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At least 829 records · Page 46Linked to original sources
PubMed1977

Characteristics of the relaxant response of adenosine and its analogs in intestinal smooth muscle.

Several characteristics of the relaxant response of the isolated longitudinal muscle of the rabbit small intestine in response to the administration of adenosine and related compounds are studied. Following administration of adenosine or ATP the preparation responded with a rapid initial suppression of spontaneous contractile activity followed by a secondary sustained phase of inhibition of lower magnitude. Cumulative application of relaxant doses of adenosine or ATP caused a lesser total response than that obtained by single application of the cumulative dose. Neither procaine, lidocaine or guanethidine antagonized the responses to adenosine or ATP and the responsiveness of muscles obtained from reserpinized animals appeared unchanged. A number of adenosine derivatives and analogs was tested for the ability to relax the muscle. Generally, compounds containing a primary or secondary 6-amino group acted as agonists with the exception of 8-bromoadenosine. Those nucleosides found to be inactive did not modify the responsiveness of the muscle to adenosine. Responses to adenosine and ATP were not appreciably modified by papaverine, imidazole, dipyridamole, 6-(p-nitrobenzylthio)-purine riboside. Antagonism was observed, however, with phentolamine and theophylline. Theophylline at 100 muM inhibited responses to adenosine over a wide dose range; this antagonism was surmountable by high doses of adenosine. 1-Methyl-3-isobutylxanthine did not antagonize adenosine responses. A number of 1,3-alkyl-6-thioxanthines did not modify the adenosine response at doses that did not show any direct action. The results supported the concept of an extracellular receptor site of adenosine and its analogs and the absence of an indirect mechanism of action via nerve stimulation.

Adenosine↗
PubMed1983

Different types of blockade of crustacean acetylcholine-induced currents.

The voltage dependence, concentration dependence, and agonist dependence of blocking and unblocking produced by anticholinergic agents on the ionophoretically activated cholinergic currents of the lobster gastric mill 1 (g.m.1) muscle were examined. Although the ionophoretic technique provides only qualitative information as to blocking mechanisms it is useful in revealing slow components of the blocking action of some drugs. At least two qualitatively different types of voltage-dependent block of the crustacean cholinergic currents were observed. For pempidine, mecamylamine and decamethonium (also chlorisondamine: Lingle, 1983), a slowly developing voltage-dependent block was produced that led to the formation of a stable-blocked state. Recovery from this stable-blocked state is largely dependent on subsequent application of agonist. In contrast, recovery from the voltage-dependent block produced by QX-222, atropine, procaine and curare either proceeds independently of agonist application or occurs too rapidly to be observed by the present methods. Blockade by hexamethonium reveals anomalous voltage dependence, being enhanced over some voltages and relieved with additional hyperpolarization. Blockade by trimetaphan is largely independent of membrane potential except at higher concentrations.

Animals↗
PubMed1963

THE SITE OF THE 5-HYDROXYTRYPTAMINE RECEPTOR ON THE INTRAMURAL NERVOUS PLEXUS OF THE GUINEA-PIG ISOLATED ILEUM.

Dose/response measurements were made on the guinea-pig isolated ileum with six agonists, acetylcholine, 5-hydroxytryptamine, nicotine, dimethylphenylpiperazinium, choline phenyl ether and histamine. The dose effects were repeated in the presence of each of twelve antagonists and one anticholinesterase. Acetylcholine and histamine were chosen because of their direct mode of action on smooth muscle, nicotine, dimethylphenylpiperazinium and choline phenyl ether were used as examples of drugs that act at the ganglionic acetylcholine receptor. 5-Hydroxytryptamine was the drug investigated. Hyoscine blocked the contractions caused by acetylcholine, 5-hydroxytryptamine and the ganglion-stimulants but left the responses to histamine unchanged. The anticholinesterase N,N'-diisopropylphosphorodiamidic fluoride (mipafox) potentiated all the agonists except histamine. The strength of potentiation decreased in the order 5-hydroxytryptamine, nicotine, dimethylphenylpiperazinium and choline phenyl ether, and acetylcholine. The local anaesthetic procaine inhibited to the same extent contractions elicited by 5-hydroxytryptamine, nicotine, dimethylphenylpiperazinium and choline phenyl ether. These results showed that 5-hydroxytryptamine, like nicotine, choline phenyl ether and dimethylphenylpiperazinium, mediated its response through the nervous plexus. Of those tested 5-hydroxytryptamine was the only specific antagonist to 5-hydroxytryptamine; lysergic acid derivatives produced spasm and prolonged changes in tone; phenoxybenzamine caused non-specific block. The diverse modes of action of a number of ganglion-blocking agents were selectively used. Thus hexamethonium, pentolinium, and nicotine in its competitive phase, blocked contractions due to nicotine, dimethylphenylpiperazinium and choline phenyl ether and left those due to 5-hydroxytryptamine, acetylcholine and histamine unchanged. The depolarizing ganglion-blocking agents, dimethylphenylpiperazinium and nicotine, inhibited the responses to all the indirectly acting drugs. Furthermore, mecamylamine, a drug with a less well-defined mode of action, partially inhibited contractions due to 5-hydroxytryptamine in a concentration that blocked those due to nicotine, dimethylphenylpiperazinium and choline phenyl ether. Pempidine, known to act like mecamylamine, did not antagonize 5-hydroxytryptamine. It is concluded that 5-hydroxytryptamine activates specific receptors sited at the intramural parasympathetic ganglion cells.

