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

A diuretic effect of the pentapeptide BW942C [Tyr-D-Met(O)-Gly-pNO2-Phe-Pro-NH2 HCl] was demonstrated in humans and rats; it was characterized pharmacologically using whole animal, isolated tissue and in vitro binding studies. A single 2-mg dose of BW942C increased urine output 5-fold over control values in humans. In Long-Evans rats, BW942C produced a biphasic dose-response curve for urine output with lower doses increasing and higher doses suppressing output. Low doses of naltrexone antagonized the antidiuresis, and high doses antagonized the diuresis produced by BW942C. BW942C was less efficacious in producing diuresis than the full kappa agonists bremazocine and U50,488H (trans-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]- benzeneacetamide methanesulfonate, hydrate). Furthermore, BW942C antagonized the diuretic effects of bremazocine and U50,488H. Rats tolerant to U50,488H-induced diuresis were cross-tolerant to BW942C. In Brattleboro rats, which are unable to synthesize vasopressin, BW942C failed to produce a diuretic effect, demonstrating the necessity of vasopressin for its diuretic response. In the kappa-selective rabbit vas deferens bioassay, BW942C was less efficacious than a full agonist, it was antagonized by naloxone and BW942C in nondepressant doses antagonized a full agonist. In binding studies, BW942C had the highest affinity for mu and delta opioid receptors and an intermediate affinity for kappa opioid receptors. The data suggest that BW942C has the property of a partial kappa opioid agonist in addition to being a mu agonist.
 ...
PMID:Kappa opioid partial agonist activity of the enkephalin-like pentapeptide BW942C based on urination and in vitro studies in humans and animals. 215 1

A convergent synthesis of the peptide [1-(beta-mercapto-beta, beta-cyclopentamethylenepropionic acid)- 2-(O-ethyl-D-tyrosine)-4-valine-9-desglycine]arginine vasopressin (1), based on the classical solution phase method, was developed. The molecule is assembled by a 3 + 4 coupling via the azide method; then the disulfide bridge is installed by iodine treatment of the bis-acetamidomethyl protected thiols, and the terminal arginine amide added by a 7 + 1 coupling. The method has been used to prepare gram quantities of 1 in more than 98% purity and in 13% yield (based on tetrapeptide intermediate 13) after a single stage purification. The method appears to be particularly suitable for the large scale preparation of 1 and other vasopressin congeners. A novel, albeit low level, transfer of acetamidomethyl group from the sulfur of cysteine to the asparagine amide side-chain was detected following hydrogen chloride treatment of Boc-containing intermediates.
 ...
PMID:Efficient solution phase synthesis of [1-(beta-mercapto-beta, beta-cyclopentamethylenepropionic acid)- 2-(O-ethyl-D-tyrosine)-4-valine-9-desglycine]arginine vasopressin. 235 76

A bland procedure, conducted in ice, is described for the extraction with HCl of smooth-muscle-contracting substances from plexus-containing ileal longitudinal muscle (l.m.) sheets obtained mainly from rabbits and some guinea-pigs. The spasmogenic activity in rabbit extracts was distinguished from acetylcholine, histamine and 5-hydroxytryptamine by antagonists; and from prostaglandins, by its insolubility in ether at acid pH and by pretreatment of the animals with indomethacin. The fact that it contracts the separated l.m. of the guinea-pig ileum, whether plexus-containing or plexus-free, and in atropine distinguishes it also from methionine-enkephalin, somatostatin, 13-norleucine motilin, bombesin, and cholecystokinin octapeptide (CCK8). This activity was partially purified, first by several partitions with ether at pH 1.4-2.2 and then by treatment at pH 4.5-5 with lead acetate. The virtual absence of ATP was confirmed by the firefly bioluminescence technique. The guinea-pig-ileum-contracting component in the partially purified extracts was destroyed by pepsin, chymotrypsin and DPCC-treated trypsin, indicating its peptide nature and distinguishing it from oxytocin, vasopressin, bradykinin, etc. In parallel assays the partially purified rabbit extracts were considerably more active than Substance P on jird or rat ascending colons than on the guinea-pig l.m., suggesting the presence of a second spasmogenic component in the extracts. In guinea-pig extracts the partially purified activity was 8-16 times greater when plexus-containing than when plexus-free, pointing to Auerbach's plexus as the source of the activity.
 ...
PMID:Extraction and partial purification of spasmogenic substances in Auerbach's plexus. 242 21

