Nicotinic acetylcholine receptor ligands, a patent review (2006 – 2011)
نویسندگان
چکیده
منابع مشابه
Progesterone modulates a neuronal nicotinic acetylcholine receptor.
The major brain nicotinic acetylcholine receptor is assembled from two subunits termed alpha 4 and n alpha 1. When expressed in Xenopus oocytes, these subunits reconstitute a functional acetylcholine receptor that is inhibited by progesterone levels similar to those found in serum. In this report, we show that the steroid interacts with a site located on the extracellular part of the protein, t...
متن کاملDiversity of insect nicotinic acetylcholine receptor subunits.
Nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels that mediate fast synaptic transmission in the insect nervous system and are targets of a major group of insecticides, the neonicotinoids. They consist of five subunits arranged around a central ion channeL Since the subunit composition determines the functional and pharmacological properties of the receptor the presence o...
متن کاملConformation of acetylcholine bound to the nicotinic acetylcholine receptor.
We report here the biologically active conformation of acetylcholine when bound to the high-affinity state of the receptor from Torpedo californica. The acetylcholine conformation was determined in the free and bound states by proton NMR two-dimensional nuclear Overhauser effects. In agreement with x-ray crystallographic data, acetylcholine in solution has an extended conformation with an avera...
متن کاملDesensitization of Mouse Nicotinic Acetylcholine Receptor Channels
The rate constants of acetylcholine receptor channels (AChR) desensitization and recovery were estimated from the durations and frequencies of clusters of single-channel currents. Diliganded-open AChR desensitize much faster than either unliganded- or diliganded-closed AChR, which indicates that the desensitization rate constant depends on the status of the activation gate rather than the occup...
متن کاملEmbedded cholesterol in the nicotinic acetylcholine receptor.
The nicotinic acetylcholine receptor (nAChR) is a cation-selective channel central to both neuronal and muscular processes and is considered the prototype for ligand-gated ion channels, motivating a structural determination effort that spanned several decades [Unwin N (2005) Refined structure of the nicotinic acetylcholine receptor at 4 A resolution. J Mol Biol 346:967-989]. Purified nAChR must...
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ژورنال
عنوان ژورنال: Expert Opinion on Therapeutic Patents
سال: 2011
ISSN: 1354-3776,1744-7674
DOI: 10.1517/13543776.2011.637919