Muscarinic blocking drugs are compounds that selectively antagonize the responses to acetylcholine (ACh) and other parasympathomimetics that are mediated by activation of muscarinic receptors. These agents are also referred to as muscarinic antagonists, antimuscarinic drugs, and anticholinergics. The belladonna alkaloids, such as atropine, are the oldest known muscarinic blocking compounds, and...

The crystal structures of acetylthiolcholine bromide and propionylthiolcholine iodide were elucidated. Acetylthiolcholine was found to be essentially isosteric with acetylselenolcholine, while the conformation of these compounds was quite different from that of acetylcholine. The importance of conformation and electron distribution in the biological actions of choline esters is discussed.

Earlier work by the author and coworkers (Adams & Whittaker, 1948; Adams, 1949; Whittaker, 1949; Mounter & Whittaker, 1950; Mounter, 1951) has shown that the so-called 'true' or 'specific' cholinesterases of erythrocytes, brain and cobra venom, previously believed to act only on acetylcholine and a few other esters, are in reality capable of hydrolysing a wide range of non-choline esters, 3:3-d...

THE importance of the physiologically active substance acetylcholine makes it highly desirable that the properties of the enzyme which specifically hydrolyses choline esters be established. Summaries of the past work on this enzyme have recently appeared [Ammon, 1935; Gaddum, 1935; Oppenheimer, 1935]. It is remarkable that although choline esterase has been studied in relation to its partial pu...

In this manuscript we report an integrated study to develop simple choline esters as cholinergic agents potentially useful against the Alzheimer disease. In previously reported experiments we demonstrated the capability of the pivaloylcholine to exert cholinergic effects into the Central Nervous System, so we decided to explore small variants of choline esters. The knowledge of crystallographic...

187 Abstract Underactive bladder (UAB) or detrusor underactivity (DU) is a common yet still poorly understood urological problem. In addition to true detrusor failure and neuropathy, the inhibitory effects of detrusor contraction by the striated urethral sphincter and the bladder neck through alpha-adrenergic activity may also play a role in the development of UAB or DU. Treatment of UAB or DU ...

Underactive bladder (UAB) or detrusor underactivity (DU) is a common yet still poorly understood urological problem. In addition to true detrusor failure and neuropathy, the inhibitory effects of detrusor contraction by the striated urethral sphincter and the bladder neck through alpha-adrenergic activity may also play a role in the development of UAB or DU. Treatment of UAB or DU aims to reduc...

As an extension of previous investigations (1, 2) concerning the specificity of cholinesterase, the present study deals with the effect upon enzymatic hydrolysis of variations in the chain length of the acid component of choline esters. It is known from earlier work (3, 1) that increasing the normal chain length from 2 to 4 carbon atoms results in increased cnzymatic and decreased alkaline spli...