Stereoisomerism: The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Adenosine: A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.Methylation: Addition of methyl groups. In histo-chemistry methylation is used to esterify carboxyl groups and remove sulfate groups by treating tissue sections with hot methanol in the presence of hydrochloric acid. (From Stedman, 25th ed)Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Receptors, Purinergic P1: A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).Receptor, Adenosine A2A: A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Receptor, Adenosine A3: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of locations including the BRAIN and endocrine tissues. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.Receptor, Adenosine A1: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Adenosine A2 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.Chemical Industry: The aggregate enterprise of manufacturing and technically producing chemicals. (From Random House Unabridged Dictionary, 2d ed)Phosphodiesterase I: A phosphoric diester hydrolase that removes 5'-nucleotides from the 3'-hydroxy termini of 3'-hydroxy-terminated OLIGONUCLEOTIDES. It has low activity towards POLYNUCLEOTIDES and the presence of 3'-phosphate terminus on the substrate may inhibit hydrolysis.Alligators and Crocodiles: Large, long-tailed reptiles, including caimans, of the order Loricata.Pyrophosphatases: A group of enzymes within the class EC 3.6.1.- that catalyze the hydrolysis of diphosphate bonds, chiefly in nucleoside di- and triphosphates. They may liberate either a mono- or diphosphate. EC 3.6.1.-.MichiganPhosphoric Diester Hydrolases: A class of enzymes that catalyze the hydrolysis of one of the two ester bonds in a phosphodiester compound. EC 3.1.4.Liver Cirrhosis: Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.CaliforniaGlucose-6-Phosphate Isomerase: An aldose-ketose isomerase that catalyzes the reversible interconversion of glucose 6-phosphate and fructose 6-phosphate. In prokaryotic and eukaryotic organisms it plays an essential role in glycolytic and gluconeogenic pathways. In mammalian systems the enzyme is found in the cytoplasm and as a secreted protein. This secreted form of glucose-6-phosphate isomerase has been referred to as autocrine motility factor or neuroleukin, and acts as a cytokine which binds to the AUTOCRINE MOTILITY FACTOR RECEPTOR. Deficiency of the enzyme in humans is an autosomal recessive trait, which results in CONGENITAL NONSPHEROCYTIC HEMOLYTIC ANEMIA.Lysophospholipids: Derivatives of PHOSPHATIDIC ACIDS that lack one of its fatty acyl chains due to its hydrolytic removal.TetrahydrocortisolPatents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Intraocular Pressure: The pressure of the fluids in the eye.Trabecular Meshwork: A porelike structure surrounding the entire circumference of the anterior chamber through which aqueous humor circulates to the canal of Schlemm.Inventions: A novel composition, device, or process, independently conceived de novo or derived from a pre-existing model.Carbenoxolone: An agent derived from licorice root. It is used for the treatment of digestive tract ulcers, especially in the stomach. Antidiuretic side effects are frequent, but otherwise the drug is low in toxicity.TetrahydrocortisoneAqueous Humor: The clear, watery fluid which fills the anterior and posterior chambers of the eye. It has a refractive index lower than the crystalline lens, which it surrounds, and is involved in the metabolism of the cornea and the crystalline lens. (Cline et al., Dictionary of Visual Science, 4th ed, p319)Tonometry, Ocular: Measurement of ocular tension (INTRAOCULAR PRESSURE) with a tonometer. (Cline, et al., Dictionary of Visual Science, 4th ed)Ciliary Body: A ring of tissue extending from the scleral spur to the ora serrata of the RETINA. It consists of the uveal portion and the epithelial portion. The ciliary muscle is in the uveal portion and the ciliary processes are in the epithelial portion.Publications: Copies of a work or document distributed to the public by sale, rental, lease, or lending. (From ALA Glossary of Library and Information Science, 1983, p181)Quantitative Structure-Activity Relationship: A quantitative prediction of the biological, ecotoxicological or pharmaceutical activity of a molecule. It is based upon structure and activity information gathered from a series of similar compounds.Publication Bias: The influence of study results on the chances of publication and the tendency of investigators, reviewers, and editors to submit or accept manuscripts for publication based on the direction or strength of the study findings. Publication bias has an impact on the interpretation of clinical trials and meta-analyses. Bias can be minimized by insistence by editors on high-quality research, thorough literature reviews, acknowledgement of conflicts of interest, modification of peer review practices, etc.Publishing: "The business or profession of the commercial production and issuance of literature" (Webster's 3d). It includes the publisher, publication processes, editing and editors. Production may be by conventional printing methods or by electronic publishing.Periodicals as Topic: A publication issued at stated, more or less regular, intervals.Duplicate Publication as Topic: Simultaneous or successive publishing of identical or near- identical material in two or more different sources without acknowledgment. It differs from reprinted publication in that a reprint cites sources. It differs from PLAGIARISM in that duplicate publication is the product of the same authorship while plagiarism publishes a work or parts of a work of another as one's own.Bibliometrics: The use of statistical methods in the analysis of a body of literature to reveal the historical development of subject fields and patterns of authorship, publication, and use. Formerly called statistical bibliography. (from The ALA Glossary of Library and Information Science, 1983)Authorship: The profession of writing. Also the identity of the writer as the creator of a literary production.Peer Review, Research: The evaluation by experts of the quality and pertinence of research or research proposals of other experts in the same field. Peer review is used by editors in deciding which submissions warrant publication, by granting agencies to determine which proposals should be funded, and by academic institutions in tenure decisions.Journal Impact Factor: A quantitative measure of the frequency on average with which articles in a journal have been cited in a given period of time.Anticholinergic Syndrome: Adverse drug effects associated with CHOLINERGIC ANTAGONISTS. Clinical features include TACHYCARDIA; HYPERTHERMIA; MYDRIASIS, dry skin and dry mucous membranes, decreased bowel sounds and urinary retention in peripheral anticholinergic syndrome; and HALLUCINATIONS; PSYCHOSES; SEIZURES; and COMA in central anticholinergic syndrome.Lavandula: A plant genus of the LAMIACEAE family.Starch Phosphorylase: An enzyme of the PHOSPHORYLASES family that catalyzes the degradation of starch, a mixture of unbranched AMYLOSE and branched AMYLOPECTIN compounds. This phosphorylase from plants is the counterpart of GLYCOGEN PHOSPHORYLASE in animals that catalyzes the reaction of inorganic phosphate on the terminal alpha-1,4-glycosidic bond at the non-reducing end of glucans resulting in the release of glucose-1-phosphate.Diflucortolone: A topical glucocorticoid used in various DERMATOSES. It is absorbed through the skin, bound to plasma albumin, and may cause adrenal suppression. It is also administered as the valerate.Betamethasone Valerate: The 17-valerate derivative of BETAMETHASONE. It has substantial topical anti-inflammatory activity and relatively low systemic anti-inflammatory activity.South Africa: A republic in southern Africa, the southernmost part of Africa. It has three capitals: Pretoria (administrative), Cape Town (legislative), and Bloemfontein (judicial). Officially the Republic of South Africa since 1960, it was called the Union of South Africa 1910-1960.Cholinergic Antagonists: Drugs that bind to but do not activate CHOLINERGIC RECEPTORS, thereby blocking the actions of ACETYLCHOLINE or cholinergic agonists.Drug Delivery Systems: Systems for the delivery of drugs to target sites of pharmacological actions. Technologies employed include those concerning drug preparation, route of administration, site targeting, metabolism, and toxicity.Administration, Topical: The application of drug preparations to the surfaces of the body, especially the skin (ADMINISTRATION, CUTANEOUS) or mucous membranes. This method of treatment is used to avoid systemic side effects when high doses are required at a localized area or as an alternative systemic administration route, to avoid hepatic processing for example.Ophthalmic Solutions: Sterile solutions that are intended for instillation into the eye. It does not include solutions for cleaning eyeglasses or CONTACT LENS SOLUTIONS.
(1/50) Brief, repeated, oxygen-glucose deprivation episodes protect neurotransmission from a longer ischemic episode in the in vitro hippocampus: role of adenosine receptors.

