Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C1323099 (sympathomimetic)
 2,957 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

This study has been undertaken to determine whether pentazocine induces catecholamine efflux from the adrenal medulla as a mechanism for its sympathomimetic effect. Dog isolated adrenals were perfused retrogradely with modified Locke's solution. The efflux of catecholamines from dog perfused adrenals was increased from the resting output of 0.18 +/- 0.04 micrograms min-1 (mean +/- s.e.), to 0.47 +/- 0.13 micrograms min-1 by the administration of pentazocine (50 microM). The pentazocine-induced catecholamine efflux was dose-dependent in the 50-400 microM dose range. This effect of pentazocine was not inhibited by either a combination of atropine and (+)-tubocurarine, or verapamil, in contrast to acetylcholine-induced catecholamine release. There was no significant difference in potency among stereoisomers, i.e. (+)-, (-)- and (+/-)-pentazocine, in inducing catecholamine efflux. Naloxone did not influence the effects of either (+)- or (-)-pentazocine. The interaction of pentazocine with acetylcholine-induced catecholamine release was also examined. Both (+)- and (-)-pentazocine inhibited acetylcholine-induced catecholamine release dose-dependently, and these inhibitory effects were not reversed by naloxone. Acetylcholine-induced catecholamine release was accompanied by increased dopamine-beta-hydroxylase release, whereas pentazocine-induced catecholamine efflux was not. These results suggest that pentazocine directly acts on the adrenal medulla to induce catecholamine efflux via a non-exocytotic mechanism, and that opioid receptors do not play a role in this action.
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PMID:Pentazocine-induced catecholamine efflux from the dog perfused adrenals. 168 Jan 75

After cardiac transplantation, the denervated donor atria and ventricles demonstrate increased sensitivity to infusions of sympathomimetic amines. Recently, supersensitivity of the canine sinus and atrioventricular (AV) nodes to acetylcholine has also been demonstrated after parasympathetic denervation. Acetylcholine and the endogenous nucleoside adenosine exert similar electrophysiological effects in both the sinus and AV nodes, and share a common transduction process. We, therefore, hypothesized that after orthotopic cardiac transplantation, the donor (denervated) sinus node would demonstrate greater sensitivity to exogenous adenosine than the recipient (innervated) sinus node. The effects of incremental doses of intravenous adenosine (37-112 micrograms/kg) on changes in sinus cycle length (SCL) (delta SCLmax%), changes in PR interval (delta PRmax%), time to peak effect (sec), and duration of electrophysiological effects (sec) were prospectively measured in 28 orthotopic cardiac transplant patients and nine control subjects. The baseline SCL was 795 +/- 71 msec for the control subjects, 891 +/- 43 msec for the recipient atria, and 700 +/- 18 msec for the donor atria (p less than 0.05, donor vs. recipient). The delta SCLmax% for each dose of adenosine was similar in the innervated control and recipient atria. In contrast, the donor sinus node demonstrated a threefold to fourfold increased response to adenosine as compared with the recipient sinus node and a threefold to sixfold increased response as compared with control subjects. Similarly, the donor AV node demonstrated a threefold to fivefold increase in PR interval as compared with control subjects. The duration of sinus node slowing in the denervated atria was threefold to fivefold longer than in the recipient and control atria (p less than 0.001).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Electrophysiological effects of adenosine in the transplanted human heart. Evidence of supersensitivity. 230 33

The effects of cholinomimetic and sympathomimetic drugs on the release of [3H]-gamma-aminobutyric acid ([3H]-GABA) evoked by high K+ from the isolated small intestine of the guinea-pig were investigated, in the presence of tetrodotoxin. Acetylcholine and oxotremorine, at concentrations ranging from 10(-9) to 10(-6) M inhibited the evoked release of [3H]-GABA in a concentration-dependent manner, while nicotine was without effect. Scopolamine and pirenzepine inhibited the effect of oxotremorine, while hexamethonium had no effect. The IC50 values for scopolamine and pirenzepine of the oxotremorine (3 X 10(-8) M)-induced inhibition were 1.02 X 10(-9) M and 9.78 X 10(-10) M, respectively. Noradrenaline, but not isoprenaline inhibited the evoked release of [3H]-GABA. Clonidine (10(-10)-10(-6) M) reduced the evoked release of [3H]-GABA in a concentration-dependent manner, but phenylephrine had no effect. The inhibitory effect of clonidine was antagonized by yohimbine but not by prazosin. These findings provide evidence for the localization of M1-muscarinic and alpha 2-adrenoceptors on GABAergic nerve terminals and their involvement in the presynaptic control of the release of GABA from the guinea-pig small intestine.
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PMID:Presynaptic muscarinic and alpha-adrenoceptor-mediated regulation of GABA release from myenteric neurones of the guinea-pig small intestine. 302 51

