In the first group adenosine, via activation of postsynaptic A1 receptors, reduced spontaneous firing via inhibition of the hyperpolarization-activated cation current. (nih.gov)
Both of these effects occur via postsynaptic A1 receptors, but are mediated downstream by two separate mechanisms. (nih.gov)
Reversal of Tau-Dependent Cognitive Decay by Blocking Adenosine A1 Receptors: Comparison of Transgenic Mouse Models with Different Levels of Tauopathy. (neurotree.org)
3 A non-speci®c adenosine receptor agonist 2-chloroadenosine (CAD) resulted in biphasic response with a small contraction at lower concentrations (1079 ±1078 M) followed by a signi®cant relaxation at higher concentration in endothelium-intact SHR tissues suggesting presence of both A1 and A2 adenosine receptors in SHR aorta. (uncg.edu)
SLV 320 is a potent and selective adenosine A 1 receptor antagonist (K i values are 1, 200, 398 and 3981 nM at human A 1 , A 3 , A 2A and A 2B receptors respectively). (tocris.com)
However, what is known is that it is a competitive antagonist of adenosine A1 and A2 receptors. (rxeconsult.com)
the respective roles of the A1-, A2-, A3-adenosine receptors as well as the involvement of the PI3-K/PKB/Akt and ERKp44/p42 signal transduction pathways, in the cardioprotective phenomemon of -adrenergic preconditioning and (iv) the contribution of the mitochondrial KATP channels (mKATP), reactive oxygen species and NO to the mechanism of -AR-induced cardioprotection. (sun.ac.za)
The role of adenosine and the adenosine A1, A3, A2A and A2B receptors was studied by using adenosine deaminase and the selective antagonists DPCPX (1 μM), MRS 1191(1 μM), ZM241385 (1 μM) and MRS1754 (1 μM). (sun.ac.za)
Our overall hypothesis is that adenosine triphosphate (ATP) utilization during glucose absorption would increase adenosine metabolite release, which acts on adenosine A1 receptors to alter endothelial production of NO and/or activate ATP-dependent potassium channels (K + ATP ) to dilate intestinal microvessels. (arizona.edu)
Conclusion: These data suggest that glucose-induced vasodilation of premucosal jejunal arterioles is mediated through adenosine A1 receptors, and NO at least partially mediates the adenosine A1 receptor-induced vasodilation. (arizona.edu)
Antagonists of P2 receptors counteracted the enhancing effects of ATP, suggesting that HS costimulates neutrophils by means of P2 receptor activation. (escholarship.org)
Alexander SP: Flavonoids Small molecule library purchase as antagonists at A1 adenosine receptors. (inhibitorkit.com)
A1 receptors can also inhibit calcium mineral fluxes (Cerbai 1988) and induce potassium fluxes (Belardinelli and Isenberg, 1983). (thetechnoant.info)
Ramifications of A1 receptors on phosphoinositide break down likewise have been reported (Linden and Delahunty, 1989). (thetechnoant.info)
The relevance of A1 and A2 receptors to CNS function is certainly under active analysis. (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)
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)
Nevertheless, in similar research in rats, the 100- to 300-collapse greater strength of R-PIA in accordance with S-PIA is definitely more consonant using the participation of A1 receptors (Goldberg 1985). (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)
Selective8
We first utilized two pharmacological brokers W146 a selective antagonist for S1P1 (Gaengel et al. (researchassistantresume.com)
8. Melchiorre C., Bolognesi M.L., Chiarini A., Minarini A., Spampinato S., Synthesis and biological activity of some methoctramine-related tetraamines bearing A 11-Acetyl-5,11-Dihydro-6h-Pyrido[2,3-B][1,4]-Benzodiazepin-6-One moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists. (unibo.it)
The roles of the 1-, 2- and 3-ARs as well as NO were explored by using the selective antagonists CGP-20712A (300 nM), ICI -18551 (50 nM), SR59230A (100 nM) and NOS inhibitors L-NAME (50 μM) or LNNA (50 μM) respectively. (sun.ac.za)
Methods: Intravital videomicroscopy of the rat jejunum was used to record the vascular responses of inflow (termed 1A) arterioles, proximal (p3A), and distal (d3A) premucosal arterioles during exposure to isotonic glucose or mannitol solutions alone or in the presence of the selective nitric oxide synthase (NOS) inhibitor (L-NMMA), an adenosine A1 receptor antagonist (8-cyclopentyl-1,3-dipropylxanthine (DPCPX)), or a K + ATP channel inhibitor (glibenclamide). (arizona.edu)
