• Although the exact mechanism by which adenosine receptor activation relaxes vascular smooth muscle is not known, there is evidence to support both inhibition of the slow inward calcium current reducing calcium uptake, and activation of adenylate cyclase through A2 receptors in smooth muscle cells. (globalrph.com)
  • Methylxanthines act as competitive antagonists of adenosine and can blunt its pharmacological effects. (wikipedia.org)
  • This is being contested, and it is now considered a relative contraindication (however, selective adenosine antagonists are being investigated for use in treatment of asthma) Adenosine is an endogenous purine nucleoside that modulates many physiological processes. (wikipedia.org)
  • The locomotor effects in mice of selective A1 and A2 adenosine agonists, antagonists and combinations of agonists were investigated utilizing a computerized activity monitor. (thetechnoant.info)
  • The depressive ramifications of N6-cyclopentyladenosine, a detailed analog of CHA, are reversed by extremely A1-selective antagonists such as for example CPT, indicating that A1 receptors triggered by N6-cycloalkyladenosines subserve behavioral major depression (Bruns 1988). (thetechnoant.info)
  • Although A1-selective agonists have already been created, adenosine agonists or antagonists really selective for A2 adenosine receptors for make use of as physiological probes have already been difficult to recognize. (thetechnoant.info)
  • Pharmacological studies have shown that KW-6356 is a potent and selective ligand for the A2A receptor (the -log of inhibition constant = 9.93 ± 0.01 for human receptor) with a very low dissociation rate from the receptor (the dissociation kinetic rate constant = 0.016 ± 0.006 minute-1 for human receptor). (bvsalud.org)
  • SIGNIFICANCE STATEMENT: KW-6356 is a potent and selective adenosine A2A receptor antagonist/inverse agonist and exhibits insurmountable antagonism, whereas istradefylline, a first-generation adenosine A2A receptor antagonist, exhibits surmountable antagonism. (bvsalud.org)
  • Here, we have investigated the effect of A2A and A2B -selective agonists on vasodilatation in three distinct vascular beds of the rat cardiovascular system. (bvsalud.org)
  • The regional hemodynamic effects of adenosine A2A and A2B selective agonists were investigated in conscious rats. (bvsalud.org)
  • The A2A -selective agonist CGS 21680 produced a striking increase in heart rate (HR) and hindquarters vascular conductance (VC) that was accompanied by a significant decrease in mean arterial pressure (MAP) in conscious rats. (bvsalud.org)
  • In marked contrast, the A2B -selective agonist BAY 60-6583 significantly increased HR and VC in the renal and mesenteric vascular beds, but not in the hindquarters. (bvsalud.org)
  • Taken together, these data indicate that A2A and A2B receptors are regionally selective in their regulation of vascular tone. (bvsalud.org)
  • Hence, it would appear that A1- and A2-selective adenosine agonists possess different central depressant results, which may be potentiative. (thetechnoant.info)
  • The fairly high strength of NECA could possibly be because of a synergism between central A1 and A2receptor activation by this non-selective agonist. (thetechnoant.info)
  • At the same time, adenosine modulates striatal DA release by stimulating glutamate release at adenosine receptors in the striatum , which increases dopamine levels. (adxs.org)
  • In contrast, caffeine at doses reflecting daily human consumption does not induce a release of dopamine in the shell of the nucleus accumbens but leads to a release of dopamine in the prefrontal cortex, which is consistent with its reinforcing properties. (medscape.com)
  • These results suggest that the development of A2B receptor agonists to induce vasodilatation in the kidney may provide a good therapeutic approach for the treatment of acute kidney injury. (bvsalud.org)
  • A1 receptors can also inhibit calcium mineral fluxes (Cerbai 1988) and induce potassium fluxes (Belardinelli and Isenberg, 1983). (thetechnoant.info)
  • We demonstrate that deletion of the macrophage vitamin D receptor (VDR) in mice (KODMAC) is sufficient to induce insulin resistance by promoting M2 macrophage accumulation in the liver as well as increasing cytokine secretion and hepatic glucose production. (regenerativemedicine.net)
  • Adenosine is a potent vasodilator in most vascular beds, except in renal afferent arterioles and hepatic veins where it produces vasoconstriction. (globalrph.com)
