Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P01178 (oxytocin)
 15,767 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The effect of verapamil, flunarizine, nimodipine, nicardipine, and nifedipine, calcium channel inhibitors, and of indomethacin and aspirin, inhibitors of prostaglandin synthesis, on penile erection and yawning induced by oxytocin was studied in male rats. All calcium channel inhibitors given intraperitoneally (IP) 60 min before the intracerebroventricular (ICV) injection of oxytocin (30 ng) prevented in a dose-dependent manner oxytocin effect. Nimodipine and nicardipine were the most effective being active at doses between 5 and 20 mg/kg, while the others were active at doses higher than 15 mg/kg. Prevention of oxytocin effect was also seen after ICV injection of the above compounds. Unlike calcium channel inhibitors, indomethacin given either IP (10 and 50 mg/kg) or ICV (50 micrograms), or aspirin (100 mg/kg IP) were ineffective. Microinjection of calcium, but not of prostaglandin E2 and prostaglandin F2 alpha in the paraventricular nucleus of the hypothalamus, the brain area most sensitive for the induction of the above behavioral responses by oxytocin, induced a symptomatology similar to that induced by oxytocin. The present results suggest that calcium might be the second messenger which mediates the expression of penile erection and yawning induced by oxytocin.
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PMID:Oxytocin-induced penile erection and yawning: role of calcium and prostaglandins. 233 53

The effect of omega-conotoxin GVIA, a potent and selective inhibitor of N-type calcium channels and of the organic calcium channel inhibitors nimodipine, verapamil and flunarizine, on stretching, yawning and penile erection induced by ACTH 1-24 was studied in male rats. omega-Conotoxin (1-10 ng ICV 15 min before ACTH, 10 micrograms ICV), but not carboxymethylated omega-conotoxin, induced a dose-dependent prevention of all ACTH effects. In contrast, organic calcium channel inhibitors (20 mg/kg IP 30-60 min before ACTH) failed to modify ACTH-induced stretching and yawning but induced a 25% decrease in the number of penile erection episodes induced by the peptide, and prevented, like ICV omega-conotoxin, oxytocin- and apomorphine-induced yawning and penile erection. When injected in the paraventricular nucleus of the hypothalamus, omega-conotoxin prevented the above behavioral responses induced by apomorphine and oxytocin but not by ACTH 1-24. The present results suggest that ACTH induces stretching, yawning and penile erection by mobilizing calcium through central omega-conotoxin-sensitive calcium channels in brain sites different from those sensitive to oxytocin and apomorphine.
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PMID:Role of calcium in the expression of ACTH-induced stretching, yawning and penile erection. 237 2

The hormone relaxin has recently been shown to inhibit not only uterine muscle contraction, but also the release of oxytocin into the plasma. Intravenous injection of porcine relaxin in anaesthetized lactating rats inhibits milk ejection and injection of relaxin into the cerebral ventricles disturbs the pattern of the milk ejection reflex. Recent experiments performed in vivo indicate that relaxin might act not only in the uterus, but also in the hypothalamus and possibly in the neurohypophysis. We tested this hypothesis in vitro by studying the effect of relaxin on hormone release from isolated neural lobes of the pituitary and isolated neurosecretory nerve endings of the neurohypophysis from the rat. We report here that relaxin has a dual effect on neurohypophysial hormone secretion. Under basal conditions, vasopressin and oxytocin release was inhibited by relaxin but, when the nerve endings were depolarized, vasopressin and oxytocin secretion was potentiated. We also found that relaxin acts at a stage before the increase in cytoplasmic free Ca2+ that is necessary for inducing hormone release, possibly by gating the calcium channel.
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PMID:Relaxin affects the release of oxytocin and vasopressin from the neurohypophysis. 243 61

Isolated rat paraventricular (PVN) and supraoptic (SON) nuclei were perifused in vitro and oxytocin and vasopressin releases were measured by radioimmunoassay during rest and during electrical stimulation. Stimulations at a frequency of 10 Hz (10-s bursts, every 10 s for 5 min) and an intensity of 4 mA, induced significant hormone release only with long duration pulses (10 ms). Short pulses (1 ms) applied at various frequencies (10, 20, 40 or 80 Hz) and intensities (4, 5, 10 or 20 mA) had no effect. The electrically evoked release of both hormones was not affected by tetrodotoxin (TTX), a sodium channel blocker, but was blocked in low-calcium medium or in the presence of gallopamil hydrochloride (D-600), a calcium channel blocker. These results suggest that, following electrical stimulation, oxytocin and vasopressin are released locally within the magnocellular nuclei even when blocking action potentials. The possibility of dendritic release is discussed.
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PMID:Electrical stimulations of perifused magnocellular nuclei in vitro elicit Ca2+-dependent, tetrodotoxin-insensitive release of oxytocin and vasopressin. 243 5

