1.
J Med Chem
; 42(10): 1684-6, 1999 May 20.
Article
in English
| MEDLINE
| ID: mdl-10346920
Subject(s)
Neurons/metabolism , Nicotinic Agonists/chemical synthesis , Nootropic Agents/chemical synthesis , Phenols/chemical synthesis , Pyrrolidines/chemical synthesis , Receptors, Nicotinic/metabolism , Animals , Binding, Competitive , Cell Line , Cerebral Cortex/metabolism , Humans , In Vitro Techniques , Nicotinic Agonists/metabolism , Nicotinic Agonists/pharmacology , Nootropic Agents/metabolism , Nootropic Agents/pharmacology , Oocytes , Patch-Clamp Techniques , Phenols/metabolism , Phenols/pharmacology , Pyrrolidines/metabolism , Pyrrolidines/pharmacology , Rats , Rats, Sprague-Dawley , Transfection , Xenopus
2.
Bioorg Med Chem Lett
; 8(16): 2173-8, 1998 Aug 18.
Article
in English
| MEDLINE
| ID: mdl-9873508
ABSTRACT
A series of conformationally restricted analogues of nicotine has been synthesized and evaluated as agonists of neuronal acetylcholine receptors. Compound 2 (SIB-1663), which selectively activated human recombinant alpha 2 beta 4 and alpha 4 beta 4 nAChRs, was shown to be active in animal models of Parkinson's disease and pain.