  • Adenosine is one of the four nucleoside building blocks of RNA (and its derivative deoxyadenosine is a building block of DNA), which are essential for all life on earth. (wikipedia.org)
  • The intracellular uptake of adenosine is mediated by a specific transmembrane nucleoside transport system. (globalrph.com)
  • Methylxanthines (e.g. caffeine found in coffee, theophylline found in tea, or theobromine found in chocolate) have a purine structure and bind to some of the same receptors as adenosine. (wikipedia.org)
  • Adenosine is thought to exert its pharmacological effects through activation of purine receptors (cell-surface A1 and A2 adenosine receptors). (globalrph.com)
  • Nevertheless, the potencies of adenosine agonists in locomotor major depression were recently discovered to correlate towards the potencies from the analogs at A2 adenosine receptors rather than to potencies at A1 adenosine receptors (Durcan and Morgan, 1989a), resulting in the proposal that mainly A2 receptors get excited about these results. (thetechnoant.info)
  • Lately, we reported that APEC is normally a powerful locomotor depressant in mice which the pharmacological profile of the actions suggests activation of A2 adenosine receptors (Nikodijevic 1990). (thetechnoant.info)
  • NanoBRET ligand binding studies were used to confirm receptor selectivity. (bvsalud.org)
  • Fasiglifam Utilizing a functionalized congener strategy, some long string derivatives of "type":"entrez-protein","attrs":"text message":"CGS21680″,"term_identification":"878113053″,"term_text message":"CGS21680″CGS21680 that maintain A2 strength and selectivity and don't support the carboxylic features was synthesized (Jacobson 1989). (thetechnoant.info)
  • Crystallography of KW-6356- and istradefylline-bound A2A receptor have indicated that interactions with His2506.52 and Trp2466.48 are essential for the inverse agonism, whereas the interactions at both deep inside the orthosteric pocket and the pocket lid stabilizing the extracellular loop conformation may contribute to the insurmountable antagonism of KW-6356. (bvsalud.org)
  • Adenosine is certainly a modulator of several physiological features. (thetechnoant.info)
  • In this study, we investigated the in vitro pharmacological profile of KW-6356 as an A2A receptor antagonist/inverse agonist and the mode of antagonism and compared them with istradefylline. (bvsalud.org)
  • Thus, we aim to determine whether leptin and adiponectin as two potent regulators of insulin secretion in islets can Gemcitabine HCl price influence the transcription of PPAR as their target. (irjs.info)
  • Caffeine has a three-dimensional structure similar to that of adenosine," which allows it to bind and block its receptors. (wikipedia.org)
  • In humans, tolerance to some subjective effects of caffeine may occur, but most of the time, complete tolerance to many effects of caffeine on the central nervous system (CNS) does not occur. (medscape.com)
  • In humans, the reinforcing stimulus functions of caffeine are limited to low or moderate doses, while high doses usually are avoided. (medscape.com)
  • Classic drugs of abuse lead to specific increases in cerebral functional activity and dopamine release in the shell of the nucleus accumbens (the key neural structure for reward, motivation, and addiction). (medscape.com)
  • Through this mechanism, the increased level of adenosine after sleep deprivation could affect the light sensitivity of the circadian clock. (adxs.org)
  • insulin secretion was evaluated by ELISA. (irjs.info)
  • Results Leptin decreased PPAR transcription and insulin secretion, while adiponectin significantly increased Pdx1 and PPAR transcription and insulin secretion in rat islets. (irjs.info)
  • Conclusions These results indicate the chance that Pdx1 and PPAR transcription can be a mediator of leptin and adiponectin function in charge of insulin secretion and blood sugar homeostasis in pancreatic islets. (irjs.info)
  • These outcomes suggest the immediate inhibitory actions of leptin on insulin secretion from pancreatic -cells (7-9). (irjs.info)
  • Furthermore, it's been reported that adiponectin affected blood sugar induced insulin secretion because its receptors had been determined in the pancreatic islet cells (11). (irjs.info)
  • Furthermore, it controls many areas of adult cell function, including glucose-mediated insulin secretion in Gemcitabine HCl price adult islet beta cells (12). (irjs.info)
  • We hypothesized how the inhibitory actions of leptin or the stimulatory aftereffect of adiponectin on insulin secretion may occur through alteration in Pdx1 transcription. (irjs.info)
