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)

We prepared nine analogues (1-9) of MCPA-D-Phe-Phe-Ile-Asn-Cys-Pro-Arg-Gly-NH2, [MCPA1, D-Phe2, Phe3, Ile4, Arg8]oxytocin (MCPA = beta-mercapto-beta,beta-pentamethylenepropionic acid), a potent antagonist of the rat uterotonic action of oxytocin (OT). We replaced D-Phe with D-Trp and made [MCPA1,D-Trp2,Phe3,Ile4,Arg8]OT (1), which had OT pA2 of 7.51, somewhat higher than that of the D-Phe2 antagonist which has OT pA2 = 7.35 in our rat uterotonic assay. Both compounds are equipotent as antagonists of [Arg8]vasopressin in the rat antidiuretic assay, with pA2 = 8.1. Other substitutions gave [MCPA1,D-Trp2,4-Cl-Phe3,Ile4,Arg8]OT, (2), OT pA2 7.44; [MCPA1,D-Trp2,Phe3,Ile4,3,4-dehydro-Pro7,Arg8]OT (3), OT pA2 = 7.42; [MCPA1,D-Trp2,Phe3,Arg8]OT (4), OT pA2 = 7.58; [MCPA1,D-Trp2,Phe3,Arg8,Gly9-NHEt]OT (5), OT pA2 = 7.49; [MCPA1,D-Trp2,Ile4,Arg8]OT (6), OT pA2 = 7.46; [MCPA1,D-Trp2,Val4,Arg8]OT (7), OT pA2 = 7.58; [MCPA1,D-Trp2,Thr4,Arg8]OT (8), OT pA2 = 7.48; and finally, [MCPA1,D-Trp2,Arg8]OT (9), which was a more potent and more selective OT antagonist, with OT pA2 = 7.77 in the uterotonic assay and ADH pA2 less than 5.9 in the antidiuretic assay and hence is an important lead for the design of OT antagonists.
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PMID:Design of potent oxytocin antagonists featuring D-tryptophan at position 2. 199 88

The maturity of the hypothalamic-neurohypophyseal system in the first 10 days of the postnatal life of rats was analysed through the potential inhibitory effect of ethanol on oxytocin and vasopressin secretion. Experimental animals were intraperitoneally injected with ethanol, and the control ones with the corresponding amount of physiological solution. Hypophyses were extracted 30 min later to be histologically analysed. Although the morphological features of neurohypophysis with functionally active pituicytes and dense vascular net were present even from the first natal day, neurosecretory grains were noticed not before the 8 th day. But the inhibitory effect of ethanol on neurosecretion did not manifest itself until the 10 th day, so it can be concluded that in this period the hypothalamic-neurohypophyseal system had not yet reached its level of complete maturity. Fatty acids in pituicytes being elements of neurohypophyseal neuroglia are pronunced even in animals younger than 10 days, which indicates that their origin could not be necessarily linked to the process of neurosecretion. In acutely alcoholized offsprings the amount of fatty acids in the neurohypophysis was reduced. This is substantiated by the engagement of the alcohol dehydrogenase (ADH) and the microsomal ethanol-oxidizing system (MEOS) in alcohol metabolism with which follows retarded oxidation process of fatty acids.
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PMID:[Reactive characteristics of the neurohypophysis in the early postnatal period]. 228 3

To test the effects of colchicine and cytochalasin B on the ADH-induced response, unidirectional and net water fluxes were measured at one or two minutes intervals in frog urinary bladder. The action of these agents on the appearance of intramembrane particles aggregates in the luminal membrane of target cells under oxytocin stimulation and the changes in the tissue ultrastructure induced by cytochalasin B were also studied. It was observed that: the time-course of the response to oxytocin was strongly slowed by colchicine while the washout was not affected; the time-course of the 'on and off' of the response to oxytocin was not modified by cytochalasin B; cytochalasin B pretreatment proportionally reduced unidirectional and net water fluxes measured after glutaraldehyde fixation; the combined action of colchicine and cytochalasin B proportionally reduced the net water flux and the number of intramembrane particles aggregates, observed in freeze-fracture studies; after cytochalasin B action the dilation of intercellular spaces classically observed under oxytocin stimulation is strongly reduced. It is concluded that: microtubules probably play an important role in the water channels plug-in, but not in their removal; microfilaments integrity is necessary for the mechanisms inducing intercellular space dilation and the observed results confirm that water permeability is controlled by the number of permeation units present in the luminal border of granular cells and probably represented by the intramembrane particle aggregates.
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PMID:The role of microtubules and microfilaments in the hydrosmotic response to antidiuretic hormone. 241 25

