Nicotine structure-activity relationship

Thus, cholinergic receptor classification can be considered in terms of three stages of development. Initially, Dale [2] distinguished nicotinic and muscarinic receptor subtypes with crude alkaloids. Then, chemical synthesis and structure-activity relationships clearly revealed that nicotinic and muscarinic receptors were heterogeneous, but chemical selectivity could not come close to uncovering the true diversity of receptor subtypes. Lastly, analysis of subtypes came from molecular cloning, making possible the classification of receptors on the basis of primary structure (Fig. 11-2). 

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Swanson, K.L., Aronstam, R.S., Wotmacott, S., Rapoport, H., and Albuquerque, E.X. 1991. Nicotinic pharmacology of anatoxin analogues. 1. side-chain structure-activity-relationships at peripheral agonist and noncompetitive antagonist sites. 

Nicolotti, O., Pellegrini-Calace, M., Altomare, C., Carotti, A., Carrieri, A., and Sanz, F. 2002. Ligands of neuronal nicotinic acetylcholine receptor (nAChR) Inferences from the Hansch and 3-D quantitative structure-activity relationship... 

Holladay, M. W., Lebold, S. A., Lin, N. H. Structure-activity relationships of nicotinic acetylcholine receptor agonists as potential treatments for dementia. Drug. Dev. Res. 1995(35), 191-213. 

Caldwell, W.S., Benchenif, M., Bhatti, B.S., Deo, N.M., Dobson, G.P., Dull, G.M., Lipiello, P.M., Lovette, M.E., Miller, C.H., Ravard, A., Schmitt, J.D., Crooks, P.A., 1997. Synthesis and structure-activity relationships of analogs of RJR-2403, a CNS-selective nicotinic agonist. Abstracts of International Business Communications Symposium on Nicotinic Acetylcholine Receptors as Pharmaceutical Targets, Washington, DC, July 24-25. 

D. J., Campbell, J.E., Kuntzweiler, T.A., Donnelly-Roberts, D.L., Piattoni-Kaplan, M Briggs, C.A., Williams, M., Arneric, S.P., 1998. Identification and structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors. J. Med. Chem. 41, 407-412. 

Rahnasto, M., Raunio, H., Poso, A., Wittekindt, C., Juvonen, R.O. Quantitative structure-activity relationship analysis of inhibitors of the nicotine metabolizing CYP2A6 enzyme, J. Med. Chem. 2005,48,440-9. 

Wishka, D. G., Walker, D. R, Yates, K. M. et al. Discovery of N-[(3/ )-l-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the al nicotinic acetylchohne receptor, for the potential treatment of cognitive deficits in schizophrenia synthesis and structure-activity relationship. J. Med. Chem. 2006,49, 4425 1436. 

Wonnacott S, Jackman S, Swanson KL, Rapoport H, Albuquerque EX (1991) Nicotinic pharmacology of anatoxin analogs, n. Side chain structure-activity relationships at neuronal nicotinic ligand binding sites. J Pharmacol Exp Ther 259 387-391... 

T0nder JE, Olesen PH (2001) Agonists at the a4P2 nicotinic acetylcholine receptors structure-activity relationships and molecular modelling. Curr Med Chem 8 651-674... 

Structure activity relationship In terms of spasmolytic activity of Kavaln (15) and other active constituents of P. methystiowrfi was reported. They all Inhibited or abolished contractions of Isolated guinea pig Ileum induced by acetylcholine, histamine, 5-HT or nicotine and were halt as active as papavarlne sulfate. Reduction of the styryl double bond In Kavaln reduced whereas unsaturation In the pyrone ring and eubstltution by methylenedloxy>... 

Matsuo H, Tomizawa M, Yamamoto 1 (1998) Structure-activity relationships of acychc nicotinoids and neonicotinoids for insect nicotinic acetylcholine receptor/ion channel complex. Arch Insect Biochem Physiol 37 17-23... 

R 442 F. Mesnard and R.G. Ratcliffe, NMR Analysis of Plant Nitrogen Metabolism , Photosynth.Res., 2005,83,163 R 443 E.L. Millard, N.L. Daly and DJ. Craik, Structure-Activity Relationships of a-Conotoxins Targeting Neuronal Nicotinic Acetylcholine Receptors , Eur.J.Biochem., 2004,271,2320 R 444 K. Moebius, A. Savitsky, A. Schnegg, M. Plato and M. Fuchs, High-Field EPR Spectroscopy Applied to Biological Systems Characterization of Molecular Switches for Electron and Ion Transfer , Phys.Chem.Chem.Phys., 2005,7,19... 

Synthesis and structure activity relationship (SAR) studies of [3,6-diazabicyclo[3.2.0]-heptan-3-yl]pyridin-2-yl -indoles as novel and potent o7 neuronal nicotinic receptors (NNRs) agonists with cognition-enhancing properties... 

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