Chemical Properties
Crystalline Solid
Uses
mydriatic and anticholinergie agent in ophthalmie preparations and pre-anesthetie medications; antidote to organophosphous
insecticides
Uses
Anticholinergic;Muscarinic antagonist
Uses
Atropine sulfate is mydriatic; antispasmodic; used in preanesthetic medication.
Application
Atropine sulfate monohydrate is an alkaloid derived from belladonna, a cholinergic receptor antagonist drug, which has been shown to be a competitive non-selective antagonist of central and peripheral mAChR M (muscarinic acetylcholine receptor). It can be used in the treatment of cardiac arrhythmias. Atropine Sulfate is also used as a pharmaceutical reference standard for a variety of analytical applications.
brand name
Atrophate [Veterinary]
(Schering-Plough Animal Health); Atropisol
(Ciba Vision, US Ophthalmics); Isopto Atropine (Alcon).
General Description
Atropine is isolated from
Atropa belladonna,
Datura stramonium and
Mandragora officinarum. It is a tertiary amine, which acts as a cholinergic receptor antagonist.
Biological Activity
atropine is a competitive antagonist of muscarinic acetylcholine receptor with ic50 values of 2.22±0.60nm, 4.32±1.63nm, 4.16±1.04nm, 2.38±1.07nm and 3.39±1.16nm for m1, m2, m3, m4 and m5, respectively [1].atropine is an antimuscarinic agent and has shown the pharmacological effects because of binding to muscarinic acetylcholine receptors. atropine, the orthosteric antagonist, has been reported to compete with [3h]-nms for all muscarinic subtypes with a potency consistent with the high affinities at the machr subtypes. the ki values are 1.27±0.36nm, 3.24±1.16nm, 2.21±0.53nm, 0.77±0.43nm and 2.84±0.84nm, respectively [1, 2, 3].
References
[1] lebois ep1, bridges tm, lewis lm, dawson es, kane as, xiang z, jadhav sb, yin h, kennedy jp, meiler j, niswender cm, jones ck, conn pj, weaver cd, lindsley cw. discovery and characterization of novel subtype-selective allosteric agonists for the investigation of m(1) receptor function in the central nervous system.acs chem neurosci. 2010;1(2):104-121.
[2] busch h, allen h, anderson dc.effects of atropine and carbachol on labeling of protein fractions of mouse pancreas in vitro.j pharmacol exp ther. 1959 nov; 127:200-4.
[3] feron o1, smith tw, michel t, kelly ra.dynamic targeting of the agonist-stimulated m2 muscarinic acetylcholine receptor to caveolae in cardiac myocytes. j biol chem. 1997 jul 11; 272(28):17744-8.
