Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P01185 (vasopressin)
 23,126 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

1. The effect of intramuscular injection of 8-arginine vasotocin, 8-arginine vasopressin, 8-lysine vasopressin, oxytocin, 8-ornithine oxytocin and 8-ornithine vasopressin on fluid uptake across the skin was studied in the live toad, Bufo melanostictus, bathed either in distilled water or in NaCl solution (0.1 g/100 ml.).2. When the bathing solution was distilled water, 8-arginine vasotocin was the most potent, 0.14 nmole/kg augmenting the rate of fluid uptake by 50%. Compared with it the others had relative potencies of: 8-arginine vasopressin 0.8, 8-lysine vasopressin 0.8 x 10(-3), oxytocin 0.8 x 10(-3), 8-ornithine oxytocin 0.8 x 10(-2), 8-ornithine vasopressin < 1.4 x 10(-4).3. When the bathing solution contained 0.1% NaCl, 8-arginine vasotocin was again the most potent, 0.06 nmole/kg augmenting the rate of fluid uptake by 50%. Compared with it the others had relative potencies of: 8-arginine vasopressin 0.3, 8-lysine vasopressin 0.3 x 10(-3), oxytocin 0.3 x 10(-2), 8-ornithine oxytocin 0.8 x 10(-2), 8-ornithine vasopressin < 0.6 x 10(-4).4. Dose-response curves for each peptide showed that in the case of 8-arginine vasopressin, 8-lysine vasopressin and 8-ornithine vasopressin the augmentation of rate of fluid uptake did not differ in the absence or in the presence of NaCl in the bathing solution; whereas in the case of 8-arginine vasotocin, oxytocin, and 8-ornithine oxytocin the augmentation was greater in the presence of sodium chloride.5. Support has been found for the postulate of a binary action of some neurohypophysial peptides on amphibian skin, arginine in position 8 being correlated with hydrosmotic effect, and isoleucine in position 3 with natriferic effect.
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PMID:Natriferic and hydrosmotic effects of neurohypophysial peptides and their analogues in augmenting fluid uptake by Bufo melanostictus. 567 41

A sensitive and precise method for assaying the water permeability response evoked by neurohypophyseal hormones and their synthetic analogues on the isolated urinary bladder of the toad (Bufo marinus L.) is described. The method permits detection of 8-arginine-vasotocin at concentrations as low as 10(-12)M. This sensitivity, not achieved heretofore with this tissue, results largely from minimizing interference of inhibitory substances by means of an "in vitro circulation assembly." The precision of the method derives from a direct comparison between the cumulative dose-response curve of an agonist of unknown potency acting on one hemibladder and that of a reference compound acting on the contralateral hemibladder. Crystalline deamino-oxytocin is used as the reference standard in this assay. The intrinsic activity of 2-(O-methyltyrosine)-oxytocin, as defined by the maximal response, is 12% lower than that of deamino-oxytocin. All other hormonal peptides investigated have the same intrinsic activity as deamino-oxytocin, even 5-valine-oxytocin, in spite of its extremely low affinity. A comparison of the potencies of 8-arginine-vasotocin vs. 8-arginine-vasopressin, 8-ornithine-vasotocin vs. 8-ornithine-vasopressin, 8-alanine-oxytocin vs. 8-alanine-oxypressin, and deamino-8-alanine-oxytocin vs. deamino-8-alanine-oxypressin suggests that an isoleucine residue in position 3 imparts a higher specificity for binding of the hormonal peptide molecule to the bladder receptor than a phenylalanine residue in this locus.
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PMID:A sensitive hydroosmotic toad bladder assay. Affinity and intrinsic activity of neurohypophyseal peptides. 569 11

A simple technique to inject the synthetic vasoconstrictor agent ornithine-8-vasopressin endoscopically into the prostate has been developed. The method has been assessed by two prospective randomised controlled trials on patients undergoing transurethral resection of the prostate. Results from the first trial, involving 56 patients who had general anaesthesia, were that the mean operative blood loss was 48% less in the treated group, a significant difference (P = 0.05). Results from the second trial, involving 57 patients who had spinal anaesthesia, were that the mean operative blood loss was 75% less in the treated group, a highly significant difference (P = 0.01). The pharmacology of the drug is reviewed, and it seems to be a safe agent which aids transurethral resection. It frequently causes a modest and transient elevation in blood pressure shortly after injection and, although not encountered by the author, it is possible that a more severe elevation necessitating treatment may rarely occur.
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PMID:Endoscopic injection of the vasoconstrictor ornithine-8-vasopressin in transurethral resection. 638 15

