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 35-year-old man with refractory low grade diffuse centroblastic centrocytic non-Hodgkin's lymphoma was treated accidentally with an overdose of multiple chemotherapeutic agents. He was given adriamycin 50 mg/m2 and cyclophosphamide 350 mg/m2 for 6 days followed by 4 days of vincristine 1 mg/m2 and bleomycin 10 mg/m2. He was transferred when he developed pancytopenia, fever, severe mucositis, ileus and peripheral neuropathy. He was treated with broad spectrum antibiotics, red cell and single donor platelet transfusions and strict parenteral nutrition. In addition, he was given a continuous infusion of 400 micrograms daily human recombinant granulocyte macrophage-colony stimulating factor (rh GM-CSF) for 17 days. Intractable severe bleeding from his oral mucositis necessitated treatment with a continuous infusion of 8-ornithine-vasopressin for 8 days. He recovered and could be discharged home after 36 days of hospitalization with normal blood counts and without severe sequelae.
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PMID:Accidental overdose of multiple chemotherapeutic agents. 248 48

Optimized C18 reversed-phase systems for oxytocin, desamino-oxytocin, lysine-vasopressin, ornithine-vasopressin and felypressin with gradient elution are discussed, focussing on precision, selectivity and ruggedness of the methods. Data from collaborative studies are presented, demonstrating the equivalence of high-performance liquid chromatography (HPLC) assays to bioassays. The findings suggest that HPLC is an excellent alternative to the time-consuming and less reliable animal testing.
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PMID:The use of high-performance liquid chromatography in the quality control of oxytocin, vasopressin and synthetic analogues. 248 22

The first case of tubal desterilization after Yoon rings through exclusive laparoscopy is reported. Yoon ring tubal segment excision was performed with CO2 laser and coelioscopic scissors, after mesosalpinx haemostasis by ornithine--vasopressin infiltration. Tubal anastomosis was managed with biological glue on an intraluminal guide which was pulled out after 48 h. Follow-up hysterosalpingography 3 months later showed perfect tubal patency. This case proves that complete tubal reversal by exclusive coelioscopy is possible. At present, this procedure is restricted to only one tube during coelioscopic evaluation, preserving, in case of failure, the chance of microsurgery either on the contralateral tube or even on the previously operated one. The advantages of such a technique are those of coeliosurgery: no laparotomy, shortened hospitalization and minimal post-operative adhesions. Since this first case, others have been performed. It is still too early to appreciate the results in terms of intrauterine pregnancy.
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PMID:Tubal desterilization through exclusive laparoscopy. 252 64

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)
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PMID:[The single intercostal block--surgical and therapeutic indications]. 264 21

Excision and skin grafting is the best treatment for burn wounds. In order to avoid excessive bleeding during the operation, sub-eschar infiltration with POR 8 (para ornithine 8 - vasopressin) has been performed in 115 patients between 1979 and 1984. The results being encouraging, infiltration was later also performed under the donor site. Bleeding was reduced enough by this technique to allow one stage excision and grafting of surfaces up to 20% of the body surface. No general or local complication of POR 8 infiltrations has been observed except a slight increase of blood pressure without clinical consequence.
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PMID:[Value of POR 8 in the treatment of burns]. 266 63

