TY - JOUR. T1 - The selective vasopressin type 1a receptor agonist selepressin (FE 202158) blocks vascular leak in ovine severe sepsis. AU - Maybauer, Marc O.. AU - Maybauer, Dirk M.. AU - Enkhbaatar, Perenlei. AU - Laporte, Régent. AU - Winiewska, Halina. AU - Traber, Lillian D.. AU - Lin, Chiidean. AU - Fan, Juanjuan. AU - Hawkins, Hal K.. AU - Cox, Robert A.. AU - Winiewski, Kazimierz. AU - Schteingart, Claudio D.. AU - Landry, Donald W.. AU - Rivière, Pierre J M. AU - Traber, Daniel L.. PY - 2014. Y1 - 2014. N2 - OBJECTIVE:: To determine if the selective vasopressin type 1a receptor agonist selepressin (FE 202158) is as effective as the mixed vasopressin type 1a receptor/vasopressin V2 receptor agonist vasopressor hormone arginine vasopressin when used as a titrated first-line vasopressor therapy in an ovine model of Pseudomonas aeruginosa pneumonia-induced severe sepsis. DESIGN:: Prospective, randomized, controlled laboratory experiment. SETTING:: University animal research facility. ...
Title: Specificity of Three Vasopressin Receptor Antagonists. VOLUME: 8 ISSUE: 6. Author(s):Jeremy T. Saks, Barbara Truitt and Menachem Shoham. Affiliation:Case Western Reserve University, School of Medicine, Department of Biochemistry, 10900 Euclid Ave, Cleveland, OH 44106-4935, USA.. Keywords:Antagonist, GPCR, Receptor, Mozavaptan, Tolvaptan, Vaptan, Vasopressin, arginine vasopressin (AVP), hV1R, vasodilation, hyponatremia, hypervolemia, V2R, adenylyl cyclase. Abstract: Vasopressin receptor antagonists (vaptans) are a new class of drugs to treat congestive heart failure. Since there are three subtypes of the receptor located in different tissues, it is important to devise tailor-made vaptans to target the appropriate receptor subtype. The binding of three vaptans, OPC21268, mozavaptan and tolvapatan was measured to the human V1-vascular vasopressin receptor (hV1R). Whereas arginine vasopressin (AVP) binds to hV1R and hV2R with equal affinity, vaptans interact differently with the receptor ...
Abstract: We examined the extent to which the arginine vasopressin receptor 1a (AVPR1a) and dopamine receptor D4 (DRD4) were related to sensitive maternal behavior directly or indirectly via maternal social cognition. Participants were 207 (105 European-American and 102 African-American) mothers and their children (52% females). Sensitive maternal behavior was rated and aggregated across a series of tasks when infants were 6 months, 1 year and 2 years old. At 6 months, mothers were interviewed about their empathy, attributions about infant behavior and beliefs about crying to assess their parenting-related social cognition. Mothers with long alleles for AVPR1a and DRD4 engaged in more mother-oriented social cognition (i.e. negative attributions and beliefs about their infants crying, ß = 0.13, P < 0.05 and ß = 0.16, P < 0.05, respectively), which in turn predicted less sensitive maternal behavior (ß = -0.23, P < 0.01). Both indirect effects were statistically significant independent of one ...
Abstract: We examined the extent to which the arginine vasopressin receptor 1a (AVPR1a) and dopamine receptor D4 (DRD4) were related to sensitive maternal behavior directly or indirectly via maternal social cognition. Participants were 207 (105 European-American and 102 African-American) mothers and their children (52% females). Sensitive maternal behavior was rated and aggregated across a series of tasks when infants were 6 months, 1 year and 2 years old. At 6 months, mothers were interviewed about their empathy, attributions about infant behavior and beliefs about crying to assess their parenting-related social cognition. Mothers with long alleles for AVPR1a and DRD4 engaged in more mother-oriented social cognition (i.e. negative attributions and beliefs about their infants crying, ß = 0.13, P < 0.05 and ß = 0.16, P < 0.05, respectively), which in turn predicted less sensitive maternal behavior (ß = -0.23, P < 0.01). Both indirect effects were statistically significant independent of one ...