Antidromically identified paraventricular neurones were recorded simultaneously with intramammary pressure in urethane (1.2 g/kg) anaesthetized rats during suckling. The correlation of the firing pattern of these neurones with milk ejection enabled distinction between oxytocin and vasopressin neurones. Oxytocin neurones displayed a short (2-6 s) characteristic high-frequency burst of spikes. This activation probably occurred simultaneously in all oxytocin neurones 12-18 s before milk ejection and was regular in both frequency and amplitude (total number of spikes). The role of neurohypophysial peptides and analogues in the control of these characteristics was studied. Injecting 10 pg, 100 pg and 1 ng of oxytocin into the 3rd ventricle increased background activity of slow-firing oxytocin neurones (less than 3 spikes/s) and had a strong dose-dependent facilitatory effect on the milk ejection reflex, increasing both the amplitude and frequency of neurosecretory bursts. No effect was observed on non-neurosecretory neurones. Such injection also triggered the milk ejection reflex when it had not appeared an hour after suckling began. Oxytocin did not itself induce neurosecretory activation, which only appeared if the young rats were sucking. Injecting oxytocin into the lateral ventricle was less effective than into the 3rd ventricle. No effect was observed after injection into the venous blood or into the 4th ventricle, which suggested that oxytocin acts in the hypothalamus. Injecting mesotocin or isotocin into the 3rd ventricle had a facilitatory effect similar to that of oxytocin but vasopressin, vasotocin, MIF I (pro-leu-gly-NH2, terminal triplet oxytocin) or bovine neurophysins I and II did not modify neurosecretory activation or the milk ejection pattern. Injecting an oxytocin antagonist, ([1(beta-mercapto-beta, beta cyclopentamethylene propionic acid), 8-ornithine] vasotocin, d(CH2)5OVT) into the 3rd ventricle decreased milk ejection frequency and considerably delayed the reappearance of the first milk ejection. This resulted from a decrease in both frequency and amplitude of neurosecretory bursts, which were too small to induce detectable oxytocin release. Moreover, d(CH2)5OVT suppressed the facilitatory effect of exogenous oxytocin. Under normal conditions, endogenous oxytocin seemed to be involved in the control of neurosecretory activation. Injecting 1 ng oxytocin or 1 or 10 ng vasopressin into the 3rd ventricle did not modify the firing pattern of vasopressin neurones whether activated by hyperosmotic stimulation (1 ml NaCl, 9% solution (w/v) I.P.) or not.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Electrophysiological evidence for facilitatory control of oxytocin neurones by oxytocin during suckling in the rat. 674 98

We synthesized a series of analogs of arginine vasotocin by systematically substituting each residue, and we then evaluated the anovulatory activity of these compounds in the rat, investigating the correlation between molecular structure and anovulatory, pressor, and antidiuretic activities. Substitution of the N-terminus cysteine with 3-mercaptopropanoic acid in arginine vasotocin and arginine vasopressin produced a 3- to 4-fold increase in both anovulatory and antidiuretic activity and only a 10% change in pressor activity. A similar substitution with lysine vasopressin produced no significant change in either anovulatory or antidiuretic potency; however, the pressor activity was reduced by half. Substitution of this cysteine in arginine vasotocin with 2-hydroxy-3-mercaptopropanoic acid produced an analog more potent in anovulatory activity than arginine vasotocin but less potent than [1-(3-mercaptopropanoic acid)]-arginine vasotocin. The most potent anovulatory analog synthesized was [1-(3-mercaptopropanoic acid)]-8-ornithine vasotocin, which gave a 10-fold increase in anovulatory activity, a 4-fold reduction in antidiuretic activity, and only a 10% increase in pressor potency when compared with arginine vasotocin. These data suggest that different receptors are involved in the anovulatory and antidiuretic responses, but that the anovulatory and pressor effects may be mediated through similar receptors. Further work is necessary to produce a peptide that possesses specific anovulatory activity.
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PMID:Anovulatory effect of synthetic analogs of arginine vasotocin in the rat. 684 22

In this comparative study, we carried out liposuction on 20 patients randomly divided in two groups to find an alternative medication to epinephrine that would not result in secondary effects at the cardiovascular level but would offer a similar vasoconstricting capacity. Also, a variation of the wet technique is described that decreases blood loss secondary to liposuction. The area to undergo liposuction is infiltrated with a cannula of our own design. Epinephrine is not used as a vasoconstrictor but rather L-ornithine 8-vasopressin at a concentration of 0.01 IU/ml chilled saline. With this new technique, the amount of blood removed is minimal, even in the case of extraction of large volumes of fat.
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PMID:Effect of L-ornithine 8-vasopressin on blood loss during liposuction. 766 38