1. Ischemic preconditioning in the brain consists of reducing the sensitivity of neuronal tissue to further, more severe, ischemic insults. We recorded field epsps (fepsps) extracellularly from hippocampal slices to develop a model of in vitro ischemic preconditioning and to evaluate the role of A1, A2A and A3 adenosine receptors in this phenomenon. 2. The application of an ischemic insult, obtained by glucose and oxygen deprivation for 7 min, produced an irreversible depression of synaptic transmission. Ischemic preconditioning was induced by four ischemic insults (2 min each) separated by 13 min of normoxic conditions. After 30 min, an ischemic insult of 7 min was applied. This protocol substantially protected the tissue from the irreversible depression of synaptic activity. 3. The selective adenosine A1 receptor antagonist, 8-cyclopentyl-1,3-dipropylxanthine (DPCPX, 100 nm), completely prevented the protective effect of preconditioning. The selective adenosine A2A receptor antagonist 4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phe nol (ZM 241385, 100 nm) did not modify the magnitude of fepsp recovery compared to control slices. The selective A3 adenosine receptor antagonists, 3-propyl-6-ethyl-5[ethyl(thio)carbonyl]-2-phenyl-4-propyl-3-pyridinecarboxylate (MRS 1523, 100 nm) significantly improved the recovery of fepsps after 7 min of ischemia. 4. Our results show that in vitro ischemic preconditioning allows CA1 hippocampal neurons to become resistant to prolonged exposure to ischemia. Adenosine, by stimulating A1 receptors, plays a crucial role in eliciting the cell mechanisms underlying preconditioning; A2A receptors are not involved in this phenomenon, whereas A3 receptor activation is harmful to ischemic preconditioning.  (+info)

(2/50) Pharmacological preconditioning with resveratrol: role of CREB-dependent Bcl-2 signaling via adenosine A3 receptor activation.

Recent studies demonstrated that resveratrol, a grape-derived polyphenolic phytoalexin, provides pharmacological preconditioning (PC) of the heart through a NO-dependent mechanism. Because adenosine receptors play a role in PC, we examined whether they play any role in resveratrol PC. Rats were randomly assigned to groups perfused for 15 min with 1) Krebs-Henseleit bicarbonate buffer (KHB) only; 2) KHB containing 10 microM resveratrol; 3) 10 microM resveratrol + 1 microM 8-cyclopentyl-1,3-dimethylxanthine (CPT; adenosine A(1) receptor blocker); 4) 10 microM resveratrol + 1 microM 8-(3-chlorostyryl)caffeine (CSC; adenosine A(2a) receptor blocker); 5) 10 microM resveratrol + 1 microM 3-ethyl-5-benzyl-2-methyl-4-phenylethynyl-6-phenyl-1,4-(+/-)-dihydropyridine-3,5- dicarboxylate (MRS-1191; adenosine A(3) receptor blocker); or 6) 10 microM resveratrol + 3 microM 2-(4-morpholinyl)-8-phenyl-1(4H)-benzopyran-4-one hydrochloride [LY-294002, phosphatidylinositol (PI)3-kinase inhibitor], and groups perfused with adenosine receptor blockers alone. Hearts were then subjected to 30-min ischemia followed by 2-h reperfusion. The results demonstrated significant cardioprotection with resveratrol evidenced by improved ventricular recovery and reduced infarct size and cardiomyocyte apoptosis. CPT and MRS 1191, but not CSC, abrogated the cardioprotective abilities of resveratrol, suggesting a role of adenosine A(1) and A(3) receptors in resveratrol PC. Resveratrol induced expression of Bcl-2 and caused its phosphorylation along with phosphorylation of cAMP response element-binding protein (CREB), Akt, and Bad. CPT blocked phosphorylation of Akt and Bad without affecting CREB, whereas MRS 1191 blocked phosphorylation of all compounds, including CREB. LY-294002 partially blocked the cardioprotective abilities of resveratrol. The results indicate that resveratrol preconditions the heart through activation of adenosine A(1) and A(3) receptors, the former transmitting a survival signal through PI3-kinase-Akt-Bcl-2 signaling pathway and the latter protecting the heart through a CREB-dependent Bcl-2 pathway in addition to an Akt-Bcl-2 pathway.  (+info)

(3/50) Activation of A3 adenosine receptors attenuates lung injury after in vivo reperfusion.