Freshly isolated hearts of fetal mice of gestational ages ranging between 12 and 22 days (term) were exposed to several concentrations of a variety of chronotropic agents. Acetylcholine (10(-4)-10(-2) M) caused marked bradycardia in all hearts, even after only 12-14 days' gestation (i.e., even before cardiac innervation had occurred), and the intensity of the response increased steadily with advancing age throughout gestation. Responsiveness to norepinephrine was present but minimal at 12-14 days, so that mean atrial rate rose by < 10% with a maximal concentration of the drug (10(-5) M); responsiveness became more marked by 15-16 days (just after the time atrial innervation is thought to begin) and still greater effects appeared just before term. Glucagon had no effect in hearts of < 17 days' gestational age, but caused tachycardia thereafter, indicating that cardiac responsiveness to glucagon differentiates later than does responsiveness to norepinephrine. Responses to theophyl-line in 12-14 day hearts exceeded those to norepinephrine, indicating that the drug can affect heart rate independently of its ability to cause release of endogenous catecholamines. In contrast, tyramine caused no response until 21-22 days, well after the time the beta-receptor has differentiated and after innervation is fairly well developed, suggesting that the drug's primary sympathomimetic effect is indirect rather than direct. Dibutyryl cyclic AMP did not cause tachycardia at any fetal age. It is concluded that maturation of responsiveness of the mouse heart to cardioactive drugs develops in specific patterns for different agents. The identification of differential patterns of maturation for various drugs may provide valuable means for characterizing the differentiation of specific receptors and for investigating possible mechanisms of action of the drugs.
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PMID:Maturation of responsiveness to cardioactive drugs. Differential effects of acetylcholine, norepinephrine, theophylline, tyramine, glucagon, and dibutyryl cyclic AMP on atrial rate in hearts of fetal mice. 435 75

Human lung tissue passively sensitized with anti-grass pollen IgE antibodies releases histamine upon exposure to specific grass pollen antigen. Beta-sympathomimetic agents inhibit the antigen-induced release of histamine, thus beta-sympathomimetic drugs might exhibit a combination of prophylactic and direct bronchodilating properties in the treatment of allergic bronchial asthma. The anticholinergic agent ipratropium bromide had no direct effect on the immunologically induced release of histamine. Acetylcholine increased the antigen-induced release of histamine significantly. This enhanced release was almost completely inhibited by ipratropium bromide as a result of competitive inhibition. This mode of action may add to the usefulness of anticholinergic agents in vagus-controlled chronic obstructive ventilatory disorders.
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PMID:Anti-allergic effect of beta-2 agonists and cholinoceptor antagonists in vitro. 619 94

The effects of some cholinomimetic and sympathomimetic drugs have been investigated on the isolated rectal muscles of West African rainbow lizard (Agama agama) and land tortoise (Kinixys crosa). Acetylcholine and its natural or synthetic analogues evoked concentration-related atropine-sensitive contractions of the muscle preparations, whereas all the catecholamines examined relaxed the lizard (and guinea-pig), but not the tortoise, isolated rectum in a dose-dependent fashion. The ganglionic stimulant drugs used, nicotine and DMPP, did not produce any effect on the isolated rectum of the two reptiles, although they contracted the guinea-pig isolated rectum in a concentration-dependent manner. Concentrations of physostigmine, which induced spasms or contractions in the isolated rectum of the guinea-pig, failed to excite reptilian rectal muscle preparations. Histamine induced biphasic responses in the lizard isolated rectum without affecting the isolated rectum of the tortoise. Serotonin (5-HT) which contracted the isolated rectum of the guinea-pig (like histamine) also provoked variable contractions of the lizard rectum but did not affect the tortoise isolated rectum. It is therefore concluded that although the rectal smooth muscles of these two terrestrial West African reptiles possess cholinergic innervation with mainly "muscarinic" cholinoceptors, their autonomic innervation differs from that of a conventional mammalian (e.g. guinea-pig) gastrointestinal tract smooth muscle.
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PMID:Comparative effects of some autonomic drugs on lizard (Agama agama) and tortoise (Kinixys crosa) isolated rectum. 666 73

The responses of the isolated rectum of the domestic chick (Gallus domesticus) to some drugs have been investigated. The tissue was found to be qualitatively and quantitatively similar to conventional mammalian gastrointestinal smooth muscles in its responses to pharmacological agents, and serves as a useful isolated smooth muscle preparation for investigating drug actions and interactions. Acetylcholine and its natural or synthetic analogues induced atropine-sensitive contractions of the tissue, while noradrenaline and other sympathomimetic drugs examined caused phentolamine-sensitive relaxations. 5-hydroxytryptamine contracted the tissue preparation, while histamine evoked a biphasic action (either a contraction or a relaxation, or even both occurring together one after the other). Potassium or barium ions contracted the muscle while magnesium ions relaxed it. Nicotine and dimethylphenylpiperazinium showed no effects on the muscle. The pharmacological implications of these findings are discussed. The receptor types present on the muscle have been classified as muscarinic cholinoceptors; histamine H1-and H2receptors; 5-hydroxytryptamine receptors, and alpha-adrenoceptors respectively.
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PMID:Studies on the responses of the isolated rectum of domestic chick (Gallus domesticus) to drugs. 734 58