Since the first paravertebral blockade was carried out by Sellheim in 1905, this method has proved effective for the isolated blockade of spinal nerves. The efficacy of preoperative intercostal blockade (ICB) in combination with neuroleptanalgesia (NLA) or Pentothal-pentazocine-N2O anesthesia (Pe-Pz) was studied (unilateral analgesia for cholecystectomy). Group 1: NLA; group 2: NLA with ICB; group 3: Pe-Pz; group 4: Pe-Pz with ICB. The analgesic requirement differed significantly between groups 1 (0.33 mg fentanyl) and 2 (0.15 mg fentanyl) and groups 3 (63.5 mg pentazocine) and 4 (31.5 mg pentazocine). There were also significant differences in circulatory responses. The maximum deviation from the initial value at the beginning of the operation in group 1 compared to group 2 was pulse rate + 28.7% vs + 2.4%, mean arterial pressure (Part) + 24.6% vs + 3.1%, and systolic pressure (Psyst) + 33% vs +/- 0%; group 3 compared to group 4: pulse rate + 16.4% vs + 3.2%, Part + 24.5% vs 0.0%, and Psyst + 26.5% vs + 196. The times of action of ICB extended from 7.54 h to 11.33 h for partial analgeisa, time to the first dose of analgesic from 12.3 h to 16.9 h (etidocaine 0.5% and 1% respectively without and with epinephrine). The mean blood levels after 100 mg bupivacaine-CO2 rose to 1.16 micrograms/ml after 5 min and reached a maximum after 15 min (1.29 micrograms/ml) as compared to 0.98 micrograms/ml after addition of ornithine-vasopressin. These values are very much higher than those after the use of bupivacaine-HCl solution. Etidocaine and bupivacaine-HCl have comparable durations of analgesia. Toxicologically, both substances can be applied safely with consideration of all pharmacological data for ICB. Of a total of 3,485 intercostal blockades, 2,775 were applied perioperatively (pre- and postoperatively); 265 were carried out for trauma patients (rib fractures) and 445 for therapeutic indications (herpes zoster neuralgia, tumor pain, costovertebral pain). In 8 blocks 10% ammonium sulfate, in 4 blocks absolute alcohol, and in 19 blocks 5% phenol were used for neurolysis. In 2 cases a marginal pneumothorax was seen, which was resorbed spontaneously (0.06%). Altogether 16,270 single intercostal nerves were blocked. Single-session intercostal blockade can be combined as unilateral analgesia with general anesthesia. This combination is characterized by stable circulatory conditions with avoidance of hypertensive reactions. The long-lasting analgesia allows early mobilization and physiotherapy both postoperatively and posttraumatically in patients with unilateral thoracic and abdominal pain.(ABSTRACT TRUNCATED AT 400 WORDS)
 ...
PMID:[The single intercostal block--surgical and therapeutic indications]. 264 21

In animal experiments, an in vivo comparison was made of the alkaline secretion (AS) of the duodenal mucosa and of its ability to defend against hydrochloric acid. An i.v. infusion of NaHCO3 and glucagon was applied to stimulate AS, and one of NH4Cl, vasopressin and furosemide to depress it. In the stage of AS influenced via various mechanisms and to different extents, the luminal surface of the duodenum was exposed with HCl. The extent of mucosal damage was determined by quantitative morphometry. The mucosa-damaging effect of standardized HCl-exposure was significantly lower in the stage of enhanced AS than in the control experiments. In contrast, during inhibition of AS hydrochloric acid caused more extensive and deeper mucosal damage. A linear correlation was observed between the degree of AS of the duodenum and the proportion of damaged intestinal villi. In the opinion of the authors, inhibition of the As of the duodenum is accompanied by a decreased acid tolerance of the mucosa, while its stimulation enhances the ability of the mucosa to defend against hydrochloric acid.
 ...
PMID:[The role of alkaline secretion of the duodenal mucosa in protecting the mucosa from hydrochloric acid]. 277 84