An oxytocic antagonist, [1-(beta-mercapto-beta, beta-cyclopentamethylenepropionic acid,2-O-methyltyrosine,4-threonine, 8-ornithine,9-tyrosylamide]vasotocin (d(CH2)5[Tyr(Me)2, Thr4,Tyr-NH2(9)]OVT [corrected], was monoiodinated at the phenyl moiety of the tyrosylamide residue at position 9. 125I-labelling was performed with 1,3,4,6-tetrachloro-3 alpha,6 alpha-diphenyl-glycoluril. Iodination resulted in an increased affinity for rat uterine oxytocin receptors. A considerably lower affinity for rat vascular V1- and renal V2-receptors was found, resulting in a highly specific oxytocin receptor ligand. 125I-labelled d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH2(9)]OVT [corrected] was demonstrated to bind selectively to one population of binding sites in rat uterus and ventral hippocampal membrane preparations. Dissociation constants ranged between 0.03 and 0.06 nM. After 3 days of exposure autoradiography revealed binding in regions known to contain oxytocin receptors as well as labelling in some new regions, while no binding was found in the lateral septum, a structure containing mainly [8-arginine]vasopressin receptors. The high specific radioactivity of 125I-labelling allowed important reductions in membrane protein amount, gain in precision of binding analysis as well as considerably lower exposure times for autoradiography.
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PMID:125I-labelled d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH2(9)]OVT: a selective oxytocin receptor ligand. 283 49

A new, highly selective radio-iodinated oxytocin receptor antagonist [( 1-(beta-mercapto-beta, beta-cyclopentamethylenepropionic acid, 2-O-methyltyrosine, 4-threonine, 8-ornithine, 9-tyrosylamide]-vasotocin) was used to identify and quantitate specific binding sites for the neurohypophyseal hormone oxytocin with in vitro incubation of rat brain sections and autoradiography. Exclusively oxytocin binding sites were detected in view of the high affinity of the [125I]-labelled oxytocin antagonist for oxytocin binding sites and the negligible affinity for the vasopressin liver (V1) and kidney (V2) receptor types. The putative oxytocin receptors were abundantly present in several brain regions, where previously discrimination between oxytocin and vasopressin binding was difficult, i.e. the olfactory nucleus, the islands of Calleja, the ventromedial nucleus of the hypothalamus, the central amygdaloid nucleus and the ventral subiculum of the hippocampus. In addition oxytocin receptors were demonstrated in other areas, such as the taenia tecta, dorsolateral caudate putamen, ventral pallidum, accumbens, lateral septum, bed nucleus of the stria terminalis, thalamic paraventricular nucleus, lateral, basolateral and medial amygdala, the dorsal subiculum, perirhinal cortex and the amygdaloid-hippocampal area. The high affinity and the low detection threshold of this [125I]-labelled oxytocin antagonist permitted identification of oxytocin receptors in new regions such as the ventral part of the lateral septum, medial septum, dorsal motor nucleus of the vagus nerve and the olive nuclei in the brain stem.
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PMID:Topography of the oxytocin receptor system in rat brain: an autoradiographical study with a selective radioiodinated oxytocin antagonist. 285 12

The sensitivity of the mouse anococcygeus to contraction by oxytocin was shown to be Mg2+-dependent. Decreasing [Mg2+]0 from the optimal concentration of 1 to 0 mM caused a 20-fold parallel rightward displacement of the oxytocin dose-response curve. Contractions to oxytocin-related peptides (Arg-vasotocin, Arg-vasopressin and Lys-vasopressin) were also Mg2+-dependent, but those to other drugs (carbachol, methoxamine and thyrotrophin releasing hormone) were not. The onset of the potentiating effect of Mg2+ was rapid, full potentiation occurring within 70 s. 1-Deaminopenicillamine 8-ornithine-vasotocin produced competitive antagonism of responses to oxytocin, but was more potent in the absence (pA2 = 8.01) than in the presence of Mg2+ (1 mM; pA2 = 7.52). Thus, physiological concentrations of [Mg2+]0 enhanced oxytocin agonist potency but decreased oxytocin antagonist potency; possible mechanisms are discussed.
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PMID:Magnesium ions and oxytocin sensitivity of the male mouse anococcygeus. 286 97