BACKGROUND: A3 adenosine receptor (AR) activation worsens or protects against renal and cardiac ischemia-reperfusion (IR) injury, respectively. The aims of the current study were to examine in an in vivo model the effect of A3AR activation on IR lung injury and investigate the mechanism by which it exerts its effect. METHODS: The arterial branch of the left lower lung lobe in intact-chest, spontaneously breathing cats was occluded for 2 h and reperfused for 3 h (IR group). Animals were treated with the selective A3 receptor agonist IB-MECA (300 microg/kg intravenously) given 15 min before ischemia or with IB-MECA as described, with pretreatment 15 min earlier with the selective A3AR antagonist MRS-1191, the nonsulfonylurea adenosine triphosphate-sensitive potassium channel-blocking agent U-37883A, or the nitric oxide synthase inhibitor N-nitro-l-arginine benzyl ester. RESULTS: IB-MECA markedly (P < 0.01) reduced the percentage of injured alveoli (IR, 48 +/- 4%; IB-MECA, 18 +/- 2%), wet:dry weight ratio (IR, 8.2 +/- 0.4; IB-MECA, 4 +/- 2), and myeloperoxidase activity (IR, 0.52 +/- 0.06 U/g; IB-MECA, 0.17 +/- 0.04 U/g). This protective effect was completely blocked by pretreatment with the selective A3AR antagonist MRS-1191 and the adenosine triphosphate-sensitive potassium channel blocking agent U-37883A but not the nitric oxide synthase inhibitor N-nitro-l-arginine benzyl ester. CONCLUSIONS: In the feline lung, the A3AR agonist IB-MECA confers a powerful protection against IR lung injury. This effect is mediated by a nitric oxide synthase-independent pathway and involves opening of adenosine triphosphate-sensitive potassium channels. Therefore, selective activation of A3AR may be an effective means of protecting the reperfused lung.  (+info)

(4/50) A3 adenosine receptor activation inhibits cell proliferation via phosphatidylinositol 3-kinase/Akt-dependent inhibition of the extracellular signal-regulated kinase 1/2 phosphorylation in A375 human melanoma cells.

Adenosine exerts its effects through four subtypes of G-protein-coupled receptors: A(1), A(2A), A(2B), and A(3). Stimulation of the human A(3) receptor has been suggested to influence cell death and proliferation. The phosphatidylinositide-3-OH kinase (PI3K)/Akt and the Raf/mitogen-activated protein kinase (MAPK/ERK) kinase (MEK)/mitogen-activated protein kinase (MAPK) pathways have central roles in the regulation of cell survival and proliferation. Due to their importance, the cross-talk between these two pathways has been investigated. Here, we show that the A(3) adenosine receptor agonist Cl-IB-MECA stimulates PI3K-dependent phosphorylation of Akt leading to the reduction of basal levels of ERK1/2 phosphorylation, which in turn inhibits cell proliferation. The response to Cl-IB-MECA was not blocked by A(1), A(2A), or A(2B) receptor antagonists, although it was abolished by A(3) receptor antagonists. Furthermore, the response to Cl-IB-MECA was generated at the cell surface, since the inhibition of A(3) receptor expression, by using small interfering RNA, abolished agonist effects. Using A375 cells, we show that A(3) adenosine receptor stimulation results in PI3K-dependent phosphorylation of Akt, leading to the reduction of basal levels of ERK1/2 phosphorylation, which in turn inhibits cell proliferation.  (+info)

(5/50) Resveratrol-mediated activation of cAMP response element-binding protein through adenosine A3 receptor by Akt-dependent and -independent pathways.

A recent study documented a role of adenosine A(3)-Akt-cAMP response element-binding protein (CREB) survival signaling in resveratrol preconditioning of the heart. In this study, we demonstrate that resveratrol-mediated CREB activation can also occur through an Akt-independent pathway. Isolated rat hearts were perfused for 15 min with Krebs-Henseleit bicarbonate (KHB) buffer containing resveratrol in the absence or presence of adenosine A(3) receptor blocker MRS-1191 [3-ethyl-5-benzyl-2-methyl-4-phenylethynyl-6-phenyl-1,4-(+/-)-dihydropyridine-3,5 -dicar-boxylate], phosphatidylinositol 3 (PI3)-kinase inhibitor LY294002 [2-(4-morpholinyl)-8-phenyl-1(4H)-benzopyran-4-one hydrochloride], mitogen-activated extracellular signal-regulated protein kinase inhibitor PD098059 [2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one], or a combination of LY294002 and PD098059. All hearts were subsequently subjected to 30-min ischemia followed by 2-h reperfusion. Cardioprotection was examined by determining infarct size, cardiomyocyte apoptosis, and ventricular recovery. Resveratrol phosphorylated both Akt and CREB that was blocked by MRS-1191, which also abolished cardioprotective abilities of resveratrol. LY294002 completely inhibited Akt phosphorylation but partially blocked the phosphorylation of CREB. Inhibition of PI3-kinase also partially blocked resveratrol's ability to precondition the heart. PD098059 partially blocked the phosphorylation of CREB and resveratrol-mediated cardioprotection. Preperfusing the hearts with LY294002 and PD098059 together completely abolished the phosphorylation of CREB, simultaneously inhibiting resveratrol-mediated cardioprotection. The results indicate that resveratrol preconditions the hearts through adenosine A(3) receptor signaling that triggers the phosphorylation of CREB through both Akt-dependent and -independent pathways, leading to cardioprotection.  (+info)

(6/50) Phosphatidylinositol 3-kinase and ERK1/2 are not involved in adenosine A1, A2A or A3 receptor-mediated preconditioning in rat ventricle strips.

