Synthesis and binding of 3-aminopyridine derivatives at central nicotinic receptors.
A series of secondary and tertiary pyridyl amides as potential central nicotinic acetylcholine receptors (nAChRs) ligands were prepared. Amides displayed negligible or very low affinity, whereas two amines achieved by reduction of corresponding secondary amides, showed affinity in the nanomolar range for nAChRs.
Dipartimento di Tossicologia dell'Università di Cagliari, Italy.
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G
Balboni
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M
Marastoni
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S
Merighi
P A
PA
Borea
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R
Tomatis
D000631:Aminopyridines / Q000138:chemical synthesis* / Q000378:metabolism*; D000818:Animals; D002490:Central Nervous System / Q000187:drug effects / Q000378:metabolism*; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D066298:In Vitro Techniques; D008297:Male; D009538:Nicotine / Q000378:metabolism; D018722:Nicotinic Agonists / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D011978:Receptors, Nicotinic / Q000187:drug effects / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000631:Aminopyridines; D018722:Nicotinic Agonists; D011978:Receptors, Nicotinic; D009538:Nicotine