| Title : Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release - Crooks_2004_Bioorg.Med.Chem.Lett_14_1869 |
| Author(s) : Crooks PA , Ayers JT , Xu R , Sumithran SP , Grinevich VP , Wilkins LH , Deaciuc AG , Allen DD , Dwoskin LP |
| Ref : Bioorganic & Medicinal Chemistry Lett , 14 :1869 , 2004 |
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Abstract :
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. |
| PubMedSearch : Crooks_2004_Bioorg.Med.Chem.Lett_14_1869 |
| PubMedID: 15050618 |
Crooks PA, Ayers JT, Xu R, Sumithran SP, Grinevich VP, Wilkins LH, Deaciuc AG, Allen DD, Dwoskin LP (2004)
Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release
Bioorganic & Medicinal Chemistry Lett
14 :1869
Crooks PA, Ayers JT, Xu R, Sumithran SP, Grinevich VP, Wilkins LH, Deaciuc AG, Allen DD, Dwoskin LP (2004)
Bioorganic & Medicinal Chemistry Lett
14 :1869