Mitogen-activated protein kinase kinase (MEK)/extracellular signal-regulated kinase 1 and 2 (ERK1/2) and phosphatidylinositol 3-kinase (PI3-kinase)/protein kinase B (PKB; also known as Akt) are important antiapoptotic signalling pathways which have recently been implicated in cardioprotection. However, at present the involvement of ERK1/2 and PI3-kinase/PKB in adenosine receptor-mediated cardioprotection is poorly understood. In this study we used isolated rat right ventricular strips, contracted by electrical-field stimulation, in order to investigate the role of ERK1/2 and PI3-kinase/PKB in adenosine receptor-induced cardioprotection. Ventricle strips were pretreated for 2 min with the agonists adenosine (non-selective), CPA (A1 selective), CGS 21680 (A2A selective) and Cl-IB-MECA (A3 selective) before 30 min hypoxia followed by 30 min reoxygenation. Each agonist significantly improved posthypoxic percentage contraction recovery compared to control strips. Similarly hypoxic preconditioning (10 min hypoxia followed by 20 min reoxygenation) significantly improved posthypoxic percentage contraction recovery compared to non-preconditioned strips. The selective adenosine receptor antagonists DPCPX (A1), ZM 241385 (A2A) and MRS 1220 (A3) attenuated cardioprotection induced by CPA, CGS 21680 and Cl-IB-MECA, respectively. Pre-incubation (30 min) of ventricle strips with the MEK1 inhibitor PD 98059 (50 microM) or the PI3-kinase inhibitor wortmannin (100 nM) significantly reduced posthypoxic percentage contraction recovery induced by hypoxic preconditioning. In contrast, PD 98059 and wortmannin had no significant effect on cardioprotection induced by CPA, Cl-IB-MECA or CGS 21680. Overall these data indicate that although selective A1, A2A and A3 adenosine receptor agonists induce preconditioning in rat right ventricular strips the effects are independent of ERK1/2- and PI3-kinase-dependent pathways. In contrast ERK1/2 and PI3-kinase-dependent pathways do appear to be involved in early hypoxic preconditioning.  (+info)

(7/50) "Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.

The dedifferentiation agent "reversine" [2-(4-morpholinoanilino)-N(6)-cyclohexyladenine 2] was found to be a moderately potent antagonist for the human A(3) adenosine receptor (AR) with a K(i) value of 0.66 microM. This result prompted an exploration of the structure-activity relationship of related derivatives, synthesized via sequential substitution of 6-chloro-2-fluoropurine with selected nucleophiles. Optimization of substituents at these two positions identified 2-(phenylamino)-N(6)-cyclohexyladenine (12), 2-(phenylamino)-N(6)-cycloheptyladenine (19), and 2-phenylamino-N(6)-endo-norbornyladenine (21) as potent A(3) AR ligands with K(i) values of 51, 42, and 37 nM, respectively, with 30-200-fold selectivity in comparison to A(1) and A(2A) ARs. The most selective A(3) AR antagonist (>200-fold) was 2-(phenyloxy)-N(6)-cyclohexyladenine (22). 9-Methylation of 12, but not 19, was well-tolerated in A(3) AR binding. Extension of the 2-phenylamino group to 2-benzyl- and 2-(2-phenylethylamino) reduced affinity. In the series of 2-(phenylamino), 2-(phenyloxy), and 2-(phenylthio) substitutions, the order of affinity at the A(3) AR was oxy > or = amino > thio. Selected derivatives, including reversine (K(B) value of 466 nM via Schild analysis), competitively antagonized the functional effects of a selective A(3) AR agonist, i.e., inhibition of forskolin-stimulated cAMP production in stably transfected Chinese hamster ovary (CHO) cells. These results are in agreement with other studies suggesting the presence of a lipophilic pocket in the AR binding site that is filled by moderately sized cycloalkyl rings at the N(6) position of both adenine and adenosine derivatives. Thus, the compound series reported herein comprise an important new series of selective A(3) AR antagonists. We were unable to reproduce the dedifferentiation effect of reversine, previously reported, or to demonstrate any connection between A(3) AR antagonist effects and dedifferentiation.  (+info)

(8/50) The cross-species A3 adenosine-receptor antagonist MRS 1292 inhibits adenosine-triggered human nonpigmented ciliary epithelial cell fluid release and reduces mouse intraocular pressure.

PURPOSE: Antagonists to A3 adenosine receptors (ARs) lower mouse intraocular pressure (IOP), but extension to humans is limited by species variability. We tested whether the specific A3AR antagonist MRS 1292, designed to cross species, mimicks the effects of other A3AR antagonists on cultured human nonpigmented ciliary epithelial (NPE) cells and mouse IOP. METHODS: NPE cell volume was monitored by electronic cell sorting. Mouse IOP was measured with the Servo-Null Micropipette System. RESULTS: Adenosine triggered A3AR-mediated shrinkage of human NPE cells. Shrinkage was blocked by MRS 1292 (IC50 = 42 +/- 11 nM, p < 0.01) and by another A3AR antagonist effective in this system, MRS 1191. Topical application of the A3AR agonist IB-MECA increased mouse IOP. MRS 1292 reduced IOP by 4.0 +/- 0.8 mmHg at 25-microM droplet concentration (n = 10, p < 0.005). CONCLUSIONS: MRS 1292 inhibits A3AR-mediated shrinkage of human NPE cells and reduces mouse IOP, consistent with its putative action as a cross-species A3 antagonist.  (+info)

