Carbamylcholine

1 mM Carbamylcholine added after two hours of incubation had no effect on the secretion of Clara cell secretory protein by lung explants (Hook et al. 1990). 

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Important derivatives of choline are acetylcholine, acetyl-P-methylcholine, and carbamylcholine. Many other choline derivatives have been synthesized and studied, but have not been found satisfactory for clinical use. 

Carbamylcholine chloride [51 -83-2] is also called carbachol (47). Its principal use is as a parasympathornimetic in veterinary practice for large animals. 

Carbamylcholine Synthetic carbamate analogue of ACh Muscarinic > nicotinic... 

Figure 2. Potency of anatoxin-a analogs to induce contracture in frog rectus abdominis muscle. The data from two experiments are combined in this figure. In one, anatoxinmethylester was found to be equipo-tent with carbamylcholine. In the other, the anatoxin isomers were assayed against ACh [after cholinesterse inhibition by diisopropylfluoro-phosphate (DFP) followed by washing of the preparation] (19). Maximal contracture was measured by depolarization with KCl at the end of each experiment.

Potential oscillation was measured in the presence of cholinergic agents (acetylcholine chloride, carbamylcholine chloride, carbamyl- d-methylcholine chloride, and acetyl-/6-methylcholine chloride) and anticholinergic agents (tetramethylammonium chloride, tetra-ethylammonium chloride, succinylcholine chloride, hexamethonium chloride, scopolamine hydrobromide, atropine sulfate, homatropine hydrochloride, and tubocurarine chloride)... 

FIG. 18 Chemical structures of (a) acetylcholine chloride, (b) carbamylcholine chloride, (c) carba-myl-y8-methylcholine chloride, (d) acetyl-/i-methylcholine chloride, (e) tetramethylammonium chloride, (f) tetraethylamonium chloride, (g) succinylcholine chloride, (h) hexamethonium chloride, (i) scopolamine hydrobromide, 0 atropine sulfate, (k) homatropine hydrochloride, and (1) tubocurar-ine chloride. 

FIGURE 1.9 Records of the minute electrical currents (downward deflections) that flow through single ligandgated ion channels in the junctional region of frog skeletal muscle. The currents arise from brief transitions of individual nicotinic receptors to an active (channel open) state in response to the presence of various agonists (ACh = acetylcholine SubCh = suberyldicholine DecCh = the dicholine ester of decan-1,10-dicarboxylic acid CCh = carbamylcholine). (From Colquhoun, D. and Sakmann, B., J. Physiol., 369,501-557, 1985. With permission.)... 

I/R, inward rectification O/R, outward rectification CPA, cyclopiazonic acid TG, thapsigargin CCh, carbamylcholine CIF, Ca2+ influx factor CAM-ant., calmodulin antagonist W/C, whole-cell recording C/A, cell-attached recording P-W/C, perforated whole-cell recording. 

Buisson B, Bertrand D (2001) Chronic exposure to nicotine upregulates the human alpha4beta2 nicotinic acetylcholine receptor function. J Neurosci 21 1819-1829 CeUe PH, van Rossum-Fikkert SE, van Dijk WJ, Brejc K, Smit AB, Sixma TK (2004) Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures. Neuron 41 907-914... 

Wagley48 found that V produced a dose-related decrease in the endplate potential of the curarized iliofibularis muscle of the frog at 1-3 x 10 2 m. A similar effect of 2-PAM I was found at 1-3 x 10-3 M, whereas concentrations below 10 3 M produced dose-related increases in the endplate potential. Fleisher et al.47 found that III, unlike I, had no excitatory action on the Isolated frog rectus abdominis, but had a more potent effect than I in inhibiting the response of that muscle to decamethonlum, carbamylcholine, and acetylcholine. 

The finding by Fleisher et al. 7 that 2-PAM I facilitated response by skeletal muscle to acetylcholine and depressed responses to decamethonium and carbamylcholine, whereas III had only the depressant actions, suggests that 2-PAM has an activity that is not duplicated in III. The nature of this difference is not entirely clear. 

Celie PH et al Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures. Neuron 2004 41 907. [PMID 15046723]... 

Besides this remarkably fast commercial development, other research groups designed their own laboratory-compatible LAPS systems for similar purposes. The use of, e.g., a nicotinic acetylcholine receptor was reported to create a LAPS-receptor biosensor capable of detecting receptor ligands (acetylcholine, carbamylcholine, succinylcholine, sub-eryldicholine, nicotine as well as d-tubocurarine, a-bungarotoxin and a-Naja toxin) [85]. Another system quite similar to the Cytosensor setup was introduced, where mouse fibroblast fine 3T6 cells were chosen to demonstrate the determination of metabolic processes of these cells [86]. 

Carbamylcholine (= Carbachol)] (tertiary amine) Synthetic nACh-R agonist (non-specific, resistant to AChE)... 

Eldefrawi and Eldefrawi [98] reported the purification of the acetylcholine of Torpedo electroplax on an affinity column consisting of cobra (Naja naja siamensis) toxin coupled to Sepharose 4B. Desorption with 10 mM benzoquinonium produced a protein that bound [ I]a-bungarotoxin but not [ H]acetyl-choline. However, desorption with 1 mM carbamylcholine gave a receptor protein that bound pH]acetylcholine decamethonium, [ H]nicotine [ C]dimethyl-(-l-)-tubocuranrine, and [ I]a bungarotoxin. Schmidt and Raftery [99] also purified acetylcholine receptor, from Narcine, on a N-(e-aminohexanoyl)-3-aminopropyltrimethyl-ammonium bromide-HBr-agarose column. 

Figure 7.7. Calibration curves of relative fluorescence response against log concentration for three analytes at the fiber/AcChR/FITC-BTX sensor (a) BTX (b) tubocurarine and (c) carbamylcholine. [Reprinted, with permission, from K. R. Rogers, J. J. Valdes, and M. E. Eldefrawi, Analytical Biochemistry 182, 1989, 353-359. Acetylcholine Receptor Fiber-Optic Evanescent Fluorosensor . Copyright 1989 by Academic Press, Inc.]...

Nicotinic noncompetitive carbamylcholine-induced NaCl influx 0.02 0.007tc 125... 

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