• The homogeneous assay kit format allows you to detect agonists, antagonists, and allosteric modulators. (discoverx.com)
  • Tectorigenin and aristofone acted as muscarinic receptor M3 antagonists, while synephrine, ephedrine and pseudoephedrine were ß2-adrenoceptor agonists. (bvsalud.org)
  • Central-type and peripheral-type benzodiazepine receptor antagonists did not abrogate proliferation inhibition by midazolam, while the specific TRPM7 agonist bradykinin reversed this effect. (elsevierpure.com)
  • Hypotensive effects of Lys-des-Arg9-bradykinin and metabolically protected agonists of B1 receptors for kinins. (aspetjournals.org)
  • B1 receptors for kinins are selectively stimulated by bradykinin (BK) or Lys-BK (kallidin) fragments without the C terminal arginine residue. (aspetjournals.org)
  • We report here that some, but not all, TAS2R agonists decrease [Ca2+]i and relax HASM contracted by G-protein coupled receptors (GPCRs) that stimulate [Ca2+]i. (jefferson.edu)
  • The transferred B1-receptors induced calcium influx after B1-receptor agonist stimulation: a response abrogated by a specific B1-receptor antagonist. (lu.se)
  • Enhanced Gi2 signalling HTRA3 defends the center from ischaemic damage Adenosine, opioids, bradykinin, and various other agonists that work at Gi-coupled receptors protect the center from ischaemic damage. (woofahs.com)
  • Galnon inhibited adenylate cyclase activity, suggesting an agonist action at galanin receptors. (phoenixpeptide.com)
  • Furthermore, ET-1 and BK heterologously desensitized the stimulation of PI hydrolysis by PE, ET-1 or BK homologously uncoupled their own receptors from [3H]InsP3 formation, but there was no evidence of heterologous desensitization with these two agonists. (reading.ac.uk)
  • There has been recent evidence linking bradykinin (BK) receptors with inflammation. (cmich.edu)
  • Data suggest that in persistent inflammatory conditions in the rat bradykinin B 1 receptors are involved in the accompanying hyperalgesia. (cmich.edu)
  • Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. (bvsalud.org)
  • Other dichotomous responses were found when [Ca2+]i was stimulated by bradykinin, angiotensin, and acetylcholine. (jefferson.edu)
  • AA is released from cell membrane(endogenous AA) by several agonists such as histamine, bradykinins, angiotensin, cytokines and growth factors, including shear stress. (tci-thaijo.org)
  • Angiotensin-converting enzyme (ACE) is crucial in the synthesis of angiotensin II, breakdown of bradykinin and the hydrolysis of several other neuropeptides such as enkephalin, substance P, dynorphin and neurotensin. (unboundmedicine.com)
  • The peptide, bradykinin, has cardiovascular effects similar to those of histamine and plays prominent roles in inflammation and nociception. (mhmedical.com)
  • The agonist profile of M40, a representative chimeric peptide, was found not to be the result of receptor reserve because receptor inactivation by partial alkylation experiments confirmed its full intrinsic efficacy under conditions of a "zero" reserve state. (phoenixpeptide.com)
  • Atractyline and shogaol showed as a cannabinoid receptor CB2 agonist and a histamine receptor H1 antagonist, respectively. (bvsalud.org)
  • Samples were incubated in the presence or absence of agonist (CaM) and antagonist (KN-93), and Ca2+ uptake was evaluated over a 45-min period. (brinda.info)
  • We utilized eight TAS2R agonists and five procontractile GPCR agonists in cultured HASM cells. (jefferson.edu)
  • In the present study, we extended this previous observation by comparing the effect of Tg and other calcium-mobilizing G-protein-coupled receptor (GPCR) agonists on the expression of different pro-inflammatory genes in response to tumor necrosis factor (TNF)-α in ASM cells. (tmu.edu.tw)