*  Adenosine receptor
Newer adenosine receptor agonists and antagonists are much more potent and subtype-selective, and have allowed extensive ... The role of A3 receptor is less defined in this field. Studies have shown that it plays a role in the downregulation of ... The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as endogenous ... Br J Pharmacol 170(6):1167-1176 "Entrez Gene: ADORA2A adenosine A2A receptor". Jacobson KA, Gao ZG (2006). "Adenosine receptors ...
*  Adenosine A3 receptor
... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ... adenosine receptor". Mol. Pharmacol. 63 (5): 1021-31. doi:10.1124/mol.63.5.1021. PMID 12695530. "Adenosine Receptors: A3". ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ...
*  Reversine
... is known to act as an antagonist of the adenosine A3 receptor. Reversine is a potent inhibitor of the mitotic kinase ...
*  KF-26777
... is a drug which acts as a potent and selective antagonist for the adenosine A3 receptor, with sub-nanomolar affinity ( ... a new potent and selective adenosine A3 receptor antagonist". European Journal of Pharmacology. 444 (3): 133-41. doi:10.1016/ ... Baraldi PG, Tabrizi MA, Gessi S, Borea PA (January 2008). "Adenosine receptor antagonists: translating medicinal chemistry and ... A3 Ki=0.2nM) and high selectivity over the other three adenosine receptor subtypes. Simple xanthine derivatives such as ...
*  PSB-10
... is a drug which acts as a selective antagonist for the adenosine A3 receptor (ki value at human A3 receptor is 0.44 nM ... Müller CE (2003). "Medicinal chemistry of adenosine A3 receptor ligands". Current Topics in Medicinal Chemistry. 3 (4): 445-62 ... a novel high-affinity antagonist radioligand for human A(3) adenosine receptors". Bioorg Med Chem Lett. 12 (3): 501-3. doi: ... "Adenosine receptor subtype-selective antagonists in inflammation and hyperalgesia". Naunyn-Schmiedeberg's Archives of ...
*  Adenosine A2A receptor
3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists". Journal of Medicinal Chemistry. 46 (7 ... Older research on adenosine receptor function, and non-selective adenosine receptor antagonists such as aminophylline, focused ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ... The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it. This ...
*  Adenosine A2B receptor
2001). "Differential gene expression of adenosine A1, A2a, A2b, and A3 receptors in the human enteric nervous system". J. Comp ... Cacciari B, Pastorin G, Bolcato C, Spalluto G, Bacilieri M, Moro S (December 2005). "A2B adenosine receptor antagonists: recent ... The adenosine A2B receptor, also known as ADORA2B, is a G-protein coupled adenosine receptor, and also denotes the human ... "The A2b adenosine receptor mediates cAMP responses to adenosine receptor agonists in human intestinal epithelia". J. Biol. Chem ...
*  Caffeine
... is an antagonist at all four adenosine receptor subtypes (A1, A2A, A2B, and A3), although with varying potencies. The ... this is a receptor complex with 1 adenosine A1 receptor and 1 dopamine D1 receptor) and the A2A-D2 receptor heterotetramer ( ... this is a receptor complex with 2 adenosine A2A receptors and 2 dopamine D2 receptors). The A2A-D2 receptor heterotetramer has ... a receptor complex composed of 1 adenosine A1 receptor and 1 adenosine A2A receptor) in the axon terminal of glutamate neurons ...
*  Theophylline
... and reduces inflammation and innate immunity nonselective adenosine receptor antagonist, antagonizing A1, A2, and A3 receptors ... Daly JW, Jacobson KA, Ukena D (1987). "Adenosine receptors: development of selective agonists and antagonists". Prog Clin Biol ... asthma infant apnea Blocks the action of adenosine; an inhibitory neurotransmitter that induces sleep, contracts the smooth ...
*  Caffeine-induced anxiety disorder
Caffeine acts as an antagonist of adenosine A1 and A2A receptors. Adenosine is a normal neuromodulator that activates adenosine ... There are four well-known adenosine receptors found in the body, A1, A2A, A2B, and A3. The endogenous agonist for these ... Caffeine has been proven to act as an antagonist on adenosine receptors, which acts as a stimulant and therefore fulfills this ... Caffeine also has an excitatory effect on mesocortical cholinergic neurons by acting as an antagonist on adenosine receptors ...
*  Methoctramine
... such as nicotinic ACh receptors -at micromolar concentrations- or adenosine A3. The exact effects of methoctramine still remain ... Watson, N.; Barnes, P.J.; Maclagan, J. (1992). "Actions of methoctramine, a muscarinic M2 receptor antagonist, on muscarinic ... Gallamine triethiodide M2 receptor Muscarinic receptor Acetylcholine Jakubik, Jan; Zimcik, Pavel; Randakova, Alena; Fuksova, ... Hence, the presence of the antagonist methoctramine provokes an increase of the heart rate. In marked contrast of the above, ...
*  Adenosine
All adenosine receptor subtypes (A1, A2A, A2B, and A3) are G-protein-coupled receptors. The four receptor subtypes are further ... This is being contended and it is now considered a relative contraindication (however, selective adenosine antagonists are ... Cellular signaling by adenosine occurs through four known adenosine receptor subtypes (A1, A2A, A2B, and A3). Extracellular ... The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ...
*  Adenosine diphosphate receptor inhibitor
"Anti-platelet therapy: ADP receptor antagonists". British Journal of Clinical Pharmacology. 72 (4): 647-657. doi:10.1111/j.1365 ... 157 (1): 148.e1-148.e5. doi:10.1016/j.ahj.2008.09.017. Drepper, Michael D; Spahr, Laurent; Frossard, Jean Louis (2012-05-14). " ... P2Y12 receptor is a G-coupled receptor and is activated by adenosine diphosphate. ADP binds to the P2Y12 receptor that leads to ... Adenosine diphosphate (ADP) receptor inhibitors are a drug class of antiplatelet agents, used in the treatment of acute ...