PGE2 synthesis was measured along the nephron of Brattleboro (DI) rats, lacking ADH, and control LE rats, using an enzyme immunoassay. Experiments were performed in vitro, in the absence of exogenous arachidonic acid, using microdissected tubular segments. The effect of a chronic treatment of dDAVP was tested on three ADH sensitive tubular segments, medullary thick ascending limb (MTAL), medullary collecting tubule (OMCD) and papillary collecting duct (IMCD). No difference in PGE2 synthesis was present between LE and DI in glomerulus and tubular segments up to OMCD. In both strains, values were low in the proximal tubule and the loop of Henle, and gradually increased along the collecting tubule. In IMCD, PGE2 synthesis was much higher in DI (12.8 +/- 2.0 pg per 30 min per mm tubular length) than in LE (3.8 +/- 0.5, LE vs. DI p less than 0.001). In MTAL and OMCD, dDAVP treatment did not affect PGE2 synthesis. In IMCD, dDAVP reduced PGE2 synthesis to values (5.3 +/- 0.8 pg per 30 min per mm tubular length), which were not significantly different from those of LE. Neither oxytocin, which has been shown to be elevated in DI rats, nor furosemide, that reduced papillary osmolarity to values comparable to those of DI rats, were able to increase PGE2 synthesis in IMCD of LE rats. The mechanism of the increase in PGE2 synthesis in IMCD of DI rats, and of the inhibitory effect of dDAVP is yet unknown; it may participate to compensate for the lack of ADH in the Brattleboro rat.
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PMID:Antidiuretic hormone reduces the high PGE2 synthesis in papillary collecting duct of DI rats. 279 42

To find out whether plasma vasopressin (PAVP) response to a water load during pregnancy is inappropriately high, as had been speculated, we measured PAVP by radioimmunoassay in 30 women at the time of delivery. Ten women had received infusion of aqueous glucose solution during labor for hydration (GW group); another ten received infusion of glucose solution as a vehicle for oxytocin (OT group), and ten women did not receive any intrapartum intravenous fluid therapy (controls). Serum sodium and osmolality were also determined in all the subjects. PAVP levels were significantly lower in GW (0.70 +/- 0.4 pg/ml) and OT groups (0.7 +/- 0.6 pg/ml) (P less than 0.05). Significant negative correlation was seen between the amount of glucose solution infused and levels of PAVP (r = -0.66; P less than 0.01), while a significant positive correlation was seen between PAVP and serum sodium (r = 0.61; P less than 0.01). These findings suggest that during labor, the physiological relationship between serum osmolality and PAVP is intact, and that infusion of a water load in the form of aqueous glucose solution is attended by an expected lowering of PAVP. We infer that inappropriate ADH response is not the cause of water retention and hyponatremia often seen in women receiving aqueous glucose solution during labor.
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PMID:Plasma arginine vasopressin response to water load during labor. 286 30

Experiments were designed to determine the action of regulatory peptides and potassium on the secretion of tissue kallikrein by the isolated perfused rat kidney. Such experiments indicated that in spite of the directly evoked release of kallikrein by arginine-vasopressin (AVP, ADH), oxytocin and potassium from isolated renal cortical slices, the secretion and clearance of active and total tissue kallikrein by the isolated kidney was primarily sensitive to changes in the perfusion pressure.
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PMID:Release of tissue kallikrein from the isolated perfused kidney. 294 42

The most examined tumor markers in lung cancer patients are CEA, hormonal peptides, and some neurogenic enzymes in small cell carcinoma. Calcitonin, ACTH, ADH, CEA, neurophysin, oxytocin, beta-endorphin, neuron-specific enolase, and CK BB are elevated in serum specimens in 25-75% of cases of small cell carcinoma. The level of these markers is related to the stage of the disease in groups of patients; elevated pretreatment levels decrease with tumor regression. Marker levels are not valid in defining the tumor load and the presence of disease in the individual patient. It has not yet been documented that the markers can be used for clinical decisions on antineoplastic therapy. A recent development is the finding that measurement of CSF and plasma concentrations of ADH, calcitonin, CK BB, bombesin, and neuron-specific enolase may contribute in the diagnosis of CNS metastases including meningeal carcinomatosis.
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PMID:Tumor markers in patients with lung cancer. 300 40