  • These results show that calcium-mobilizing GPCR agonists functionally interact with TNF-α to differentially regulate pro-inflammatory genes expression in human ASM cells, possibly by involving Tg-sensitive intracellular calcium stores, SOC and PKC. (tmu.edu.tw)
  • In this kinetic assay, agonist-induced release of Venus-tagged Gβγ subunits from Gα12 is followed in real time using nano-luciferase (Nluc)-tagged BRET donor. (nih.gov)
  • Using this assay, we characterized bradykinin B2 receptor (BDKRB2) and found that the receptor couples to Gα12 in addition to Gαo, and Gαq, but not to Gαs. (nih.gov)
  • To test the effect of B 1 receptor agonists, each assay was carried out overnight at 37°C in 5% CO 2 -95% air on neutrophils primed with 1 ng/ml interleukin-1β. (uai.cl)
  • Metabolically stable bradykinin B2 agonists, methionine-lysine-bradykinin and labradimil, had differential effects on the transvascular flow rate of Gd-DTPA across the blood-brain tumor barrier. (biomedcentral.com)
  • MacKenzie, A. , Cooper, E.J. and Dowell, F.J. (2008) Differential effects of glucose on agonist-induced relaxations in human mesenteric and subcutaneous arteries. (gla.ac.uk)
  • The protective effects of this phenomenon have been demonstrated to be mediated by release of autocoids such as adenosine, opioids and bradykinin. (sun.ac.za)
  • Kallikrein is a protease that cleaves high-molecular-weight-kininogen (HMWK) to generate cleaved HMWK and bradykinin, a potent vasodilator that increases vascular permeability resulting in swelling and pain associated with HAE. (medscape.com)
  • Danielisova V, Gottlieb M, Nemethova M et al (2009) Bradykinin postconditioning protects pyramidal CA1 neurons against delayed neuronal death in rat hippocampus. (springer.com)
  • These peptides behaved as full agonists as determined by the inhibition of forskolin-stimulated cyclic 3'5'-adenosine monophosphate production and the stimulation of guanosine 5'-O-(3-[35S]thiotriphosphate binding. (phoenixpeptide.com)
  • Relaxations to acetylcholine and bradykinin were determined in a control (5 mM) and high glucose (20 mM) environment over a 2 and 6 h incubation period. (gla.ac.uk)
  • Key results: Bradykinin-induced relaxation in both sets of vessels was mediated entirely by EDHF whilst that generated by acetylcholine, though principally generated by EDHF, also had contribution from prostacyclin and possibly nitric oxide in mesenteric and subcutaneous vessels, respectively. (gla.ac.uk)
  • We analyzed the chemotactic effect of kinin B 1 receptor agonists on neutrophils isolated from peripheral blood of human healthy subjects. (uai.cl)
  • A generation of kinin B 1 receptor agonists during the early phase of acute inflammation may favor the recruitment of neutrophils to the inflammatory site. (uai.cl)
  • Pharmacological and biochemical characterization of a recombinant human galanin GALR1 receptor: agonist character of chimeric galanin peptides. (phoenixpeptide.com)
  • The intravenous co-infusion of labradimil, a metabolically stable bradykinin B2 receptor agonist, has been shown to temporarily enhance the transvascular delivery of small chemotherapy drugs, such as carboplatin, across the blood-brain tumor barrier. (biomedcentral.com)
  • Metabolically stable bradykinin B2 receptor agonists, methionine-lysine-bradykinin and labradimil, enhance the transvascular delivery of small chemotherapy drugs across the BBTB of malignant gliomas by increasing the blood half-life of the co-infused drug. (biomedcentral.com)
  • We found that in resting cells, Tg (10-100 nM) or the bradykinin (BK) (1-10 μM) and thrombin (Thr) (1 U/ml) stimulated interleukin (IL)-6 secretion but had no effect on regulated on activation, normal T cells expressed and secreted (RANTES) levels. (tmu.edu.tw)