*  Multiple electrode aggregometry
The antagonist reagent is used together with TRAP-test, and allows assessment of a positive control. Prostaglandin E1 (PGE1) is ... Thrombin receptor activating peptide-6 (TRAP-6) activates platelets through the thrombin receptor protease activated receptor-1 ... Adenosine diphosphate (ADP) is a platelet agonist. When it is added to saline-diluted whole blood in the test cuvette, it ... The GPIIb/IIIa antagonist blocks the binding of fibrinogen to the GPIIb/IIIa receptors, preventing the formation of platelet- ...
*  Hydrogen potassium ATPase
Björklund O, Shang M, Tonazzini I, Daré E, Fredholm BB (2008). "Adenosine A1 and A3 receptors protect astrocytes from hypoxic ... H2-receptor antagonists, like cimetidine (Tagamet), inhibit the signaling pathway that leads to activation of the ATPase. This ... eCollection 2015 Gessi S, Merighi S, Stefanelli A, Fazzi D, Varani K, Borea PA (2013). "A(1) and A(3) adenosine receptors ... Memory has been associated with astrocytes and the alpha3 subunit of adenosine receptor found in hydrogen/Sodium-potassium ...
*  Purinergic signalling
... leading to an accumulation of adenosine. On the other hand, the adenosine-receptor antagonist caffeine reverses the anti- ... On the other hand, nanomolar concentrations of adenosine activate A1 and A3 receptors, resulting in neutrophilic chemotaxis ... In the airways of patients with asthma, the expression of adenosine receptors is upregulated. Adenosine receptors affect ... the expression of adenosine receptors on the neutrophil, and the affinity of these receptors for adenosine. Micromolar ...
*  Adrenergic receptor
Antagonists may be used primarily in hypertension, anxiety disorder, and panic attacks. The α2 receptor couples to the Gi/o ... 81 (1): 211.e1-7. doi:10.1016/j.urology.2012.09.011. PMID 23200975. Fitzpatrick D, Purves D, Augustine G (2004). "Table 20:2". ... "Convergence of major physiological stimuli for renin release on the Gs-alpha/cyclic adenosine monophosphate signaling pathway ... a Gq coupled receptor) and α2 (a Gi coupled receptor). Phenylephrine is a selective agonist of the α receptor. β receptors have ...
*  Prostaglandin EP3 receptor
These Receptor antagonist, which block EP3 from responding to PGE2 or other agonists of this receptor, include Sulprostone, DG- ... Prostaglandin E1 (PGE1), which has one less double bond than PGE2, has the same binding affinity and potency for EP3 as PGE2. ... and pathways that inhibit adenyl cyclase which thereby lowers cellular levels of cyclic adenosine monophosphate (cAMP) to ... Eicosanoid receptor Prostaglandin E2 receptor 1 (EP1) Prostaglandin E2 receptor 2 (EP2) Prostaglandin E2 receptor 4 (EP4) ...
*  History of catecholamine research
J. W. Black; A. F. Crowther; R. G. Shanks; A. C. Dornhorst (1964). "A new adrenergic beta-receptor antagonist". The Lancet. 283 ... A. Vulpian (1856). "Note sur quelques réactions propres à la substance des capsules surrénales". Comptes Rendus de l'Académie ... In addition the vesicles contained adenosine triphosphate (ATP), with a molar noradrenaline:ATP ratio in sympathetic nerve ... he called alpha adrenotropic receptor (now α-adrenoceptor or α-adrenergic receptor), while the receptor with the second rank ...
*  Arachidonate 5-lipoxygenase
Montelukast, Zafirlukast, and Pranlukast are receptor antagonists for the Cysteinyl leukotriene receptor 1 which contributes to ... Leukotriene-A4 hydrolase), or are the cellular receptors responsible for mediating the cellular responses to the down-stream ... may serve as a mobile lid over ALOX5's substrate-binding site An Adenosine triphosphate (ATP) binding site; ATP is crucial for ... as well as of LTC4 and LTD4 receptor antagonists have proven inferior to corticosteroids as single drug therapy for persistent ...
*  Cannabinoid receptor type 1
Endogenous CB1 antagonist and CB2 agonist) Rimonabant Taranabant Lipoxin A4 - endogenous, PAM ZCZ-011 - PAM Pregnenolone - ... Through its primary action as a Gi coupled receptor, CB1 inhibits production of cyclic adenosine monophosphate (cAMP), ... Discovery and development of Cannabinoid Receptor 1 Antagonists Cannabinoid receptor Cannabinoid receptor type 2 (CB2) GRCh38: ... As a consequence, CB1 receptor antagonists can reduce drug seeking behavior in some addicts. The CB1 receptor is expressed by a ...
*  Cannabinoid receptor type 2
Cannabinoid receptor agonists reduce gut motility in IBS patients. Application of CB2-specific antagonists has found that these ... CB2 receptor agonists cause a reduction in the intracellular levels of cyclic adenosine monophosphate (cAMP). Although the ... 11: e3. doi:10.1017/S1462399409000957. PMC 2768535 . PMID 19152719. Galiègue S, Mary S, Marchand J, Dussossoy D, Carrière D, ... Unlike the CB1 receptor, in the brain, CB2 receptors are found primarily on microglia. The CB2 receptor is expressed in some ...
*  Mechanism of anoxic depolarization in the brain
... involve sigma-1 receptor ligands, to modulate Ca2+ release, NMDA receptor antagonists, to prevent Ca2+ overload, and ion ... This compensatory stimulation of glycolysis occurs because, in the turtle's brain, cytochrome a and a3 have a low affinity for ... the turtle's brain reduces its ATP consumption by suppressing its neuronal activity and gradually releasing adenosine. This re- ... They include the NMDA receptors, AMPA receptors, P2X7 purinergic receptors, pannexin channels (Panx1), transient receptor ...
*  Portopulmonary hypertension
2005;128:164-8 Wilkins et al.Sildenafil versus Endothelin Receptor Antagonist for Pulmonary Hypertension (SERAPH) study. Am J ... Prostacyclin and Prostaglandin E1: Molecular mechanisms and therapeutic utility. Prog Hemostasis Thrombosis 1991;10:307-37 Vane ... Another drug, Milrinone, a Type 3 PDE-i increases vascular smooth muscle adenosine-3,5-cyclic monophosphate concentrations to ... Use of a mixed endothelin receptor antagonist in portopulmonary hypertension: a safe and effective therapy? Gastroenterology. ...