A human plasma CRH-binding protein (CRH-BP) was identified and characterized by chemical cross-linking of 125I-Tyr-hCRH to human plasma using disuccinimidyl suberate. The apparent mol wt of the cross-linked complex determined by sodium dodecyl sulfate-polyacrylamide gel electrophoresis followed by autoradiography was approximately 43,000. The mol wt was slightly lower in the nonreduced state, suggesting the presence of intramolecular disulfide bonds. Subtracting the mol wt of 125I-Tyr-CRH, the BP appeared to have a mol wt of approximately 38,000. Binding was specific since the appearance of the 43,000 dalton band was not affected by unlabeled ACTH, vasopressin, serum albumin, or gamma-globulin, but was inhibited by unlabeled hCRH dose dependently. Pretreatment of plasma with 0.1 mol/L HCl, 0.01 mol/L NaOH, 10 mmol/L dithiothreitol, or trypsin before cross-linking abolished its ability to bind 125I-Tyr-hCRH. Rat, rabbit, or goat plasma or human cerebrospinal fluid did not bind 125I-Tyr-CRH. It is unlikely that CRH-BP is a CRH receptor, because the estimated mol wt of the CRH-BP is smaller than the reported size of CRH receptors, and the CRH-BP did not bind to ovine CRH. The binding of 125I-Tyr-CRH to CRH-BP decreased in the third trimester of pregnancy, when plasma CRH levels were markedly elevated. However, after dissociating endogenous CRH from the CRH-BP, the binding was almost the same as in nonpregnant subjects. In addition, CRH-BP inhibited CRH-induced ACTH secretion from cultured rat anterior pituitary cells. We conclude that most of the increased plasma CRH found in pregnant women is bound to CRH-BP, and so is inactive, therefore plasma ACTH levels do not increase to above the normal range.
 ...
PMID:Characterization of corticotropin-releasing hormone binding protein in human plasma by chemical cross-linking and its binding during pregnancy. 284 56

In addition to its peripheral endocrine actions, arginine vasopressin (AVP) has been implicated in the central control of blood pressure. Intracerebroventricular (i.c.v.) injections (0.01-1.0 nmol) of AVP or arginine vasotocin (AVT), but not oxytocin (OXY), into unanesthetized rabbits caused a rapid, dose related rise in blood pressure as well as increases in heart rate. The lowest centrally administered dose of AVP and AVT (0.01 nmol) had no effect on blood pressure when given intravenously. In search of tissue locus for the pressor effect of AVP microinjection of AVP and OXY into the posterior hypothalamus and septum of conscious rabbits was without effect. However, microinjection (0.01-0.04 nmol) of AVP into the nucleus tractus solitarius of anesthetized rabbits caused a rise in blood pressure similar to the response seen after i.c.v. injection. Comparable volumes of the vehicle into the ventricle or the tissue sites had no effect on resting blood pressure. The pressor response after AVP given i.c.v. was significantly reduced up to 3 h after administration of the ganglionic blocker, chlorisondamine HCl. The central antagonist, d(CH2)5Tyr (Me) vasopressin, eliminated the usual increase in blood pressure after administration of AVP in half the animals tested. The results indicate that AVP acts centrally to mediate cardiovascular responses in unanesthetized as well as anesthetized rabbits.
 ...
PMID:The action of centrally administered arginine vasopressin on blood pressure in the conscious rabbit. 293 25