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)
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)
A1 adenosine receptor agonist), formoterol (β2-adrenoceptor agonist) or isoprenaline (non-selective β-adrenoceptor agonist) were added before hypoxia/reoxygenation (pre-conditioning) or at the start of reoxygenation following hypoxia (post-conditioning). (ntu.ac.uk)
DPCPX4
Materials and Methods: The expression of casps3 was measured by real-time polymerase chain reaction and then flow cytometery and MTT assay were used to assess the apoptotic and proliferation cell rate after the treatment of T47D cells with specific agonist N6-cyclopentyladenosine (CPA) and antagonist 1,3-dipropyl-8-cyclopentylxanthine (DPCPX) of this receptor 24, 48, and 72 hours after treatment. (uitm.edu.my)
The effects of adenosine, adenosine A 1 receptor antagonist (DPCPX), or NMDA receptor antagonist (APV) on the spontaneous release of [ 3 H]-5- hydroxytryptamine ([ 3 H]-5-HT) during normoxic/normoglycemic or hypoxic/hypoglycemic period were studied in the rat hippocampal slices. (ewha.ac.kr)
Adenosine A 1 receptor specific antagonist, 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) exacerbate GOD-induced increase of spontaneous release of [ 3 H]-5-HT. (ewha.ac.kr)
Pre-treatment with pertussis toxin (Gi/o-protein inhibitor), DPCPX (A1 adenosine receptor antagonist) or TG2 inhibitors (Z-DON and R283) attenuated the A1 adenosine receptor-induced pharmacological pre- and post-conditioning. (ntu.ac.uk)
the A2 receptor antagonists 8-(p-sulfophenyl)theophylline, 3,7-dimethyl-1-(2-propynyl)xanthine, 1,3,7-trimethyl-8-(3-chlorostyryl)xanthine, and 3-propylxanthine, but not A1 and A3 receptor antagonists, decreased the suppressive effect of HS, indicating that HS suppresses neutrophils via A2 receptor activation. (escholarship.org)
Cheuvront SN, Ely BR, Kenefick RW, Michniak-Kohn BB, Rood JC, Sawka MN: No effect of nutritional adenosine receptor antagonists on exercise performance in the heat. (inhibitorkit.com)
T he administration of kappa-opioid receptor antagonists, nor-binaltorphimine (norBNI) and 5'-guanidinonaltrindole (GNTI) enhanced allodynia in rats and mice after sciatic nerve ligation. (opioids.wiki)
The animals were i.t. injected with norBNI, GNTI (kappa-opioid receptor antagonists), dynorphin A1-17 antiserum (DYN A/S), ketamine (NMDA receptor antagonist) and their combinations. (opioids.wiki)
Potent1
Akahane A., Katayama H., Mitsunaga T., 1999, Discovery of 6-oxo-3- (2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1(6H)-pyridazinebutanoic acid (FK 838): A novel non-xanthine adenosine A1 receptor antagonist with potent diuretic activity, J Med Chem. (ugm.ac.id)
Agonists1
7 Endothelium-dependent contractions elicited by A1 receptor agonists were blocked by indomethacin and by free radical scavengers. (uncg.edu)
Allosteric3
2009, 3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists. (wustl.edu)
Functional evaluation showed these compounds to be state-dependent antagonists which show a positive allosteric interaction. (johnshopkins.edu)
The development of a T-type calcium channel radioligand has been used to demonstrate structurally distinct TTAs interact at allosteric sites and to confirm the potential for synergistic inhibition of T-type calcium channels with structurally diverse antagonists. (johnshopkins.edu)
Inhibition2
The aim of this study was to evaluate the effect of the A1 receptor function on cell programmed death or proliferation, as well as the relationship between this receptor stimulation/inhibition and caspase 3 (casp3) expression in T47D cell line that has a mutant and non-functional P53 gene. (uitm.edu.my)
Similarly, pertussis toxin, ICI 118,551 (β2-adrenoceptor antagonist) or TG2 inhibition attenuated the isoprenaline-induced cell survival. (ntu.ac.uk)
Inhibitor2
Simultaneous application of both the NOS inhibitor and the adenosine A1 receptor antagonist gave the same reduction in glucose-induced dilation of the premucosal arterioles as the adenosine A1 receptor antagonist alone. (arizona.edu)