We describe the synthesis and some pharmacological properties of 16 new in vivo antagonists of oxytocin. These are based on modifications of three peptides: A, B, and C. A is our previously reported potent and selective antagonist of the vasopressor (V1 receptor) responses to arginine-vasopressin (AVP)/weak oxytocin antagonist, [1-(beta-mercapto-beta,beta-pentamethylenepropionic acid), 2-O-methyltyrosine]arginine-vasopressin (d(CH2)5[Tyr(Me)2]AVP. B reported here, the Ile3 analogue of A, is d(CH2)5[Tyr(Me)2]AVT (5 below) and C is our previously reported potent nonselective oxytocin antagonist/AVP V1 antagonist, [1-(beta-mercapto-beta,beta-pentamethylenepropionic acid),2-O- methyltyrosine,8-ornithine]vasotocin (d(CH2)5[Tyr(Me)2]OVT). The following substitutions and deletions, alone or in combination, were employed in A, B, and C: 1-deaminopenicillamine (dP); D-Tyr(Alk)2 (where Alk = Me or Et), D-Phe2; Val4, Thr4; delta 3-Pro7; Lys8, Cit8; desGly9, desGly-NH2(9), Ala-NH2(9); Leu-NH2(9); Arg-NH2(9). The 16 new analogues are (1) d(CH2)5[D-Tyr(Me)2]AVP, (2) d(CH2)5[D-Tyr(Me)2, Val4,delta 3-Pro7]AVP, (3) d(CH2)5[D-Tyr-(Et)2, Val4,Lys8]VP, (4) d(CH2)5[D-Tyr(Et)2,Val4,Cit8]VP, (5) d(CH2)5[Tyr(Me)2]AVT, (6) d(CH2)5[Tyr(Me)2,Lys8]VT, (7) dP[Tyr(Me)2]AVT, (8) dP[Tyr(Me)2,Val4]AVT, (9) d(CH2)5[D-Tyr(Me)2, Val4]AVT, (10) d(CH2)5[D-Phe2,Val4]AVT, (11) d(CH2)5[Tyr(Me)2,Thr4]OVT, (12) d(CH2)5[Tyr(Me)2,Thr4,Ala-NH2(9)]OVT, (13) d(CH2)5[Tyr(Me)2,Thr4,Leu-NH2(9)]OVT, (14) d(CH2)5[Tyr(Me)2,Thr4,Arg-NH2(9)]OVT, (15) desGly-NH2(9),d(CH2)5[Tyr(Me)2,Thr4]OVT, (16) desGly9,d(CH2)5[Tyr(Me)2,Thr4]OVT. 1-4 are analogues of A, 5-10 are analogues of B, and 11-16 are analogues of C. Their protected precursors were synthesized either entirely by the solid-phase method or by a combination of solid-phase and solution methods (1 + 8 or 8 + 1 couplings). All analogues were tested in rats for agonistic and antagonistic activities in oxytocic (in vitro, without and with Mg2+, and in vivo) assays as well as by antidiuretic and vasopressor assays. All analogues exhibit potent oxytocic antagonism in vitro and in vivo. With an in vitro pA2 (in the absence of Mg2+) = 9.12 +/- 0.09, dP[Tyr(Me)2]AVT is (7) one of the most potent in vitro oxytocin antagonists reported to date. Fifteen of these analogues (all but 6) appear as potent or more potent in vivo oxytocin antagonists than C (pA2 = 7.37 +/- 0.17). Analogues 1-9 and 14 are potent AVP V1 antagonists. Their anti-V1 pA2 values range from 7.92 to 8.45. They are thus nonselective oxytocin antagonists.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Solid-phase synthesis of 16 potent (selective and nonselective) in vivo antagonists of oxytocin. 291 98

A bilateral cleft lip and palate case received ornithine-vasopressin intra-operatively in preparation for a vasoconstricted field of the various lip segments prior to the repair of the cleft lip. A cyanotic tinge appeared immediately. This eventually led to total necrosis of the upper lip. Various relevant blood tests were done and a mild thrombocytosis was found. Surgical reconstruction of the upper lip was performed by means of a forked cross-lip flap--the main blood supply coming from the columella--as well as by means of an inferiorly pedicled cheek flap from the para-nasal area.
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PMID:Ornithine-vasopressin gangrene and reconstruction of the upper lip. Case report. 292 34


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