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Twenty-one non-peptide substituted desloratadine class compounds were synthesized as novel arginine vasopressin receptor antagonists from desloratadine via successive acylation, reduction and acylation reactions. Their structures were characterized by 1H-NMR and HRMS, their biological activity was evaluated by in vitro and in vivo studies. The in vitro binding assay and cAMP accumulation assay indicated that these compounds are potent selective V2 receptor antagonists. Among them compounds 1n, 1t and 1v exhibited both high affinity and promising selectivity for V2 receptors. The in vivo diuretic assay demonstrated that 1t presented remarkable diuretic activity. In conclusion, 1t is a potent novel AVP V2 receptor antagonist candidate.
Although many signalling molecules appear relevant to the production of complex behaviours, those that are important to the physiological regulation of behaviour, and so those that characterise individual styles of behaviour, are unknown. Vasopressin is the strongest candidate regulator of social behaviour. Experiments were carried out in consideration that vasopressin may directly regulate aggressive behaviour in lactating rats. Patterns of immediate early gene expression during/subsequent to aggressive behaviour suggested specific neural circuits may have significant direct regulatory influence over particular behaviours, and that activation of the V1b vasopressin receptor, in these circuits, may contribute to this putative regulatory signalling. In situ hybridisation studies indicated that patterns of vasopressin release, rather than receptor expression, might be important for any peripartum changes in behaviour driven by vasopressin. Although their relative importance is unknown, central ...
Human Arginine Vasopressin Receptor V1B (AVPR1B) is one of the three major receptor types for vasopressin (AVPR1A and AVPR2 being the others).
Background: We had previously shown that vasopressin levels rise by 100-fold with fetal bypass, suggesting a possible role in rising placental vascular resistance seen with fetal cardiac surgery. To test our hypothesis that vasopressin may play a central role in placental dysfunction following fetal bypass, we carried out isolated vessel bath studies with placental vasculature, using vasopressin and selective vasopressin receptor antagonism (V1-a).. Methods: Adult rat aortas (controls) and fourth order ovine placental vessels were harvested and 5 mm rings mounted in temperature controlled aerated Radnoti vessel baths with continuous isometric tension measurement and recording. All vessels were tested with phenylephrine and acetylcholine to demonstrate viability of endothelium and baseline vascular smooth muscle responses. Placental vessels (n=6) and rat aortas (n=8) were exposed to log doses of vasopressin (10−11 to 10−7 g/mL). Placental vessels (n=5) and rat aortas (n=4) were treated with ...
Argipressin binds to the V1, V2, V3-vascular arginine vasopressin receptor, with a Kd value of 1.31 nM in A7r5 rat aortic smooth muscle cells for V1. Argipressin is a selective V2 agonist. - Mechanism of Action & Protocol.
Central arginine vasopressin receptor 1A (AVPR1A) modulates a wide range of behaviors, including stress management and territorial aggression, as well as social bonding and recognition. Inter- and intra-species variations in the expression pattern of AVPR1A in the brain and downstream differential behavioral phenotypes have been attributed to differences in the non-coding regions of the AVPR1A gene, including polymorphic elements within upstream regulatory areas. Gene association studies have suggested a link between AVPR1A polymorphisms and autism, and AVPR1A has emerged as a potential pharmacological target for treatment of social cognitive impairments and mood and anxiety disorders. To further investigate the genetic mechanism giving rise to species differences in AVPR1A expression patterns and associated social behaviors, and to create a preclinical mouse model useful for screening drugs targeting AVPR1A, we engineered and extensively characterized bacterial artificial chromosome (BAC) ...
PMID 25016245] Association between the arginine vasopressin receptor 1A (AVPR1A) gene and preschoolers executive functioning ...
AVPR1B antibody (arginine vasopressin receptor 1B) for IHC-P. Anti-AVPR1B pAb (GTX78015) is tested in Human samples. 100% Ab-Assurance.
AVPR1B antibody (arginine vasopressin receptor 1B) for IHC-P. Anti-AVPR1B pAb (GTX70663) is tested in Human samples. 100% Ab-Assurance.