  • Receptores de la superficie celular que poseen una alta afinidad para unirse a la BRADIQUININA y a las QUININAS relacionadas y que generan cambios intracelulares que influyen en el comportamiento de las células. (bvsalud.org)
  • Effect of calmodulin kinase II (CaMKII) inhibition on decay of ACh and bradykinin-induced [Ca2+]i transients in human ASM cells. (brinda.info)
  • Anticonvulsant activity of a nonpeptide galanin receptor agonist. (phoenixpeptide.com)
  • A low molecular weight galanin receptor agonist, 7-((9-fluorenylmethoxycarbonyl)cyclohexylalanyllysyl)amino-4-methylcoumarin (galnon) was found to displace (125)I-galanin with micromolar affinity at Bowes cellular and rat hippocampal membranes. (phoenixpeptide.com)
  • These findings introduce a systemically active nonpeptide galanin agonist anticonvulsant. (phoenixpeptide.com)
  • In this study we (1) characterized the endothelial-dependent relaxation of two similarly sized but anatomically distinct human arteries to two different agonists and (2) determined how these responses are modified by acute exposure to high glucose. (gla.ac.uk)
  • Conclusions and implications: Short periods of high glucose exert a variable influence on endothelial function in human isolated blood vessels that is dependent on factors of time, agonist-used and vessel studied. (gla.ac.uk)
  • With the use of fluorescent Ca 2+ dye, it was found that epinephrine and isoprenaline, a β-adrenoceptor agonist, induced endothelial Ca 2+ influx in the presence of bradykinin. (edu.hk)
  • In summary, CNG channels, CNGA2 in particular, mediate β-adrenoceptor agonist-induced endothelial Ca 2+ influx and subsequent vascular dilation. (edu.hk)
  • In this study we investigated the systemic actions of labradimil, as well as other bradykinin B2 receptor agonists with a range of metabolic stabilities, in context of the local actions of the respective B2 receptor agonists on the blood-brain tumor barrier of rodent malignant gliomas. (biomedcentral.com)
  • The decrease in systemic blood pressure correlated with the known metabolic stability of the bradykinin B2 receptor agonist infused. (biomedcentral.com)
  • The vascular endothelium modulates contractile responses to 5-HT and ET-1 in human subcutaneous resistance arteries but this effect is lost in patients with NPG, indicating a selective defect in agonist mediated release of endothelium derived vasodilators. (bmj.com)
  • An infusion of the B1 agonist Sar-[D-Phe8]des-Arg9-BK (1 microgram/min) in lipopolysaccharide-pretreated rabbits led to a very important and persistent hypotensive state that was not prevented by indomethacin. (aspetjournals.org)
  • To rule out extraneous effects of KN-93, additional experiments were performed in the absence of extracellular Ca2+ where, following initial evaluation of [Ca2+]i responses to ACh or bradykinin in zero-Ca2+ HBSS, cells were washed in HBSS (to allow for SR Ca2+ refilling) and then preexposed to KN-93 before reevaluation of the [Ca2+]i responses to the same agonist. (brinda.info)
  • Baseline blood and brain tumor tissue pharmacokinetics were imaged with the 1st bolus of Gd-DTPA over the first hour, and then re-imaged with a 2nd bolus of Gd-DTPA over the second hour, during which normal saline or a bradykinin B2 receptor agonist was infused intravenously for 15 minutes. (biomedcentral.com)
  • Both methionine-lysine-bradykinin and labradimil increased the blood half-life of Gd-DTPA sufficiently enough to increase significantly the tumor tissue Gd-DTPA area under the time-concentration curve. (biomedcentral.com)
  • Regulation of phospholipases C and D in rat ventricular myocytes: stimulation by endothelin-1, bradykinin and phenylephrine. (reading.ac.uk)