  • The nuclear hormone receptor, peroxisome proliferator-activated receptor (PPAR), can be mixed up in rules of insulin level of sensitivity and blood sugar homeostasis (14). (irjs.info)
  • Two thiazolidinediones (TZDs), pioglitazone and rosiglitazone, and agonists of PPAR, furthermore to their Rabbit Polyclonal to 14-3-3 zeta impact on peripheral insulin-sensitive cells, could be effective in endocrine pancreas also. (irjs.info)
  • Recently, impaired insulin secretion has been reported in heterozygous PPAR-deficient mice, which is related to increased islet triacylglycerol content (16). (irjs.info)
  • It has been reported that this TZD, troglitazone, increase the amount of insulin secretion from isolated islets and HIT-T15 cells (17). (irjs.info)
  • mice and leptin receptor insufficiency in mice resulted in hyperinsulinemia even prior to the development of weight problems and diabetes which hyperinsulinemia was ameliorated by administration of recombinant leptin towards the mice. (irjs.info)
  • Adenosine is used as an adjunct to thallium (TI 201) or technetium (Tc99m) myocardial perfusion scintigraphy (nuclear stress test) in patients unable to undergo adequate stress testing with exercise. (wikipedia.org)
  • Istradefylline is a first-generation A2A receptor antagonist approved for use as adjunct treatment to levodopa/decarboxylase inhibitor in adult PD patients experiencing "OFF" episodes. (bvsalud.org)
  • The dose is often decreased in patients on dipyridamole (Persantine) and diazepam (Valium) because adenosine potentiates the effects of these drugs. (wikipedia.org)
  • Drugs intended for human or veterinary use, presented in their finished dosage form. (drugbank.com)
  • Common contraindications for adenosine include Asthma, traditionally considered an absolute contraindication. (wikipedia.org)
  • KW-6356 is a novel adenosine A2A (A2A) receptor antagonist/inverse agonist, and its efficacy as monotherapy in Parkinson's disease (PD) patients has been reported. (bvsalud.org)
  • Adenosine (symbol A) is an organic compound that occurs widely in nature in the form of diverse derivatives. (wikipedia.org)
  • Cellular signaling by adenosine occurs through four known adenosine receptor subtypes (A1, A2A, A2B, and A3). (wikipedia.org)
  • May also be used to suppress thyroid stimulating hormone (TSH) secretion in patients with simple (nontoxic) goiter, subacute or chronic. (drugbank.com)
  • Part of this adenosine is discharged from the cell and binds to adenosine receptors of neighboring cells, which is supposed to compensate for the disturbed balance between energy consumption and energy supply. (adxs.org)
  • Among other things, adenosine is used for autoregulation in the event of an imminent lack of energy in the cell (e.g. when the cell's performance is overloaded or when there is a lack of oxygen): If the ATP content in a cell drops, more adenosine is produced as a hydrolysis product. (adxs.org)
  • Increased foam cell formation results from lack of VDR-SERCA2b interaction, causing SERCA dysfunction, activation of ER stress-CaMKII-JNKp-PPARγ signaling, and induction of the scavenger receptors CD36 and SR-A1. (regenerativemedicine.net)
  • Adenosine is found in almost all body cells. (adxs.org)
  • When adenosine is used to cardiovert an abnormal rhythm, it is normal for the heart to enter ventricular asystole for a few seconds. (wikipedia.org)
  • Each I.V. bolus of adenosine should be followed with normal saline flush. (globalrph.com)
  • The adenosine system is closely linked to the dopaminergic system. (adxs.org)
  • The role of TRAIL/TRAIL receptors in central nervous system pathology. (mdc-berlin.de)
  • Fast rhythms of the heart that are confined to the atria (e.g., atrial fibrillation and atrial flutter) or ventricles (e.g., monomorphic ventricular tachycardia), and do not involve the AV node as part of the re-entrant circuit, are not typically converted by adenosine. (wikipedia.org)
  • A NICU with an improved work environment and better trained nurses and neonatologists can guarantee breastfeeding support to mothers and babies and therefore achieve a higher rate of newborns discharged home with exclusive human milk feeding. (biomedcentral.com)
  • In addition, atrial tachycardia can sometimes be terminated with adenosine. (wikipedia.org)
  • In addition, we determined cocrystal structures of A2A receptor in complex with KW-6356 and istradefylline to explore the structural basis of the antagonistic properties of KW-6356. (bvsalud.org)