We used an A10 rat vascular smooth muscle cell line to examine the regulation of the V1a receptor gene by glucocorticoids. A10 cells express a high density of V1a receptors and are well known as an ideal cell line for the study of vascular type V1a receptor regulation.9 10 Incubation of A10 cells with a glucocorticoid resulted in a marked increase in the V1a receptor protein, in agreement with a previous observation obtained in rat mammary tumor cells.22 In the present study we found that the A10 cells contain three different sizes of V1a receptor mRNA and that glucocorticoid upregulates each of these mRNAs. This change in mRNA expression was due to an increase in mRNA stability rather than an elevated transcription rate. Morel et al17 showed that a single signal of 2.1-kb mRNA was exclusively expressed in rat liver, kidneys, spleen, and testis; they did not report the expression profile in A10 cells. Three different sizes of V1a receptor mRNA were evident after washing at a high stringency and ...
Fast, simple luminescent calcium flux assays using an AequoScreen cell line stably-transfected with human vasopressin V2 receptor.
In this study, we demonstrate that selective pharmacological inhibition of AVP V1a receptors after SAH reduces the posthemorrhagic increase in systemic blood pressure (Cushing response), thereby attenuating the primary bleeding and preventing the detrimental effect of rebleedings. As a result, brain edema formation is blunted, mortality is reduced from 50% to 20%, and animals have a better functional outcome.. Our data indicate that the underlying mechanism of this finding is the involvement of AVP and AVP V1a receptors in the ICP-induced increase in systemic blood pressure (Cushing reflex) immediately after SAH. A sharp increase in ICP triggers the release of AVP into the bloodstream; consecutive activation of vascular V1a receptors results in systemic arterial constriction and a subsequent hypertensive response, which exacerbates SAH and potential rebleedings. Inhibition of AVP V1a receptors blunts the Cushing response, thereby resulting in less severe initial bleeding, prevention of ...
The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dep
beta,mercapto-beta,beta-cyclopentamethylene propionic acid(1),Tyr(2),Ile(4),Lys(9)(N(6)-tetramethylrhodamylaminothiocarbonyl)- argipressin: vasopressin receptor antagonist; structure given in first source
Gentaur molecular products has all kinds of products like :search , Alpha Dia \ Anti_Rat AVP V1b IgG, aff pure \ AVP1B13-A for more molecular products just contact us
Supplementary MaterialsSupplementary 1: Shape S1: ear thickness, TEWL, and serum IgE level in FAg-induced dermatitis. The local mRNA manifestation of IFN-increased in mite fecal antigen-induced Read More. ...
The generation of non-thienamycin-producing mutants with mutations in the genes inside the gene cluster from and their involvement in thienamycin biosynthesis and regulation were previously reported. biosynthesis simply because thienamycin production had not been affected in these mutants. High-performance liquid chromatography (HPLC)-mass spectrometry (MS) evaluation of all obtainable mutants uncovered some putative intermediates in the thienamycin biosynthetic pathway. A substance using a mass matching to carbapenam-3-carboxylic acidity was detected in CI-1033 a few from the mutants recommending that the set up from the bicyclic nucleus of thienamycin might move forward in ways analogous compared to that of the easiest organic carbapenem 1 acidity biosynthesis. The deposition of the compound using a mass matching to 2 3 in the mutant suggests that it might be the last intermediate in the biosynthetic pathway. These data together with the establishment of cross-feeding associations from the ...
Dept. of Biomedical Sciences, Univ. of Copenhagen, 3 Blegdamsvej, Bldg. 10.5, DK-2200 Copenhagen N, Denmark. [email protected] ...
BioAssay record AID 426806 submitted by ChEMBL: Antagonist activity at human cloned vasopressin V1A receptor at 2 uM by cell based beta-lactamase assay.
