TY - JOUR
T1 - Pyrrolidine analogues of lobelane
T2 - Relationship of affinity for the dihydrotetrabenazine binding site with function of the vesicular monoamine transporter 2 (VMAT2)
AU - Vartak, Ashish P.
AU - Nickell, Justin R.
AU - Chagkutip, Jaturaporn
AU - Dwoskin, Linda P.
AU - Crooks, Peter A.
PY - 2009/12/10
Y1 - 2009/12/10
N2 - Ring size reduction of the central piperidine ring of lobelane yielded pyrrolidine analogues that showed marked inconsistencies in their ability to bind to the dihydrotetrabenazine (DTBZ) binding site on the vesicular monoamine transporter-2 (VMAT2) and their ability to inhibit VMAT2 function. The structure-activity relationships indicate that structuralmodification within thepyrrolidine series resulted in analogues that interactwith two different sites, i.e., the DTBZ binding site and an alternative site on VMAT2 to inhibit transporter function.
AB - Ring size reduction of the central piperidine ring of lobelane yielded pyrrolidine analogues that showed marked inconsistencies in their ability to bind to the dihydrotetrabenazine (DTBZ) binding site on the vesicular monoamine transporter-2 (VMAT2) and their ability to inhibit VMAT2 function. The structure-activity relationships indicate that structuralmodification within thepyrrolidine series resulted in analogues that interactwith two different sites, i.e., the DTBZ binding site and an alternative site on VMAT2 to inhibit transporter function.
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U2 - 10.1021/jm900770h
DO - 10.1021/jm900770h
M3 - Article
C2 - 19691331
AN - SCOPUS:72249105289
SN - 0022-2623
VL - 52
SP - 7878
EP - 7882
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 23
ER -