  • A clear chemotactic activity was observed when primed neutrophils were challenged with Lys-des[Arg 9 ]-bradykinin (LDBK) or des[Arg 9 ]-bradykinin at 10 -10 M but not when unprimed cells were used. (uai.cl)
  • Bradykinin elicited substantial dilation in coronary arterioles, with a similar magnitude in obese and non-obese patients (to 10 -8 M: 55 ± 5% vs. 46 ± 5%, P = 0.20), but with significantly enhanced sensitivity in obesity (EC50: 8.2x10 -9 M vs. 1.9x10 -8 M, respectively, P = 0.03). (biomedcentral.com)
  • Moreover, obese patients with or without statin exhibited significantly increased coronary dilation to bradykinin, when compared to non-obese patients without statin therapy. (biomedcentral.com)
  • Intrahippocampal injection of galnon also shortened the duration of self-sustaining status epilepticus in rats, confirming its agonist properties in vivo. (phoenixpeptide.com)
  • Chen TY, Goyagi T, Toung TJ et al (2004) Prolonged opportunity for ischemic neuroprotection with selective kappa-opioid receptor agonist in rats. (springer.com)
  • The naturally occurring B1 agonist Lys-des-Arg9-BK was more potent than des-Arg9-BK in the in vivo model, but the effect of either natural sequence was brief. (aspetjournals.org)
  • Chronic administration of these TRPA1 agonists was well tolerated. (nature.com)
  • Notably, the dermorphins and bombesins are opioid agonists that are similar to beta-endorphins produced naturally by the body. (sacredenergyslc.com)
  • In contrast to other chemoattractants such as fMLP, cytosolic intracellular calcium did not increase in response to the B 1 receptor agonist LDBK. (uai.cl)
  • To induce the ebook la méthode for specific exploratory bradykinin in these agonists, implantable adverse intact unit patients bind conducted characterized. (hone.world)
  • Rabbits pretreated with bacterial lipopolysaccharide (LPS) (25 micrograms/kg) and anesthetized 5 h later exhibit acute and transient hypotension in response to intra-arterial boluses of B1 receptor agonists. (aspetjournals.org)
  • We have measured activation of these phospholipases by endothelin-1 (ET-1), bradykinin (BK), or phenylephrine (PE) in ventricular myocytes cultured from neonatal rat. (reading.ac.uk)
  • Using total internal reflection fluorescence microscopy and density gradient centrifugation we found that mouse TRPA1 localizes preferably into cholesterol-rich domains and functional experiments revealed that cholesterol depletion decreases channel sensitivity to chemical agonists. (elifesciences.org)
  • Those TAS2R agonists that decreased [Ca2+]i, promoted hyperpolarization, and decreased HASM stiffness, caused relaxation of human airways. (jefferson.edu)
  • Charron C, Messier C, Plamondon H (2008) Neuroprotection and functional recovery conferred by administration of kappa- and delta 1-opioid agonists in a rat model of global ischemia. (springer.com)
  • A 2-h incubation of high glucose impaired bradykinin-induced relaxation of subcutaneous vessels whilst, in contrast, the relaxation generated by bradykinin in mesenteric vessels was enhanced at the same time point. (gla.ac.uk)
  • Bradykinin-induced coronary dilation was assessed by videomicroscopy in ex vivo coronary arterioles obtained from 64 consecutive patients undergoing heart surgery. (biomedcentral.com)
  • Treatment with the dopamine receptor agonist, apomorphine, or the dopamine-releasing drug, amphetamine, produced significant disruption of PPI in control mice but not in ACE knockout mice. (unboundmedicine.com)
  • Moreover, we identified two structural motifs in transmembrane segments 2 and 4 involved in mTRPA1-cholesterol interactions that are necessary for normal agonist sensitivity and plasma membrane localization. (elifesciences.org)
  • The beta2-adrenergic agonist terbutaline (Brethaire, Brethine) has been shown to be more effective at controlling urticaria than placebo. (medscape.com)