The Vasopressin V1A Receptor, a member of the Vasopressin/Oxytocin Family subfamily, mediates platelet aggregation, cell contraction and proliferation, release of coagula
Mada su sva tri od ovih proteina G protein spregnuti receptori, aktivacija AVPR1A i AVPR1B stimuliše fosfolipazu C, dok aktivacija AVPR2 stimuliše adenilat ciklazu.[2] Ova tri receptora za vazopresin imaju jedinstvene distribucije u tkivu. AVPR1A su izraženi u vaskularnim ćelijama glatkih mišića, hepatocitima, trombocitima, ćelijama mozga, i ćelijama materice. AVPR1B su izraženi u ćelijama prednje hipfize i širom mozga, posebno u piramidalnim neuronima hipokampalnog CA2 polja. AVPR2 su izraženi u tubulima bubrega, u fetalnom plućnom tkivu i raku pluća, zadnja dva od kojih su posledica alternativnog splajsovanja. AVPR2 je takođe izražen u jetri gde stimuliše oslobađanje raznih faktora zgrušavanja u krvotok. U bubrezima, primarna funkcija AVPR2 receptora je da odgovori na arginin vazopresin putem stimulacije mehanizma koji koncentriše urin i održava homeostaza vode u organizmu. Kad je AVPR2 funkcija izgubljena, javlja se nefrogeni dijabetes insipidus (NDI) bolest.[3] ...
Molecules and Mechanisms Implicated in the Peculiar Antigenic Activation Process of Human Vγ9Vδ2 T Cells. - Christelle Harly, Cassie-Marie Peigné, Emmanuel Scotet
Kordusprint materjalide see sait on võimalik ainult kirjaliku loata kirjastaja .Kui tsiteerida viitega kohustuslik tipsed.com. ...
Nephrogenic syndrome of inappropriate antidiuresis (NSIAD) is a recently identified chromosome X-linked disease associated with gain-of-function mutations of the V2 vasopressin receptor (V2R), a...
Title: Aquaretic Agents: Whats Beyond the Treatment of Hyponatremia?. VOLUME: 13 ISSUE: 8. Author(s):Davide Bolignano, Giuseppe Coppolino, Manila Criseo, Susanna Campo, Adolfo Romeo and Michele Buemi. Affiliation:Via Salita Villa Contino, 30,98100 Messina, Italy.. Keywords:Aquaretic, hyponatremia, heart failure, vasopressin, V2 antagonists. Abstract: Unlike the more commonly used diuretics, aquaretic agents can induce an increase in urinary volume without incurring a loss of electrolytes. These molecules belong to a family of vasopressin receptor antagonists, V2 in particular, that regulate optional renal water re-absorption via the synthesis and expression of aquaporin-2. In view of their properties, they have become the agent of choice in the treatment of hyponatremic states with water retention, and different studies have demonstrated that they are more effective and practical to use than other traditional approaches in the treatment of diseases such as cirrhosis-related ascites, SIADH and, ...
BioAssay record AID 2570 submitted by NCGC: Counterscreen Concentration-Response Assay for Antagonists of the Neuropeptide S Receptor: Vasopressin Receptor Calcium Signal Transduction.
Dancing, which is integrally related to music, likely has its origins close to the birth of Homo sapiens, and throughout our history, dancing has been universally practiced in all societies. We hypothesized that there are differences among individuals in aptitude, propensity, and need for dancing that may partially be based on differences in common genetic polymorphisms. Identifying such differences may lead to an understanding of the neurobiological basis of one of mankinds most universal and appealing behavioral traits-dancing. In the current study, 85 current performing dancers and their parents were genotyped for the serotonin transporter (SLC6A4: promoter region HTTLPR and intron 2 VNTR) and the arginine vasopressin receptor 1a (AVPR1a: promoter microsatellites RS1 and RS3). We also genotyped 91 competitive athletes and a group of nondancers/nonathletes (n = 872 subjects from 414 families). Dancers scored higher on the Tellegen Absorption Scale, a questionnaire that correlates positively ...
Dancing, which is integrally related to music, likely has its origins close to the birth of Homo sapiens, and throughout our history, dancing has been universally practiced in all societies. We hypothesized that there are differences among individuals in aptitude, propensity, and need for dancing that may partially be based on differences in common genetic polymorphisms. Identifying such differences may lead to an understanding of the neurobiological basis of one of mankinds most universal and appealing behavioral traits-dancing. In the current study, 85 current performing dancers and their parents were genotyped for the serotonin transporter (SLC6A4: promoter region HTTLPR and intron 2 VNTR) and the arginine vasopressin receptor 1a (AVPR1a: promoter microsatellites RS1 and RS3). We also genotyped 91 competitive athletes and a group of nondancers/nonathletes (n = 872 subjects from 414 families). Dancers scored higher on the Tellegen Absorption Scale, a questionnaire that correlates positively ...
