@article{7288357596d04eb4b33f0f06cfb4fc2b,
title = "Synthesis of poison-frog alkaloids 233A, 235U, and 251AA and their inhibitory effects on neuronal nicotinic acetylcholine receptors",
abstract = "We previously reported that the synthetic quinolizidine 1-epi-207I is a relatively selective blocker of α7 nicotinic acetylcholine receptors. We now synthesized the analogous poison frog alkaloids 233A, 235U, and 251AA, and investigated the biological activities at two major types of neuronal nicotinic receptors. Electrophysiological study showed that the alkaloid 233A blocked α7 and α4β2 currents with similar potencies. Alkaloids 235U and 251AA also showed similar potencies for blockade of α7 and α4β2 currents. Thus, based on these studies, it would appear that C4 substituents greater in length than the allyl of 1-epi-207I reduce α7-potency without affecting α4β2-potency.",
keywords = "1-epi-207I, 233A, 235U, 251AA, Neuronal nicotinic acetylcholine receptors, Poison-frog alkaloids",
author = "Naoki Toyooka and Soushi Kobayashi and Dejun Zhou and Hiroshi Tsuneki and Tsutomu Wada and Hideki Sakai and Hideo Nemoto and Toshiyasu Sasaoka and Garraffo, {H. Martin} and Spande, {Thomas F.} and Daly, {John W.}",
note = "Funding Information: We are grateful to Dr. Jerry A. Stitzel (University of Colorado) for providing us with plasmid DNA. We also thank Dr. John A. Dani (Baylor College of Medicine, Houston, TX) for support on electrophysiological data acquisition. This work was supported in part by a Grant-in-Aid for Scientific Research from the Japan Society for the Promotion of Science (to N.T. and H.T.). Work at NIH was supported by intramural funds of NIDDK.",
year = "2007",
month = nov,
day = "1",
doi = "10.1016/j.bmcl.2007.08.045",
language = "英語",
volume = "17",
pages = "5872--5875",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Ltd.",
number = "21",
}