Previously (Van Driessche et al. 1987) we showed that small inward (mucosa towards serosa) oriented short-circuit currents (Isc) were recorded through the toad urinary bladder when the mucosal side was exposed to Ca2+ free solutions containing K+, Na+ (+ amiloride), Cs+ or Rb+ as main cation. This current component is inhibitable by micromolar concentrations of mucosal La3+ and divalent cations (Ca2+, Cd2+) and is considerably elevated by oxytocin (0.1 U/ml). The present study demonstrates that the addition of 50 nmol/l Ag+ to the mucosal medium during oxytocin treatment caused an additional large increase of the La3+-sensitive Isc component. The power density spectrum of the fluctuation in current contained a Lorentzian component which was enhanced by oxytocin treatment. The Lorentzian component disappeared as a consequence of the administration of mucosal Ag+. In experiments with Ca2+, Ba2+ or Mg2+ as principal mucosal cation, the La3+-sensitive Isc component was negligible under control conditions and during oxytocin treatment. Mucosal Ag+ (40 nmol/l) elicited a large inward oriented current which was blockable by the calcium channel blockers, La3+ and Cd2+. Also the organic calcium entry blockers, nicardipine and verapamil (10 mumol/l) depressed the inward current considerably. Noise analysis of the currents carried by divalent cations showed a La3+-sensitive noise component. Oxytocin-Ag+ activated currents could not be recorded in the absence of the divalent cations or small inorganic cations, e.g. with solutions which contained N-methyl D-glucamine (NMDG) as main mucosal cation.
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PMID:Ca2+ channels in the apical membrane of the toad urinary bladder. 244 54

Recent progress in our understanding of uterine smooth muscle contraction is reviewed. We no longer believe that actin-myosin interaction in the myometrium occurs through activation of the thin filament; but it is triggered by calcium-dependent phosphorylation of myosin in the thick filament. Calcium is now thought to originate from both extracellular and intracellular sources. Calcium can enter the cell through either a voltage- or a hormone-controlled calcium channel. The intracellular source of calcium is the sarcoplasmic reticulum. The effect of oxytocin in human labor is no longer considered the result of increased circulating oxytocin but rather of increased oxytocin receptors. In contrast, the contractile action of some prostaglandins is related to increased prostaglandin formation at human parturition. The step between hormone binding and cellular action is mediated by second messengers. The uterine-relaxing action of cyclic adenosine monophosphate is now thought to be limited to the inhibition of myosin phosphorylation. Recently discovered second messengers for contraction of the myometrium are phosphoinositides; their turnover causes calcium release from the sarcoplasmic reticulum. Guanine nucleotides are thought to be modulators of these two second messengers.
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PMID:A new look at uterine muscle contraction. 244

Neurohypophysial hormones stimulate gonadotrophin release from dispersed rat anterior pituitary cells in vitro, acting through receptors distinct from those which mediate the secretory response to gonadotrophin-releasing hormone (GnRH). The LH response to oxytocin was not affected by the presence of the phosphodiesterase inhibitor, methyl isobutylxanthine, but was diminished in the absence of extracellular calcium and was progressively increased as the calcium concentration in the medium was raised to normal. In addition, the calcium channel antagonist, nifedipine, suppressed oxytocin-stimulated secretion of LH. It is likely that the mechanisms of LH release induced by GnRH and neurohypophysial hormones are similar, although stimulation of gonadotrophin secretion is mediated by separate receptor systems. Oxytocin was more active than vasopressin in releasing LH, but less active in releasing ACTH. The highly selective oxytocin agonist, [Thr4,Gly7]oxytocin, elicited concentration-dependent secretion of LH but had little effect on corticotrophin secretion. The neurohypophysial hormone antagonist analogues, [d(CH2)5Tyr(Me)2]vasopressin, [d(CH2)5Tyr(Me)2,Orn8]vasotocin and [d(CH2)5D-Tyr(Et)2Val4,Cit8]vasopressin, inhibited the LH response to both oxytocin and vasopressin. However, [d(CH2)5Tyr(Me)2]vasopressin was much less effective in inhibiting the ACTH response to the neurohypophysial hormones, and [d(CH2)5Tyr-(Me)2,Orn8]vasotocin and [d(CH2)5D-Tyr(Et)2,Val4,Cit8]vasopressin exhibited no inhibitory activity against ACTH release. Thus, agonist and antagonist analogues of neurohypophysial hormones display divergent activities with regard to LH and ACTH responses, and the neuropeptide receptor mediating gonadotroph activation is clearly different from that on the corticotroph. Whereas the corticotroph receptor is a vasopressin-type receptor an oxytocin-type receptor is responsible for gonadotrophin release by neurohypophysial hormones.
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PMID:Gonadotrophin-releasing activity of neurohypophysial hormones: II. The pituitary oxytocin receptor mediating gonadotrophin release differs from that of corticotrophs. 247 64