CONTEXT: Cushing disease (CD) is a rare disorder with severe sequels and incompletely understood pathogenesis. The underlying corticotroph adenomas harbor frequently somatic mutations in the ubiquitin-specific peptidase 8 (USP8) gene. These mutations render USP8 hyperactive and prevent client proteins from degradation.. OBJECTIVE: To investigate the impact of USP8 mutations on proteins deregulated in CD.. DESIGN: One hundred eight pituitary adenomas (75 corticotroph [58 USP8 wild type (WT) and 17 USP8 mutated], 14 somatotroph, and 19 nonfunctioning) were investigated by immunohistochemistry. All evaluated proteins [USP8, arginine vasopressin receptor 1b and 2, corticotropin-releasing hormone receptor, cAMP response element-binding protein (CREB), p27/kip1, cyclin E, heat shock protein 90 (HSP90), orphan nuclear receptor 4, epidermal growth factor receptor, histone deacetylase 2, glucocorticoid receptor, cyclin-dependent kinase 5 and Abelson murine leukemia viral oncogene homolog 1 enzyme ...
A New Synthetic Route to YM087, an Arginine Vasopressin Antagonist.|span||/span| | Takashi Tsunoda; Akihiro Tanaka; Toshiyasu Mase; Shuichi Sakamoto | download | BookSC. Download books for free. Find books
DESCRIPTION (provided by applicant): Diabetes and congestive heart failure are diseases that have been associated with defects in the handling of salt and water by the kidney. Common in individuals with these disorders are elevated circulating levels of vasopressin, the peptide hormone that regulates renal water excretion. Circulating vasopressin plays a critical role in extra-cellular fluid expansion and development of hypertension, thus contributes to the pathogenesis of the disease. Vasopressin has clear long-term actions in the kidney, associated with vasopressin receptor activated processes and transcriptional regulation. Circulating vasopressin also increases the concentrating capacity of the renal medulla by activating the counter current mechanism. The result is an increase in medullary osmotic stress that can directly activate renal cell signaling pathways and gene transcription. Thus specific effects of vasopressin on gene expression are not delineated from secondary alterations ...
Inhospital cardiac arrest still constitutes an important clinical problem with survival to discharge ranging within 0-42% (most common range = 15-20%). Survival after witnessed, pulseless ventricular fibrillation/tachycardia(VF/VT) that is responsive to one or two direct current countershock(s) may exceed 30%. However, survival after inhospital asystole, pulseless electrical activity, or refractory VF/VT (defined as not responsive to two countershocks) may be substantially lower (, 5-10%). As in nonsurvivors, both endogenous vasopressin and adrenocorticotrophin are reduced compared to survivors, we hypothesized that the addition of exogenous vasopressin and steroids to the standard CPR protocol may increase the rates of both the return of spontaneous circulation (ROSC) and of post-arrest survival. The mechanistic basis of this hypothesis comprises the simultaneous activation of adrenergic and vasopressin receptors, in conjunction with a potential steroid-mediated enhancement of the vascular ...
