TY - JOUR
T1 - Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release
AU - Crooks, Peter A.
AU - Ayers, Joshua T.
AU - Xu, Rui
AU - Sumithran, Sangeetha P.
AU - Grinevich, Vladimir P.
AU - Wilkins, Lincoln H.
AU - Deaciuc, A. Gabriela
AU - Allen, David D.
AU - Dwoskin, Linda P.
PY - 2004/4/19
Y1 - 2004/4/19
N2 - N-n-Alkylation of nicotine converts it from an agonist into an antagonist at neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogues exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter.
AB - N-n-Alkylation of nicotine converts it from an agonist into an antagonist at neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogues exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter.
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U2 - 10.1016/j.bmcl.2003.10.074
DO - 10.1016/j.bmcl.2003.10.074
M3 - Article
C2 - 15050618
AN - SCOPUS:1642603823
SN - 0960-894X
VL - 14
SP - 1869
EP - 1874
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 8
ER -