and a chemokine receptor type 5 antagonist, an INI, and a nonnucleoside-reverse transcriptase inhibitor (n = 1). (cdc.gov)
Ligand1
15. Ronsisvalle G., Pappalardo M.S., Prezzavento O., Marrazzo A., Caccamese S., Carboni L., Spampinato S., e-Pmtc, an opioid antagonist bivalent ligand based on N-(Phenylpropyl)-Normetazocine with very high preference for K-sites. (unibo.it)
Derivatives1
17. Minarini A., Tumiatti V., Pistacchio E., Spampinato S. , Melchiorre C., Synthesis and biological activity of 1,4 Dihydropyridine derivatives combining calcium and a1-adrenoceptor antagonistic properties. (unibo.it)
Theophylline1
Application of the A1 receptor antagonist 8-cyclo-pentyl-theophylline (200 nM) blocked the effects of adenosine. (nih.gov)
Pharmacological1
The primary aim of this study was to determine the role of TG2 in A1 adenosine receptor and β2-adrenoceptor-induced pharmacological pre- and post-conditioning in the H9c2 cells. (ntu.ac.uk)
Rats1
Both antagonists, norBNI and GNTI, significantly enhanced mechanical and therma allodynia in rats and mice with neuropathic pain. (opioids.wiki)
Pathways1
Investigation the Effect of Adenosine A1 Receptor Agonist and Antagonist on P53 Gene Expression, and Apoptosis Pathways and Rate in U87Mg Multiform Glioblastoma by: Fahimeh Zamani-Rarani, et al. (uitm.edu.my)
Gene2
Background: Adenosine receptor family, especially A1 type is-overexpressed in breast-derived tumor cells and the P53 gene is mutant in some of these cells while the casps gene is of wild type as well. (uitm.edu.my)
Interleukin-1beta and interleukin-1 receptor antagonist gene polymorphisms in Korean patients with adult-onset Still's disease. (cdc.gov)
Caffeine1
Caffeine (CAF), a nonselective adenosine A1 and A2A receptor antagonist and commonly used psychoactive substance, may affect these disorders in a dose-dependent manner. (aaem.pl)
Calcium1
Here, we radiolabel a novel amide T-type calcium channel antagonist (TTA-A1) and show that several known antagonists, including mibefradil, flunarizine, and pimozide, displace binding in a concentration-dependent manner. (johnshopkins.edu)
Activation2
renal adenosine A1 receptor activation during the renal ischemia-reperfusion injury is detrimental to renal function. (eurekamag.com)
Background: Both nitric oxide (NO) and adenosine A1 receptor activation mediate microvascular vasodilation during intestinal glucose absorption. (arizona.edu)
Functional2
Antagonists of MBT domains would serve as probes to interrogate the functional role of these proteins and initiate the chemical biology of methyl-lysine readers as a target class. (rcsb.org)
It may be from New failure( functional blood) or from resources in antagonists of the T( A1 truncal nerve). (xtenddigital.com)
Effects1
Modafinil's wakefulness-inducing effects may be mitigated by prazosin, an a1-adrenergic receptor antagonist. (targetey.com)
Protein1
These results have shown that A1 adenosine receptor and β2-adrenoceptor-induced protection against simulated hypoxia/reoxygenation occurs in a TG2 and Gi/o-protein dependent manner in H9c2 cardiomyoblasts. (ntu.ac.uk)
Kidney1
To inhibit adenosine A1 receptor in isolated pig afferent arteriole from kidney. (tocris.com)
GenBank accession numbers of the sequences used in this analysis are shown in the Table A1 . (cdc.gov)
Activity1
We have previously reported that transglutaminase 2 (TG2) activity is modulated by the A1 adenosine receptor and β2-adrenoceptor in H9c2 cardiomyoblasts. (ntu.ac.uk)
Blood1
One 10-min IPC, adenosine A1 receptor antagonist (KW-3902) also shortened the recovery time of renal blood flow (RBF) and urine flow (UF), as well as mean blood pressure (BP). (eurekamag.com)
Target1
To better understand the biological role and therapeutic potential of the target, a number of structurally diverse antagonists have been identified. (johnshopkins.edu)
Comparison1
Gamma-butyrolactone antagonism of the picrotoxin receptor: comparison of a pure antagonist and a mixed antagonist/inverse agonist. (aspetjournals.org)
Treatment1
Tamsulosin is an a1-adrenoceptor ( AR ) antagonist that has been developed for the treatment of lower urinary tract symptoms suggestive of benign prostatic. (actual-drugs.com)