Acetylcholine↗
PubMed1993

Comparison of local anesthetic activity of pentacaine (trapencaine) and some of its derivatives by three different techniques.

The local anesthetic potency of the carbanilic drug pentacaine (1; trapencaine) was compared to that of a series of its derivatives as well as procaine and cocaine. It is known that 1 exhibits potent local anesthetic, gastroprotective and antiulcer activities. The local anesthetic potency of the drugs under study was tested by three different techniques, i.e. analysis of compound action potential amplitude in rat sciatic nerve in vitro, duration of full anesthesia in rabbit cornea in vivo as well as in guinea-pig skin in vivo. The potency was expressed as drug concentration evoking either 50% reduction in action potential amplitude in the isolated nerve or anesthesia lasting for 20 min in the other two techniques. The most powerful anesthetics were found to be 1, K1905, and K2002 with their potency exceeding that of procaine and cocaine by 1-2 orders. The derivatives P1, P2, and P3 were much less effective, their potency being comparable to the two reference drugs. Although there were remarkable differences in the ranges of effective concentrations of particular drugs in the techniques used, a comparatively good agreement was found in the orders of the drug potencies. Plotting local anesthetic potency and drug lipophilicity revealed a good positive correlation between these two parameters in the group of the drugs tested.

Action Potentials↗
PubMed1972

Ionic differences between somatic and axonal action potentials in snail giant neurones.

1. The ionic requirements of the somatic and axonal action potentials of ;H' neurones of the snail Cryptomphallus aspersa were studied using intracellular micro-electrodes.2. The overshoot of the somatic action potential increased by 10 mV for a tenfold increase in [Ca(2+)](o). In calcium-free media the action potential decreased gradually to values of 50 to 90% of the control and they could be completely eliminated with 2 mM-EGTA. The maximum rate of rise also varied with [Ca(2+)](o).3. After 2 hr in sodium-free solution the somatic action potential decreased 6% in overshoot and 24% in rate of rise.4. The somatic action potential was not affected by TTX, 5 x 10(-6) g/ml. Procaine, 18 mM, reduced its rate of rise but did not eliminate it whereas 30 mM-CoCl(2) did.5. The size of the axonal action potential increased with increased [Na(+)](o), but decreased with an increase in [Ca(2+)](o).6. Procaine, 18 mM, abolished the axonal action potential whereas it was not affected by TTX, 5 x 10(-6) g/ml., nor, usually, by 30 mM-CoCl(2).7. The results obtained by studying the compound action potential of the nerves were similar to those from axonal action potentials.8. The possibility that the somatic action potential is mainly calcium dependent while the axonal action potential is mainly produced by sodium is discussed.

Action Potentials↗
PubMed1984

Rapid screening and confirmation for drugs and metabolites in racing animals by tandem mass spectrometry.

A screening and confirmation procedure for drugs and metabolites in the blood serum and urine of racing animals was developed. Equine blood serum was spiked with low concentrations of several drugs of interest. Canine blood serum and urine were collected following oral doses of diethylcarbamazine, procaine, and phenylbutazone. Serum, urine, and extracts of each were analyzed, using a triple quadrupole mass spectrometer. Simultaneous screening of up to 50 drugs was possible in a single sample, in less than 2 minutes. Detection limits for most compounds were in the ng/ml to microgram/ml range, using 1-microliter samples. This procedure provided fast, sensitive screening for selected drugs and metabolites in blood serum and urine.

Animals↗