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Results for “CHOLINE/related compounds”

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At least 19 recordsLinked to original sources
PubMed1957

Some actions of substituted choline phenyl ethers, particularly of choline 2:6-xylyl ether.

Marked nicotine-like stimulant properties are possessed by choline phenyl ether and choline o-tolyl ether, and to a decreasing extent by choline 2:6-xylyl ether and choline 2:4:6-mesityl ether. The compounds all show neuromuscular blocking properties, which are of short duration and pass from mainly decamethonium-like to mainly curare-like as more methyl groups are added to the phenyl nucleus. This series of compounds also possesses muscarinic, weak anti-adrenaline and vasodilator properties, as well as long-lasting local anaesthetic effects in the two compounds tested by intradermal injection.

Choline↗
PubMed1962

Effect of sympathomimetic amines on the blocking action of guanethidine, bretylium and xylocholine.

Experiments were carried out in which the adrenergic neurone blocking activity of xylocholine, bretylium and guanethidine was studied by the use of the inhibitory responses of the isolated rabbit ileum to lumbar sympathetic nerve stimulation, and the contractions of the nictitating membrane of the anaesthetized cat in response to stimulation of the cervical sympathetic nerves. In both these preparations, after blockade of the effects of sympathetic nerve stimulation had been produced with xylocholine, bretylium or guanethicdine, the sympathomimetic amines, dexamphetamine, mephentermine, hydroxyamphetamine, ephedrine and phenethylamine, reversed the blockade; if these amines were given first, then the adrenergic neurone blocking agents were ineffective. Tyramine and dopamine were effective on the isolated rabbit ileum but not on the cat's nictitating membrane. Effective antagonism of the adrenergic neurone blocking drugs was also shown by some substances which inhibit mono-amine oxidase but only those which in addition possess sympathomimetic effects. Thus phenelzine, pheniprazine and tranylcypromine were effective whereas iproniazid and nialamide were not. Since xylocholine, bretylium and guanethidine were all antagonized by the same agents, it seems likely that they all produce sympathetic blockade by a similar mechanism. The possibility is discussed that the sympathomimetic amines which antagonize the adrenergic neurone blocking drugs are competing with these substances for the same receptor sites.

Amidines↗
PubMed1962

Triethylcholine compared with other substances affecting neuromuscular transmission.

Triethylcholine (triethyl-2-hydroxyethyl ammonium) has been compared, in its actions on neuromuscular transmission, with the motor end-plate blocking drugs tubocurarine and decamethonium, with the anticholinesterase neostigmine, and with the closely related drug tetraethylammonium. The experiments were carried out on conscious rabbits and mice, on the tibialis anterior muscle of cats under chloralose anaesthesia and on the isolated phrenic nerve-diaphragm preparation of the rat. Anticholinesterase activity was determined manometrically using the Warburg apparatus. Triethylcholine possessed a slight curare-like action, but this effect was shown to be too weak and transient to contribute to the slowly developing and long-lasting transmission failure which occurs selectively in frequently excited nervemuscle preparations and in exercised conscious animals. It was confirmed that the site of the blocking action of triethylcholine was pre-junctional. Triethylcholine often produced a slight potentiation of the contractions before blocking them. This effect was not due to a depolarizing or an anticholinesterase action, and it was concluded that the slight initial facilitating action of triethylcholine on neuromuscular transmission was due to an increase in the quantity of acetylcholine released by the nerve impulse. Tetraethylammonium was much more powerful than triethylcholine in this respect. The pre-junctional transmission failure produced by triethylcholine could not be explained simply on the basis that an initial excessive release led to exhaustion of transmitter.

Acetylcholine↗
PubMed1958

The pharmacological actions of some murexine-like substances.

Four choline esters of imidazole acids, two imidazole ethers of choline and thirteen ringsubstituted murexine-like compounds were compared with murexine for their muscle-paralysing and their nicotine-like effects. Dihydromurexine appeared, in animal experiments, to be the most potent derivative, but it was shown to be less effective than murexine in man. Among the other compounds, imidazolebutyrylcholine and imidazolepropoxycholine appeared to be worthy of particular consideration. The relation between the chemical structure of the murexine-like substances studied and their pharmacological effects is discussed.

Anesthetics, General↗
PubMed1957

Some aspects of the pharmacology of an homologous series of choline esters of fatty acids.

The pharmacological effects of a series of fatty acid-choline esters have been studied on the isolated rabbit heart, the isolated guinea-pig ileum and the rat stomach. The effect changed with increasing chain length, and three different types of response were observed. The shortchain compounds produced depression of the isolated rabbit heart and spasm of the isolated guinea-pig ileum. Only one, butyrylcholine, had an erratic stimulating effect on hydrochloric acid secretion by the partially vagotomized rat stomach. Medium-chain compounds had a stimulating effect on the isolated rabbit heart, a mixed spasmogenic and relaxant effect on the isolated guinea-pig ileum, and no effect on the rat stomach. Long-chain compounds blocked the effect of acetylcholine on the isolated rabbit heart and the isolated guinea-pig ileum; they also depressed spontaneous hydrochloric acid secretion by the rat stomach. The nature of these three types of response is discussed.

Acetylcholine↗
PubMed1957

The enzymatic hydrolysis of imidazoleacryloylcholine (murexine) and imidazolepropionylcholine (dihydromurexine) by various cholinesterases.

Several choline esters, including the imidazoleacryloyl and imidazolepropionyl compounds, have been hydrolysed by cholinesterases from various sources. The imidazolepropionyl ester was metabolized by cholinesterases obtained from human plasma, ox spleen, ox serum, and guinea-pig liver, but not by rat liver or bovine red cell cholinesterase. It is suggested the imidazolepropionylcholine or a closely related ester might be the natural substrate for "non-specific" cholinesterase.

Acetylcholinesterase↗