geoscience.net logo
+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

Structure-activity studies on 2-methyl-3- -pyrrolidinylmethoxypyridine


, : Structure-activity studies on 2-methyl-3- -pyrrolidinylmethoxypyridine. Journal of Medicinal Chemistry 40(3): 385-390

2-Methyl-3-(2(S)-pyrrolidinylmethoxy)pyridine, ABT-089 (S-4), a member of the 3-pyridyl ether class of nicotinic acetylcholine receptor (nAChR) ligands, shows positive effects in rodent and primate models of cognitive enhancement and a rodent model of anxiolytic activity and possesses a reduced propensity to activate peripheral ganglionic type receptors. The profiles of S-4, its N-methyl analogue, and the corresponding enantiomers across several measures of cholinergic channel function in vitro and in vivo are presented, together with in vitro metabolism and in vivo bioavailability data. On the basis of its biological activities and favorable oral bioavailability, S-4 is an attractive candidate for further evaluation as a treatment for cognitive disorders.

US$29.90


Other references

Sobiesiak-Mirska, J.; Nałecz, K.A., 2002: Palmitoylcarnitine modulates interaction protein kinase C delta-GAP-43. Palmitoylcarnitine, reported previously to promote neuronal differentiation, was observed to affect distribution of protein kinase C (PKC) isoforms in neuroblastoma NB-2a cells, leading to retardation in cytoplasm of high molecular weight species...

Hu, B.; Meng, M.; Wang, Z.; Du, W.; Fossey, J.S.; Hu, X.; Deng, W-Ping., 2011: A highly selective ferrocene-based planar chiral PIP (Fc-PIP) acyl transfer catalyst for the kinetic resolution of alcohols. Novel planar chiral ferrocene nucleophilic catalysts (Fc-PIP) containing both central and planar chiral elements were designed and synthesized for catalytic enantioselective acyl transfer of secondary alcohols. A remarkably efficient catalyst with...

Jastrzebska, I.; Siergiejczyk, L.; Tomkiel, A.M.; Urbańczyk-Lipkowska, Z.; Wójcik, D.; Morzycki, J.W., 2009: On reactions of steroidal 23-oxo and 23,24-epoxysapogenins with Lewis acids. The reaction of 23-oxotigogenin acetate with TMSOTf in THF afforded the corresponding bisnorcholanic lactone in 60% yield. The analogous reactions carried out in dichloromethane or benzene gave the rearranged products—the isomeric spirostani...

Leopardi, G.; Serafini, G.; Simoncelli, C.; Ludovini, V.; Pistola, L.; Altissimi, G., 2002: Ki67 and p53 in laryngeal epithelial lesions: correlations with risk factors. Laryngeal carcinoma-the prototype of epithelial tumors in the head and neck region-has been the greatest source of information on the biological behavior of such neoplasms. Many Authors have suggested that smoke, and to a lesser extent alcohol, pl...

Sierra-Honigmann, M.R.; Murphy, P.A., 1992: Suppression of interleukin-1 action by phospholipase-A2 inhibitors in helper T lymphocytes. The mechanism by which interleukin 1 (IL-1) and T cell receptor (TCR) activation co-stimulate T helper (Th) cells is not clear. In chondrocytes, fibroblasts and several other cell types, much of the evidence suggests a linkage between IL-1 action...

Lestienne, R., 2000: Intrinsic and extrinsic neuronal mechanisms in temporal coding: a further look at neuronal oscillations. Many studies in recent years have been devoted to the detection of fast oscillations in the Central Nervous System (CNS), interpreting them as synchronizing devices. We should, however, refrain from associating too closely the two concepts of sync...

Cox Stephen F.; Munroe Stuart M., 2000: Fluid-driven faulting processes in intrusive-related hydrothermal system, Porgera, Papua New Guinea. Abstracts - Geological Society of Australia 59: 104

Szymanowska, I., 1979: Nursing department. Pielegniarka i Polozna: 14-15

Arnold, W.J.J., 1914: The Etiology of Beri-Beri. In considering the aetiology of beri-beri the author contradicts the theory that the disease is due to the eating of decorticated rice. From his own observations and from those recorded by others he has been long impressed with the probably infect...

Ivanov, P.; Piskov, A., 1979: The chemical heterogeneity of the sunflower variety Peredovik. Fatty acid composition of the oil in seeds from 147 inflorescences in 1974 and protein content in seeds from 131 inflorescences in 1974 and 73 inflorescences in 1975 were analysed. The content of individual fatty acids varied widely, linoleic acid...