Tolvaptan is an orally administered, nonpeptide, selective arginine vasopressin V(2) receptor antagonist that increases free water clearance, thereby correcting low serum sodium levels. SALT-1 and -2, two identical, randomized, double-blind, placebo-
3,4-methylenedioxymethamphetamine (MDMA) and its derivatives, 2,5-dimethoxy-4-bromo-amphetamine hydrobromide (DOB) and para-methoxyamphetamine (PMA) are recreational drugs whose pharmacological effects have recently been attributed to serotonin 5HT2A/C receptors. However, there is growing evidence that the oxytocin/vasopressin system can modulate some the effects of MDMA. In this study, MDMA (2.5-10 mg/kg), DOB (0.5 mg/kg) or PMA (0.005, 0.1 or 0.25 mg/kg) were administered intramuscularly (IM) to adult zebrafish, alone or in combination with the V1a vasopressin antagonist, SR49059 (0.01-1 ng/kg), before carrying out conditioned place preference (CPP), social preference, novel tank diving and light-dark tests in order to evaluate subsequent rewarding, social and emotional-like behaviour. The combination of SR49059 and each drug progressively blocked: 1) rewarding behaviour as measured by CPP in terms of time spent in drug-paired compartment; 2) pro-social effects measured on the basis of the
In the present dose-response study, we investigated short-term effects of tolvaptan on renal tubular function, vasoactive hormones and systemic hemodynamics during basal conditions and during tolvaptan with NO-inhibition in healthy subject. The present study is a continuation and expansion of a previous randomized, double-blinded, placebo-controlled crossover, single-dose study conducted by our laboratory [12].. At baseline, tolvaptan increased renal water excretion dose-dependently up to 30 mg, without affecting sodium excretion. During L-NMMA infusion, tolvaptan decreased water excretion dose-dependently, whereas sodium excretion decreased independently of the dose. In the post infusion period, water excretion remained reduced during all tolvaptan doses, but increased during placebo. Tolvaptan increased sodium excretion to a higher level.. Recent dose-response trials have shown that oral administration of tolvaptan 30 mg led to a fast increase in the effective concentration in plasma. This ...
Stable recombinant cell line expressing the Vasopressin, V2 receptor. Human recombinant, in 1321N1 host cell. We provide: Two vials of the recombinant cell line as frozen cells; Detailed product information including sequence, cell line properties, culture conditions, pharmacological properties of the recombinant receptor in binding and functional assays (cAMP). In addition, for total reassurance, we will provide up to two free replacements within in a 2 year period should you accidently lose your cell line ...
NEX310 [125I]-Phenylacetyl-D-Tyr(Me)-Phe-Gln-Asn-Arg-Pro-Arg-Tyr-NH2 is useful in receptor studies and autoradiography for the localization and characterization of Vasopressin V1A receptors. ...
Samsca, which contains the active substance tolvaptan, belongs to a group of medicines called vasopressin antagonists. This means that it prevents vasopress
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At the hospital I now work at we have just started using vasopressin on hypotensive pts from sepsis, the dose the doc wrote was o.o4U per min and not to be titrated. I also work at a large Level 1
Rabbit polyclonal antibody raised against synthetic peptide of AVPR1A. A synthetic peptide corresponding to 18 amino acids at cytoplasmic domain of human AVPR1A. (PAB25563) - Products - Abnova
Cumpara rapid si simplu Tinctura Splinuta. Tinctura de splinuta (Goldenrod) este folosita ca agent aquaretic, in sensul ca sustine pierderea apei din organism.
GIRL!! Suse, her DP and DS welcome the safe arrival this morning of their yet to be named daughter/sister. 3.6kg @ 9.09am Congratulations to you all a
Heres my AvP Requiem Blu-Ray Review. The film isnt a total loss, there are some genuinely good moments but the script is just awful.
Inimese kloonimine tähendab olemasolevast või varem eksisteerinud inimesest geneetiliselt identse koopia loomist. Seda mõistet kasutatakse tavaliselt selleks, et määratleda inimese kunstlikku kloonimist. Loomuliku paljunemise ajal võib toimuda samuti kloonimine, selle tulemusena sünnivad identsed kaksikud. Eristatakse kahte inimkloonimist - üks on terapeutiline kloonimine ja teine reproduktiivne kloonimine. Teoreetiliselt on võimalik ka kolmas koonimise variant, kus ühendatakse nii terapeutiline kui ka reproduktiivne kloonimine. Seda kutsutakse asenduskloonimiseks. See tähendaks ulatuslikult kahjustunud kehaosa asendamist, millele järgneks osaline või täielik ajusiirdamine. Erinevad inimkloonimise tüübid on tekitanud palju vaidlusi.[24] Enamik teadus-, valitsus- ja usuorganisatsioone on rangelt reproduktiivse kloonimise vastu. Ameerika Ühendriikide teaduse edendamise liit (AAAS) ja paljud teised teadusühingud on teinud avaldusi, et inimese kloonimine tuleks keelustada seni, ...