*  12-Hydroxyheptadecatrienoic acid
Hicks, A; Monkarsh, S. P.; Hoffman, A. F.; Goodnow Jr, R (2007). "Leukotriene B4 receptor antagonists as therapeutics for ... subsequent studies showed that it was a high affinity receptor for the arachidonic acid metabolite, lipoxin A4, but also bound ... to inhibit platelet aggregation responses to various agents by stimulating platelets to raise their levels of Cyclic adenosine ... BLT1 receptor) and its low affinity BLT2 receptor (Kd=23 nM); both receptors are G protein coupled receptors that, when ligand- ...
*  Cannabidiol
... has been found to act as an antagonist of GPR55, a G protein-coupled receptor and putative cannabinoid receptor ... is most likely associated with an increase in the extracellular adenosine offer and signaling through adenosine A2A receptor. ... "Cannabis à faible teneur en THC et CBD". bag.admin.ch. Retrieved May 20, 2017. ... Cannabidiol has very low affinity for the cannabinoid CB1 and CB2 receptors but acts as an indirect antagonist of these ...
Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A3...  Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A3...
... antagonists (1-3) selected from 4-acylamino-6-alkyloxy-2-alkylthiopyrimidines previously investigated by us were modified by ... Three A3 adenosine receptor (AR) antagonists (1-3) selected from 4-acylamino-6-alkyloxy-2-alkylthiopyrimidines previously ... of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A3 adenosine receptor ... of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A3 adenosine receptor B. Cosimelli ...
more infohttp://pubs.rsc.org/en/content/articlelanding/2018/md/c7md00375g
Synthesis, Biological Properties, and
Molecular Modeling Investigation of the
First Potent, Selective, and
Water-Soluble Human...  Synthesis, Biological Properties, and Molecular Modeling Investigation of the First Potent, Selective, and Water-Soluble Human...
... and Water-Soluble Human A3 Adenosine Receptor Antagonist ... K B value 3 Adenosine Receptor Antagonist CHO cells hA 3 ... A new, highly potent, selective, and water-soluble antagonist of the hA,sub,3,/sub, adenosine receptor was synthesized and ... Adenosine Receptor Antagonist. 2002-07-16T00:00:00Z (GMT) by Anna Maconi Giorgia Pastorin Tatiana Da Ros Giampiero Spalluto ... adenosine receptor First Potent Schild analysis K i 0.01 nM hA 3 receptor Molecular Modeling Investigation pyrimidine ...
more infohttps://figshare.com/articles/Synthesis_Biological_Properties_and_Molecular_Modeling_Investigation_of_the_First_Potent_Selective_and_Water-Soluble_Human_A_sub_3_sub_Adenosine_Receptor_Antagonist/3681432/1
CellAura fluorescent adenosine A3 antagonist [XAC] |CA200645 | Adenosine receptor antagonist | Hello Bio  CellAura fluorescent adenosine A3 antagonist [XAC] |CA200645 | Adenosine receptor antagonist | Hello Bio
... high quality Adenosine receptor antagonist from Hello Bio, a trusted supplier for life science researchers worldwide ... Buy CellAura fluorescent adenosine A3 antagonist [XAC] - an affordable, ... Fluorescent Adenosine A3 receptor Antagonist (A3-633-AN), A3-633-AN ... Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide- ...
more infohttps://www.hellobio.com/cellaura-fluorescent-adenosine-a3-antagonist-xac.html
Psoriasis: KOL Insight [2018]  Psoriasis: KOL Insight [2018]
10.2 Adenosine A3 receptor (A3AR) antagonists. *10.2.1 Piclidenoson (CF101; Can-Fite Biopharma) ...
more infohttps://www.giiresearch.com/report/dgpl372760-psoriasis-kol-insight.html
Reversine - Wikipedia  Reversine - Wikipedia
Reversine is known to act as an antagonist of the adenosine A3 receptor. Reversine is a potent inhibitor of the mitotic kinase ...
more infohttps://en.wikipedia.org/wiki/Reversine
Briddon SJ[au] - PubMed - NCBI  Briddon SJ[au] - PubMed - NCBI
Antagonist selective modulation of adenosine A1 and A3 receptor pharmacology by the food dye Brilliant Black BN: evidence for ... Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides ... Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide- ... Agonist-occupied A3 adenosine receptors exist within heterogeneous complexes in membrane microdomains of individual living ...
more infohttps://www.ncbi.nlm.nih.gov/pubmed?cmd=search&term=Briddon+SJ%5Bau%5D&dispmax=50
Adenosine A₃ Receptor Antagonist, MRS 1523 - CAS 212329-37-8 - Calbiochem CAS 212329-37-8 | 119152  Adenosine A₃ Receptor Antagonist, MRS 1523 - CAS 212329-37-8 - Calbiochem CAS 212329-37-8 | 119152
Adenosine A₃ Receptor Antagonist, MRS 1523 - CAS 212329-37-8 - Calbiochem CAS 212329-37-8 - Find MSDS or SDS, a COA, data ... Adenosine A₃ Receptor Antagonist, MRS 1523 - CAS 212329-37-8 - Calbiochem. 119152 Sigma-AldrichAdenosine A₃ Receptor Antagonist ... Adenosine A₃ Receptor Antagonist, MRS 1523 - CAS 212329-37-8 - Calbiochem: Malzeme Güvenlik Bilgi Formu (MSDS) veya SDS, Analiz ... A pyridine derivative that acts as a highly selective antagonist of A3 receptor with excellent potency in both humans and ...
more infohttp://www.merckmillipore.com/TR/tr/product/Adenosine-A3-Receptor-Antagonist-MRS-1523-CAS-212329-37-8-Calbiochem,EMD_BIO-119152
Adenosine A3 receptor - Wikipedia  Adenosine A3 receptor - Wikipedia
... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ... adenosine receptor". Mol. Pharmacol. 63 (5): 1021-31. doi:10.1124/mol.63.5.1021. PMID 12695530. "Adenosine Receptors: A3". ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ...
more infohttps://en.wikipedia.org/wiki/Adenosine_A3_receptor
A G Protein-Coupled Receptor Dimer Imaging Assay Reveals Selectively Modified Pharmacology of Neuropeptide Y Y1/Y5 Receptor...  A G Protein-Coupled Receptor Dimer Imaging Assay Reveals Selectively Modified Pharmacology of Neuropeptide Y Y1/Y5 Receptor...