The intraperitoneal (i.p.) injection of ACTH 1-24 (0.2 microgram/kg), lysine--vasopressin (10.0 micrograms/kg) or epinephrine HCl (5.0 micrograms/kg) shortly after training or prior to testing caused memory facilitation of a step-down inhibitory avoidance task in rats, acquired with low intensity training footshocks (0.3 mA, 60 Hz). Naloxone HCl (0.4 mg/kg) potentiated their posttraining effect, but antagonized their pre-test effect. Naloxone on its own caused retrograde memory facilitation but had no effect on the test session. Posttraining human beta-endorphin (1.0 microgram/kg) was amnestic, and its pre-test administration enhanced retention. Both effects were naloxone-reversible. Neither the pre-test facilitation caused by beta-endorphin nor those caused by any of the other drugs (which are possible releasers of endogenous beta-endorphin) were observed in animals in which the influence of endogenous opioids was prevented at the posttraining period by the administration of naloxone. These results are compatible with, and considerably strengthen, the previously advanced hypothesis that learning of this task, and possibly others, depends on a state induced by beta-endorphin after training, and that it would normally be dissociated because this peptide is normally not released during test sessions. In addition, the posttraining facilitation caused by ACTH, vasopressin, and epinephrine stands out as an effect separate from, and in fact normally hindered by, posttraining beta-endorphin release.
 ...
PMID:Influence on memory of posttraining or pre-test injections of ACTH, vasopressin, epinephrine, and beta-endorphin, and their interaction with naloxone. 299 40

Oxytocin (OT) and vasopressin (VP) have been localized in various sites within the central nervous system outside the classic hypothalamo-neurohypophyseal axis. This study investigated the effect of immobilization stress on the levels of OT and VP in the hypothalamus, pons-medulla, and the cervical, thoracic, and lumbosacral segments of the spinal cord. Male Long Evans rats were immobilized for 1 min and sacrificed by guillotine. The tissues were dissected out and homogenized in 0.1 N HCl. The hormone content was determined by radioimmunoassay (RIA) in Sep-pak extracted samples. The data show a decrease in OT content of 33.6% (P less than 0.02) and 42.4% (P less than 0.01) in the hypothalamus and pons-medulla, respectively. In the spinal cord, however, OT levels were increased by 39.1% (not significant), 51.1% (P less than 0.05), and 87.6% (P less than 0.001) in the cervical, thoracic, and lumbosacral segments respectively. The VP content of the hypothalamus and pons-medulla did not change. However, in the spinal cord, the VP content was also increased by 101.4% (P less than 0.01) and by 143.7% (P less than 0.01) in the cervical and lumbosacral segments. The levels of VP in the thoracic segment did not change. The data demonstrate that stress can alter hypothalamic and extra-hypothalamic levels of OT as well as spinal cord levels of VP. The exact physiological effects of these changes, particularly within the spinal cord, remain to be elucidated.
 ...
PMID:Immobilization stress affects oxytocin and vasopressin levels in hypothalamic and extrahypothalamic sites. 320 93

Like many other neuropeptides, vasopressin is not confined to the hypothalamic neurohypophysial system. Furthermore, vasopressin was found to be a potent vasoconstrictor in the rat jejunum, reducing myenteric artery flow. These associations were the basis of this investigation on the presence of vasopressin in the gastrointestinal (GI) tract by both RIA and immunohistochemistry. Portions of the gastrointestinal tract and pancreatic islets of the rat were extracted with 0.1 N HCl for RIA measurements of AVP content. Similar portions from the male cat GI tract were used for immunohistochemistry studies. Acid extracts of the GI tract were found to contain immunoreactive AVP with the highest concentration (pg/mg protein) in the fundus portion of the stomach (15.0 +/- 1.6) and slightly lower values down along the antrum-pylorus portion (6.7 +/- 0.6), proximal jejunum (8.6 +/- 0.2), distal ileum (9.7 +/- 0.3) and colon (11.9 +/- 0.5). In the pancreatic islets the concentration was much higher (72.0 pg/mg protein). The extract inhibition curves showed parallelism with the appropriate standard preparation of AVP in the specific RIA. Immunohistochemical localization showed IR-AVP in the nerve fibers around the myenteric plexus of the second portion of the duodenum. It was also found in fibers starting from where the myenteric plexus goes through the layer of muscle fibers, penetrating the submucosa and duodenal mucosa, ending near the capillaries situated along the basal side of the villous epithelium cells. Similar IR-AVP activity was found in cells located in the mucosal epithelium of the duodenum, jejunum, ileum, colon and rectum.(ABSTRACT TRUNCATED AT 250 WORDS)
 ...
PMID:Arginine-vasopressin immunoreactive material in the gastrointestinal tract. 353 11


<< Previous 1 2 3 4 5 6 Next >>