We report the solid-phase synthesis of the D-Cys6 analogues of arginine-vasopressin (AVP), peptide 1, of the selective AVP vasopressor (V1a receptor) antagonist [1-(beta-mercapto-beta,beta-pentamethylenepropionic acid),2-O-methyltyrosine]arginine-vasopressin (d(CH2)5[Tyr(Me)2]-AVP, (A)), peptide 2, of the three nonselective antidiuretic/vasopressor (V2/V1a receptor) AVP antagonists d(CH2)5[Tyr(Et)2]VAVP (B), d(CH2)5[D-Tyr(Et)2]VAVP (C), and d(CH2)5[D-Phe2]VAVP (D) (where V = Val4), peptides 3-5, of the nonselective oxytocin (OT) antagonists d(CH2)5-[Tyr(Me)2]OVT (E) and d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH2(9)]OVT (F) (where OVT = ornithine-vasotocin), peptides 6 and 7, and of the selective OT antagonists desGly-NH2,d(CH2)5[Tyr(Me)2,Thr4]OVT (G) and d(CH2)5]D-Trp2,Thr4]OVT (H), peptides 8 and 9. We also present the repeat syntheses of the previously reported d(CH2)5[D-Trp2]AVT (peptide 10) and its D-Cys6 analogue (peptide 11) (where AVT = arginine-vasotocin). Peptides 1-11 were assayed for agonistic and antagonistic activities in in vivo V1a, V2, and oxytocic assays and in in vitro oxytocic assays without and with 0.5 mM Mg2+. With V2 and V1a agonistic potencies of 0.82 and 0.41 units/mg, [D-Cys6]AVP has retained less than 0.3% of the V2 and V1a potencies of AVP. It exhibits no oxytocic activity and is an in vitro OT antagonist. pA2 = 6.67 (no Mg2+); pA2 = 5.24 (0.5 mM Mg2+). By contrast, with one or two exceptions, a D-Cys6/L-Cys6 interchange in antagonists 2-9, although resulting in reductions of antagonistic potencies in all assays for virtually all peptides 2-9 relative to A-H, has been well tolerated. For peptides 2-5, the anti-V2 and anti-V1a pA2 values range from approximately 5.54 to 7.33 and from 7.19 to 8.06, respectively; the range of in vitro anti-OT pA2 values (no Mg2+) is 7.35-7.87; with 0.5 mM Mg2+, the range is 7.24-8.21. Peptides 2 and 4 have in vivo anti-OT pA2s = 6.60 and 7.16, respectively. For peptides 6-9, the range of in vitro anti-OT pA2 values (no Mg2+) is 7.65-7.96; with 0.5 mM Mg2+, the range is 7.41-7.65, and the in vivo anti-OT pA2 values range from 6.85 to 7.33. With an in vivo anti-OT pA2 = 7.33, peptide 6 is equipotent with its parent E. The in vivo anti-OT potencies of peptides 7-9 are significantly reduced relative to those of F-H. The in vitro anti-OT (0.5 mM Mg2+) pA2 values of 10 and 11 are 7.54 and 7.50, both significantly lower than those previously reported.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Effects of a D-Cys6/L-Cys6 interchange in nonselective and selective vasopressin and oxytocin antagonists. 775 99

Cytosolic free calcium concentration ([Ca2+]i) was measured in single microdissected rat medullary collecting tubules [outer (OMCD) and inner (IMCD)] to identify receptors involved in vasopressin (AVP)-induced [Ca2+]i increases. In both segments, [Phe2,Orn8]vasotocin ([Phe2,Orn8]VT), a specific V1 agonist, as well as the V2 agonist 1-desamino-8-D-AVP (dDAVP) triggered [Ca2+]i variations. In OMCD, the mean response to 10 nM AVP roughly corresponded to the sum of V1 and V2 agonists effects. In IMCD, dDAVP (10 nM) alone reproduced the calcium response to AVP (delta[Ca2+]i = 243 +/- 34 nM, n = 6, and 248 +/- 27 nM, n = 8, with dDAVP and AVP, respectively). Furthermore, in the same experiments V1 and V2 maximal effects were not additive ([Phe2,Orn8]VT = 154 +/- 21 nM, n = 6; dDAVP + [Phe2,Orn8]VT = 233 +/- 23 nM, n = 9). As AVP, dDAVP released intracellular calcium (delta[Ca2+]i in calcium-free medium = 182 +/- 24 nM, n = 8, vs. 182 +/- 14 nM, n = 6 with 10 nM dDAVP and AVP, respectively). Neither 8-(4-chlorophenyl-thio)-adenosine 3',5'-cyclic monophosphate nor forskolin modified [Ca2+]i. A cross-reaction of dDAVP with an oxytocin (OT) receptor can be excluded since 1) the specific OT agonist [Thr4,Gly7]OT (10 nM) increased only slightly [Ca2+]i (delta-[Ca2+]i = 20 +/- 5 nM, n = 11); 2) the dDAVP response was not altered by the specific OT antagonist [1-(beta-mercapto-beta,beta-cyclopentamethylene propionic acid),2-(O-methyl)tyrosine,4-threonine, 8-ornithine,9-tyrosylamide]vasotocin [d(CH2)5(1),O-Me-Tyr2,Thr4,Tyr-NH2(9)]OVT; 3) it was insensitive to V1 antagonists but was totally blocked by the V1/V2 antagonist [d(CH2)5(1),O-Et-Tyr2,Val4]AVP ([delta[Ca2+]i = 18 +/- 4 nM, n = 6). These results indicate that in IMCD AVP increases [Ca2+]i via both V1 and V2 receptors. [Ca2+]i variations due to V2 receptors involve a mechanism independent of adenylate cyclase and coupled to the same intracellular calcium pool as V1 and V2 receptors.
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PMID:V2-like vasopressin receptor mobilizes intracellular Ca2+ in rat medullary collecting tubules. 834 13

