Nicotinic agonists, antagonists, and modulators from natural sources

JW Daly - Cellular and molecular neurobiology, 2005 - Springer
Acetylcholine receptors were initially defined as nicotinic or muscarinic, based on selective
activation by two natural products, nicotine and muscarine. Several further nicotinic agonists …

Cholinergic nicotinic receptors: competitive ligands, allosteric modulators, and their potential applications.

MN Romanelli, F Gualtieri - Medicinal research reviews, 2003 - europepmc.org
Discovery of the important role played by nicotinic acetylcholine receptors (nAChRs) in
several CNS disorders has called attention to these membrane proteins and to ligands able …

Iridium-catalyzed asymmetric hydrogenation of 2-pyridyl cyclic imines: a highly enantioselective approach to nicotine derivatives

C Guo, DW Sun, S Yang, SJ Mao, XH Xu… - Journal of the …, 2015 - ACS Publications
A highly efficient asymmetric hydrogenation of cyclic imines containing a pyridyl moiety was
established by using iridium catalysts with chiral spiro phosphine-oxazoline ligands. This …

Design of ligands for the nicotinic acetylcholine receptors: the quest for selectivity

WH Bunnelle, M MJ Dart… - Current Topics in …, 2004 - ingentaconnect.com
In the last decade, nicotinic acetylcholine receptors (nAChRs) have emerged as important
targets for drug discovery. The therapeutic potential of nicotinic agonists depends …

Agonists at the a4b2 Nicotinic Acetylcholine Receptors Relationships and Molecular Modelling

JE Tonder, PH Olesen - Current medicinal chemistry, 2001 - ingentaconnect.com
Agonists of the a4b2 nicotinic acetylcholine receptors have been synthesised as potential
drugs for treatment of a variety of diseases. In this review, the published nicotinic agonists …

Halogenated cytisine derivatives as agonists at human neuronal nicotinic acetylcholine receptor subtypes

YE Slater, LM Houlihan, PD Maskell, R Exley… - …, 2003 - Elsevier
Cytisine (cy) is a potent and competitive partial agonist at α4 subunit-containing nicotinic
acetylcholine (nACh) receptors while at homomeric α7-nACh receptors it behaves as a full …

Site of protonation of nicotine and nornicotine in the gas phase: pyridine or pyrrolidine nitrogen?

J Graton, M Berthelot, JF Gal, S Girard… - Journal of the …, 2002 - ACS Publications
The gas-phase basicities (GBs) of nornicotine, nicotine, and model pyrrolidines have been
measured by FT-ICR. These experimental GBs are compared with those calculated (for the …

Central nicotinic receptor ligands and pharmacophores

RA Glennon, M Dukat - Pharmacochemistry Library, 2000 - Elsevier
Multiple populations of pentameric nicotinic acetylcholinergic (nACh) receptors exist and
several may be classified as central or neuronal. Neuronal nACh receptors, however, are …

Activity of cytisine and its brominated isosteres on recombinant human α7, α4β2 and α4β4 nicotinic acetylcholine receptors

LM Houlihan, Y Slater, DL Guerra… - Journal of …, 2001 - Wiley Online Library
Effects of cytisine (cy), 3‐bromocytisine (3‐Br‐cy), 5‐bromocytisine (5‐Br‐cy) and 3, 5‐
dibromocytisine (3, 5‐diBr‐cy) on human (h) α7‐, α4β2‐and α4β4 nicotinic acetylcholine …

Structure−Activity Studies and Analgesic Efficacy of N-(3-Pyridinyl)-Bridged Bicyclic Diamines, Exceptionally Potent Agonists at Nicotinic Acetylcholine Receptors

WH Bunnelle, JF Daanen, KB Ryther… - Journal of medicinal …, 2007 - ACS Publications
A series of exceptionally potent agonists at neuronal nicotinic acetylcholine receptors
(nAChRs) has been investigated. Several N-(3-pyridinyl) derivatives of bridged bicyclic …