195819-22-8Relevant academic research and scientific papers
LIGANDS FOR NICOTINIC ACETYLCHOLINE RECEPTORS, AND METHODS OF MAKING AND USING THEM
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Page 72-73, (2010/02/10)
One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor. The present invention also relates to the use of a compound of the invention for treating a mammal suffering from Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism or trichtillomania.
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues
Wei, Zhi-Liang,Petukhov, Pavel A.,Xiao, Yingxian,Tückmantel, Werner,George, Clifford,Kellar, Kenneth J.,Kozikowski, Alan P.
, p. 921 - 924 (2007/10/03)
Conformationally constrained epibatidine analogues 20a,b and 23a,b were synthesized using a radical cyclization as the key step. Radioligand displacement assays to six defined rat nicotinic acetylcholine receptor (nAChR) subtypes showed that 20a,b bind with moderate affinities, while 23a,b have low affinities. 20a exhibits higher affinity for the β2 containing subtype than for the β4 containing counterpart, while 20b possesses reversed selectivity. Modeling studies suggest that the spatial distribution of the ligand's atoms around the pharmacophore elements may control their nAChR subtype selectivity.
Electrophilic aromatic substitution on pyridine rings. Intramolecular cyclization using N-acyliminium ions
Brodney, Michael A.,Padwa, Albert
, p. 6153 - 6156 (2007/10/03)
The reaction of N-acyliminium ions with several activated pyridines resulted in an intramolecular cyclization to provide novel heterocycles. The reaction exhibited a regiochemical preference for cyclization para to the electron donating substitutent.