Neurophysin 1 (a peptide associated with antidiuretic homone, ADH), ADH, and oxytocin were measured in serum or urine of 3 men who took 10 mcg ethinyl estradiol with 5 mg norethisterone acetate twice daily for 6 days and in 3 who took the estrogen only. Neurophysin in plasma was determined by radioimmunoassy, and individually by starch gel electrophoresis, extraction, and assay. Total urine neurophysin was measured by radioimmunoassy. ADH and oxytocin were quantitated by column chromatography and radioimmunoassy. With both steroids, there was no change in neurophysin, ADH, or oxytocin. Ethinyl estradiol alone increased urinary neurophysin from 112.3 to 595 ng/hour (n.s.), oxytocin from 41-132 ng/hour (p less than .005), and ADH from 9.7-57.2 ng/hour (p less than .01). As in pregnant women compared to normal women, estrogen treatment stimulated plasma neurophysin 1 more than neurophysin 2 in these subjects. These results confirm those found in rats.
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PMID:[Interactions between a progestational derivative (norethisterone acetate) and ethinyl estradiol on urinary elimination of neurophysin, ocytocin, and vasopressin and on the blood level of neurophysin I and II in normal human beings]. 460 73

1. Electrical recordings were made from antidromically identified supraoptic and paraventricular units during intracarotid injections of hypertonic and isotonic sodium chloride solutions in rats.2. The blood concentrations of vasopressin and oxytocin were estimated by bio-assay before and at different intervals after similar injections.3. Although a significant change in the action potential activity of the supraoptic nucleus was associated with hormone release, the results were not entirely consistent with a simple relationship between action potential activity and hormone secretion. Firstly, although some units were excited by the stimulus a substantial number were inhibited. Secondly, the blood concentration of the hormones, particularly ADH, remained elevated for longer than might have been expected if additional hormone had ceased to be secreted as soon as firing rates had returned to control values.4. There were substantial differences between the initial blood concentrations of vasopressin and oxytocin but the firing rates of units in the supraoptic and paraventricular nuclei appeared to be the same.5. Although significantly less paraventricular than supraoptic units were affected by hypertonic injections the blood concentration of oxytocin was increased by a factor of 8 whereas that of vasopressin was increased by a factor of 2.7.
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PMID:Oxytocin and ADH secretion in relation to electrical activity in antidromically identified supraoptic and paraventricular units. 557 37

This report concerns a review of the neuroendocrine effects of narcotic analgesics and endorphins. Acute administration of narcotic analgesics to rats increases the blood levels of ACTH, GH and prolactin, and decreases levels of LH and TSH, however, there is no general consensus regarding changes in serum FSH, ADH and oxytocin as induced by narcotics in rats. In humans, the narcotic analgesic increases in serum prolactin, decreases in serum LH and has no effect on the release of other known pituitary hormones. Endorphins mimic morphine regarding hormonal effects. Effects of naloxone on the basal levels of prolactin, LH or GH were inverse to the effects seen with narcotics and endorphins, therefore endorphins may play a role in regulating the basal levels of these hormones. Narcotics analgesics depress the increased blood levels of prolactin, gonadotropins or TSH elicited by specific measures. While chronic administration of morphine results in tolerance to the stimulant effect of ACTH, and possibly of prolactin secretion, tolerance does not develop to the stimulant effect on GH secretion. The analgesic potency of narcotic analgesics correlates with their suppressive effect on the pituitary-gonadal system and the potency with which endorphins bind to the opiate receptors correlates with their prolactin releasing activity. It is assumed that narcotic analgesics and endorphins exert their hormonal effects by altering the release of neurotransmitters in the CNS. Thus, a release of hypothalamic releasing hormones is involved rather than a direct action on the pituitary. The central neurotransmitter systems involved in the hormonal effects of narcotics are now being intensively investigated by various groups of workers.
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PMID:[Narcotic analgesics and endorphins and the release of pituitary hormones (author's transl)]. 611 Jun 21


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