy

Hostetler Greg | Zendy; Dunn Derek | Zendy; McKenna Beth Ann | Zendy; Kopec Karla | Zendy; Chatterjee Sankar | Zendy

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In Search of Potent 5‐HT6 Receptor Inverse Agonists

Author(s) -

Hostetler Greg,

Dunn Derek,

McKenna Beth Ann,

Kopec Karla,

Chatterjee Sankar

Publication year - 2014

Publication title -

chemical biology and drug design

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.59

H-Index - 77

eISSN - 1747-0285

pISSN - 1747-0277

DOI - 10.1111/cbdd.12279

Subject(s) - inverse agonist , enantiomer , chemistry , potency , stereochemistry , pharmacology , chirality (physics) , sulfonamide , selectivity , receptor , in vitro , agonist , biochemistry , medicine , nambu–jona lasinio model , chiral symmetry breaking , physics , quantum mechanics , quark , catalysis

A series of non‐sulfonamide/non‐sulfone derived potent 5‐HT 6 receptor inverse agonists has been disclosed. Representative compound 9 ( K i = 14 n m ) displayed selectivity against a set of family members as well as brain permeability 6 h post‐oral administration. In addition, the separated enantiomers of compound 9 displayed difference in activity indicating the influence of chirality on potency.

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