[Effect of alcohols on synaptic stimulation transmission in the isolated sympathetic ganglion of the frog].
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Biomedical subjects
Publications and source records attributed to E Minker.
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Phenlaxine and bisacodyl were shown to inhibit gastric emptying and motility by activating a reflex arising from the small intestine. This effect produced by the cathartics could not be prevented either by alpha or beta sympatholytic, or by parasympatholytic agents; further it was antagonized by quinine and quinidine, as well as by chloroquine and mepacrine in doses found to suppress gastric motility in untreated animals. The inhibition of gastric motility through cathartics does not appear to be due to an effect on adrenergic or cholinergic pathways but rather to involve a purinergic mechanism.
In an isolated spiral muscle preparation from the common bile duct of the dog and rabbit contraction was elicited by PGF2 alpha, in a concentration dependent manner. The contraction was long-lasting and reversible. As opposed to PGF2 alpha, morphine, noradrenaline and barium chloride did not induce a contractile response.
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Chloroquine and mepacrine appear in the stomach wall and inhibit gastric emptying in the rat after oral or parenteral administration. Measuring their concentration in the stomach wall, it was found that it depended upon on the route of application. A smaller proportion of a given dose accumulated in the stomach wall when chloroquine and mepacrine were introduced by avoiding the stomach. The side effect of the two drugs, the inhibition of gastric motility, could be minimized by not only parenteral but also duodenal administration; the latter could be realized by enteric-coated tablets.
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When tested on the isolated sympathetic ganglion of the rat and frog, beta adrenergic blocking agents were found to inhibit synaptic transmission. This effect can be attributed, in some cases, to the aspecific membrane-stabilizing effect of the drugs, and in other instances to a specific ganglionic blocking property of the agents tested. Beta blockers proved to be more potent ganglioplegics than hexamethonium, their effect was in turn surpassed by pempidine and d-tubocurarine. In some cases the duration of the transmission block induced by beta blockers was longer than that of the reference compounds. On basis of the obtained results, it might not be excluded that the antihypertensive effect of beta adrenergic blocking agents involves a ganglionic component.
The effect of various prostaglandin (PG) synthetase inhibitors such as indomethacin, diclofenac, fenoprofen, niflumic acid and sulindac was studied on the isolated sympathetic ganglion of Rana esculenta. It was found that all the tested drugs inhibited synaptic transmission, an effect related to the inhibition of PG synthetase. It has been suggested that PGF2a might be involved in the modulation of synaptic function in the frog sympathetic ganglion.
Synaptic transmission is inhibited by morphine in isolated sympathetic ganglia of frog and rat. This action of morphine can competitively be antagonized by naloxone, nalorphine as well as by increasing the Ca++ concentration of the medium. The morphine antagonistic action of Ca++ can be suspended by Mg++ applied in an equimolar concentration. These results show that morphine inhibits synaptic transmission by shifting the ionic balance necessary for transmitter release.
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It has been known that chloroquine and mepacrine, through their parasympatholytic and spasmolytic effects, inhibit the gastric motility in rats. In the present study these drugs were shown to prevent by virtue of their antispasmodic property the spontaneous and induced movements in the isolated portal vein of the rat. As measured on isolated fundus strips of the stomach, chloroquine and mepacrine possessed almost the same pD'2 as had papaverine and drotaverine on the isolated portal vein. Chloroquine and mepacrine as well as the drugs used for comparison administered in vivo into the small intestine reached such concentrations in the portal vein blood which were shown to be capable of inhibiting the spontaneous and evoked movements in vitro.
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It was shown on the isolated superior cervical ganglion of the rat that some antiobiotics exerted a blocking effect nearly as potent as that exhibited by hexamethonium or d-turbocurarine. The ganglionic blockade thus induced proved to be non-specific and due to the local anaesthetic effect of the tested drugs.
Pharmacological responses of spiral strips prepared from the guinea pig vas deferens to various adrenergic and cholinergic agonists and autacoids were studied. On the circular muscle alpha adrenergic, muscarinic cholinergic and histaminergic receptors were identified. The responses evoked on the circular and longitudinal muscles were of the same type.
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Mepacrine given orally to rats inhibits gastric motility; its blocking effect is comparable to that of chloroquine, papaverine, and drotaverine, but less expressed than that of bencyclane. Similarly as the delayed gastric emptying induced by chloroquine, the effect of mepacrine is antagonized by acetyl-beta-methylcholine in a dose-related fashion, while that of papaverine, drotaverine, and bencyclane remains unchanged after treatment with the cholinomimetic drug.