Journal ArticleDOI
Epibatidine: a novel (chloropyridyl)azabicycloheptane with potent analgesic activity from an ecuadoran poison frog
Thomas F. Spande,H. M. Garraffo,M. W. Edwards,Herman J. C. Yeh,Lewis K. Pannell,John W. Daly +5 more
Reads0
Chats0
TLDR
A potent non-opioid analgesic, epibatidine, has been isolated from skins of the Ecuadoran poison frog, Epipedobates tricolor, and its structure determined by MS, IR, and 1 H NMR analyses as exo-2-(6-chloro-3-pyridyl)-7-azabicyclo[2.2.1]heptane represents a unique new class of alkaloids.Abstract:
A potent non-opioid analgesic, epibatidine, has been isolated from skins of the Ecuadoran poison frog, Epipedobates tricolor, and its structure determined by MS, IR, and 1 H NMR analyses as exo-2-(6-chloro-3-pyridyl)-7-azabicyclo[2.2.1]heptane. It represents a unique new class of alkaloidsread more
Citations
More filters
Journal ArticleDOI
Synthesis and Structure−Activity Relationship Studies of 3,6-Diazabicyclo[3.2.0]heptanes as Novel α4β2 Nicotinic Acetylcholine Receptor Selective Agonists
Jianguo Ji,Michael R. Schrimpf,Kevin B. Sippy,William H. Bunnelle,Tao Li,David J. Anderson,Connie R. Faltynek,Carol S. Surowy,Tino Dyhring,Philip K. Ahring,Michael Meyer +10 more
TL;DR: A series of novel, potent neuronal nicotinic acetylcholine receptor (nAChR) ligands derived from 3,6-diazabicyclo[3.2.0]heptane have been synthesized and evaluated for binding affinity and agonist activity at the alpha4beta2 nA ChR subtype and led to the discovery of several compounds with interesting in vitro pharmacological profiles.
Journal ArticleDOI
Radiosynthesis and preliminary evaluation of 5-[123/125I]iodo-3-(2(S)-azetidinylmethoxy)pyridine: a radioligand for nicotinic acetylcholine receptors
Andrew G. Horti,Andrei O. Koren,Kan Sam Lee,Alexey G. Mukhin,D. Bruce Vaupel,Alane S. Kimes,Morgan Stratton,Edythe D. London +7 more
TL;DR: Preliminary in vivo assay and ex vivo autoradiography of mouse brain indicated that [125I]1 selectively labels nicotinic acetylcholine receptors (nAChRs) with very high affinity and specificity, and studies suggest that [123I] 1 may be useful as a radioligand for single photon emission computed tomography (SPECT) imaging of nA ChRs.
Journal ArticleDOI
Identification of nicotine biotransformation intermediates by Agrobacterium tumefaciens strain S33 suggests a novel nicotine degradation pathway
TL;DR: Results indicated that strain S33 can transform nicotine into renewable hydroxylated-pyridine intermediates by the special pathway, in which at least three intermediates, 6-hydroxy-L-nicotine, 7-Hydroxy-3-succinoylpyridine, and 2,5-dihydroxypyridine have potential to be further chemically modified into useful compounds.
Journal Article
The Effects of Morphine, Nicotine and Epibatidine on Lymphocyte Activity and Hypothalamic-Pituitary-Adrenal Axis Responses
Mellon Rd,Bayer Bm +1 more
TL;DR: It is suggested that, like morphine, nicotinic agonists decrease blood lymphocyte proliferation responses, apparently independent of elevated corticosterone, however, unlike morphine, Nicotinian agonists appear to act predominantly at peripheral receptors, suggesting that nicotinics receptors are downstream of opioid receptors in a centrally mediated opioid-induced immunomodulatory pathway.
Journal ArticleDOI
The quantification of biodiversity: an esoteric quest or a vital component of sustainable development?
TL;DR: Biodiversity relates through services, individual species indicating environmental change or stress, insights into the life sciences and increasingly today, through wealth generated from biodiversity at the level of the molecule.