The effects of electrical stimulation of the hypothalamus paraventricular nucleus on the spontaneous firing of mitral and granule cells in the main olfactory bulb were examined in ovariectomized female rats under urethane anaesthesia. High-frequency stimulation (0.5-1.0 mA, 10-20 pulses at 100 Hz) of the paraventricular nucleus produced inhibitory responses in 80% of mitral cells tested and excitatory responses in 74% of granule cells tested, with latencies ranging from 2 to 150 s. Both responses were blocked by infusions into the olfactory bulb of [d(CH2)5, Tyr(Me)2]ornithine-vasotocin (10 pmol), an oxytocin antagonist, and mimicked by intracerebroventricular infusions (0.2 or 0.4 nmol) or microiontophoretic applications of oxytocin but not by intracerebroventricular infusions of vasopressin (1 or 2 nmol). Infusions of 0.5% lignocaine, a local anaesthetic, into either the medial olfactory tract or the medial forebrain bundle failed to block the responses of mitral and granule cells to the stimulation. Unilateral transections at various levels between the bulb and the paraventricular nucleus also failed to block the responses. There were cases in which significant responses of mitral and granule cells to the stimulation required 60 or more pulses after the lignocaine infusions or transections, however. These results suggest that oxytocin originating in the hypothalamic paraventricular nucleus reaches the olfactory bulb following its release partly into the cerebrospinal fluid and acts to decrease olfactory processing.
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PMID:The action of oxytocin originating in the hypothalamic paraventricular nucleus on mitral and granule cells in the rat main olfactory bulb. 873 30

The affinity and specificity of an antagonist of oxytocin, [1-D(CH2)5,Tyr(ME)2,Thr4,Tyr-NH2(9)]ornithine vasotocin (OTA), to oxytocin receptors (OTR) in bovine gestational endometrium was determined in displacement experiments with oxytocin (OT) and vasopressin (AVP) analogues and compared to myometrial OTR. OTA had the highest affinity in both tissues. The effect of OTA on OT-induced increase in plasma concentration of 13,14-dihydro-15-keto-prostaglandin F2alpha metabolite (PGFM) was studied in 24 late-pregnant cows. Treatments consisted of i.v. saline; OT (50 IU); OTA (1200 microg); and OTA (400, 1200, or 4000 microg) injected i.v. 5 min before OT (50 IU) (n = 4 each). Samples were collected from jugular vein at 15-min intervals for 30 min before and 3 h after the injection of OT. Progesterone was measured in once-daily samples taken for 7 days after the experiment. OT caused a twofold increase in plasma PGFM within about 60 min (p < 0.005), with levels returning to baseline at 150-180 min; OTA (1200 microg) caused a gradual lowering of basal plasma PGFM over 180 min (p < 0.05). The 400-microg or 1200-microg dose of OTA did not alter OT-induced PGFM response, whereas the 4000-microg dose inhibited it almost completely (p < 0.005). Plasma progesterone declined after the experiment in all cows, with no differences among groups. Because OTA inhibits OT-induced release of endometrial prostaglandin F2alpha it may be a good tocolytic agent.
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PMID:Oxytocin antagonist [1-D(CH2)5,Tyr(ME)2,Thr4,Tyr-NH2(9)]ornithine vasotocin inhibits oxytocin-induced prostaglandin F2alpha release in late-pregnant cows. 924 Oct 61


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