Effects of endothelin on nonvascular smooth muscle have been examined using rat uterine horns and two modes of endothelin action have been revealed. Endothelin (0.3 nM) caused rhythmic contractions of isolated uterus in the presence of extracellular calcium. The rhythmic contractions were completely inhibited by calcium channel antagonists. These characteristics of endothelin-induced contractions were very similar to those induced by oxytocin. Binding assays using 125I-endothelin showed that endothelin and the calcium channel blockers did not compete for the binding sites. However, endothelin was unique in that it caused, in addition to rhythmic contractions, a slowly developing monophasic contraction that was insensitive to calcium channel blockers. This developing contraction became dominant at higher concentrations of endothelin and was also calcium dependent.
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PMID:Endothelin induces two types of contractions of rat uterus: phasic contractions by way of voltage-dependent calcium channels and developing contractions through a second type of calcium channels. 253 25

Tetramethylpyrazine is extracted from Rhizoma ligustici wallichii, an herb used in the Chinese medicine Chung Chong. Both herb and extract have been used in the treatment of anginal pain and stroke. Animal studies in the West have shown that tetramethylpyrazine improves coronary blood flow, is short acting, and has a low toxicity. There are no clinical or animal studies on the uterine effects of tetramethylpyrazine. We present results of a preliminary study with isolated uterine strips from rats. We found that tetramethylpyrazine, in a dose-dependent manner (0.6 to 20 micrograms/ml), reduced uterine diastolic tone and inhibited the response to oxytocin (0.02 to 0.32 micrograms/ml). Higher concentrations of tetramethylpyrazine were needed to block the uterine responses to prostaglandin E2 (0.01 to 0.1 microgram/ml). On the basis of clinical and folk experience in the Far East, tetramethylpyrazine appears to have fewer systemic effects in human beings than have the beta-adrenergic agonists or calcium channel blockers. We suggest that studies in the whole animal and in the clinic might provide reasons to use tetramethylpyrazine to reduce uterine contractions and tone in pregnant women at term.
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PMID:In vitro uterine response to tetramethylpyrazine, the active constituent of chung chong (a traditional Chinese medicine). 258 59

The synthesis of new radiolabelled compounds and the evolution of the techniques designed to study the hormonal receptors allow a better understanding of their properties. Three types of vasopressin receptors have been described: the V1a receptor of liver and blood vessels, the V1b receptor of hypophysis and the V2 receptor of kidney. Such a classification was based on two criteria: The structure of the binding site and the nature of the second messenger produced. The V2 receptor coupled positively to adenylate cyclase regulates the water reabsorption via the increase of intracellular cyclic AMP. The V1a and V1b receptors involved in glycogenolysis, contraction and probably neurotransmission mobilize intracellular calcium via a positive coupling to phospholipase C. These two receptors exhibit different recognition patterns for vasopressin analogues. In mammals, the oxytocin receptors are mainly involved in myometrial contraction and lactation. Their characterization are generally difficult since they also interact with vasopressin and are sometimes colocated with vasopressin receptors. As for V1 receptor, they are coupled to phospholipase C and mobilized intracellular calcium. The receptors of angiotensin II regulate the blood pressure by different mechanisms. They are coupled to at least two transduction mechanisms (positive coupling to phospholipase C and negative coupling to adenylate cyclase). Electrophysiological data seems to indicate that such receptor may also control a calcium channel. Yet different molecules (cAMP, calcium, inositol phosphates, diacyl-glycerol) trigger the hormonal effect of angiotensin II inside the cell.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Vasopressin, oxytocin and angiotensin receptors in mammals]. 269 9


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