2014) Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides ... For two Y1 receptor heterodimer combinations (with the Y4 receptor or β2-adrenoceptor), agonist and antagonist pharmacology was ... 2011) Allosteric interactions across native adenosine-A3 receptor homodimers: quantification using single-cell ligand-binding ... Y1 receptor (Z11504), Y4 receptor (NM_005972), Y5 receptor (NM_006174), β2-adrenoceptor (β2AR) (NM_000024), and D2 dopamine ...
more infohttp://molpharm.aspetjournals.org/content/87/4/718
Mechanisms and Therapeutic Implications of Asthma Circadian Rhythm | Bentham Science  Mechanisms and Therapeutic Implications of Asthma Circadian Rhythm | Bentham Science
A3 Adenosine Receptor Antagonists. Mini-Reviews in Medicinal Chemistry. * Respiratory Syncytial Virus and Asthma in Twin ... The Potential of Selected Prostanoid Receptors as Targets in a New Therapeutic Strategy for Allergy and Immune Diseases. ...
more infohttp://www.eurekaselect.com/79725/article/mechanisms-and-therapeutic-implications-asthma-circadian-rhythm?tracking-code=4
Kumar P[au] - PubMed - NCBI  Kumar P[au] - PubMed - NCBI
Therapeutic Potential of Agonists and Antagonists of A1, A2a, A2b And A3 Adenosine Receptors. ...
more infohttps://www.ncbi.nlm.nih.gov/pubmed?cmd=search&term=Kumar+P%5Bau%5D&dispmax=50
Abstracts -  FIP - International Pharmaceutical Federation  Abstracts - FIP - International Pharmaceutical Federation
Pharmacokinetics of lj-2698, a potent human a3 adenosine receptor antagonist, in rats ... Double maintenance dose of clopidogrel is associated with reduction in adenosine diphosphate induced aggregation ...
more infohttp://www.fip.org/?page=abstracts&action=favoriteaddlist&item=19936
Abstracts -  FIP - International Pharmaceutical Federation  Abstracts - FIP - International Pharmaceutical Federation
Pharmacokinetics of lj-2698, a potent human a3 adenosine receptor antagonist, in rats ... Double maintenance dose of clopidogrel is associated with reduction in adenosine diphosphate induced aggregation ...
more infohttp://www.fip.org/?page=abstracts&action=favoriteaddlist&item=19912
Acorn Biomedical : Leading Candidate  Acorn Biomedical : Leading Candidate
Adenosine A3 receptor (A3AR) antagonists are a novel oral treatment for glaucoma. Acorn Biomedical is developing first-in-class ... The A3AR subtype is the most recently characterized member of the adenosine receptor family. Adenosine levels have been found ... A3AR antagonists physiologically decrease inflow of aqueous humor by inhibiting Cl- channels of the NPE at the aqueous surface ... Various A3AR antagonists had been identified, yet none exhibited similar levels of specificity and selectivity for both the ...
more infohttp://acornbio.com/pipeline/acn1052.html
Federal Register
       :: 
      Prospective Grant of Start-Up Exclusive Evaluation Option License Agreement: A3 Adenosine...  Federal Register :: Prospective Grant of Start-Up Exclusive Evaluation Option License Agreement: A3 Adenosine...
5. U.S. Patent Application 13/371,081, filed February 10, 2012, titled "A3 Adenosine Receptor Agonists And Antagonists" [HHS ... 7. U.S. Provisional Application 62/033,723, filed August 6, 2014, titled "A3 Adenosine Receptor Agonists" [HHS Ref. No. E-210- ... 1. U.S. Patent 8,735,407, issued May 27, 2014, titled "Purine Derivatives As A3 Adenosine Receptor-Selective Agonists" [HHS Ref ... 6. U.S. Provisional Application 61/909,742, filed November 27, 2013, titled "A3 Adenosine Receptor Agonists" [HHS Ref. No. E- ...
more infohttps://www.federalregister.gov/documents/2014/12/09/2014-28749/prospective-grant-of-start-up-exclusive-evaluation-option-license-agreement-a3-adenosine-receptor
Journal of Alzheimers Disease - Volume 47, issue 1 - Journals - IOS Press  Journal of Alzheimer's Disease - Volume 47, issue 1 - Journals - IOS Press
... cholesterol internalization and a specific adenosine A3 receptor (A3 R) antagonist as well as siRNA knockdown of A3 Rs mimicked ... and the A3 R antagonist as well as siRNA knockdown of A3 Rs mimicked the effects of caffeine on AβPP surface expression. ... Caffeine, Through Adenosine A 3 Receptor-Mediated Actions, Suppresses Amyloid-β Protein Precursor Internalization and Amyloid-β ... Keywords: Adenosine A_3 receptor, Alzheimer's disease, amyloid-β , amyloid-β protein precursor, caffeine, endocytosis, LDL ...
more infohttps://content.iospress.com/journals/journal-of-alzheimers-disease/47/1
Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis | Journal of Pharmacology and Experimental...  Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis | Journal of Pharmacology and Experimental...
However, PAT-505 did display marginal inhibition of radiolabeled agonist or antagonist binding to the adenosine A3 receptor, ... MT1 melatonin receptor, prostaglandin E2 EP4 receptor, 5-HT5a serotonin receptor, and GABA-gated Cl− channel with 50%-70% ... The angiotensin II receptor antagonist telmisartan is used as a positive control. PAT-505 dosed from weeks 6 to 12 had no ... 2010) A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. Br J Pharmacol 160 ...
more infohttp://jpet.aspetjournals.org/content/360/1/1.long
Ophthalmic composition - Patent application  Ophthalmic composition - Patent application
0034]For the adenosine A3 receptor antagonist/THC formulation, the adenosine A3 receptor antagonist is preferably a 1,2,4 ... The preferred adenosine A3 receptor antagonist is a 1,2,4-triazolo-(1,5c)pyrimidine. [0016]Tetrahydrocortisol, especially the 3 ... 7. A composition of claim 1 where the Rho-kinase inhibitor is Y 27632 and the adenosine A3 receptor antagonist is a 1,2,4 ... The novel ophthalmic formulations of the invention comprise about 0.2 to 5% (w/w) of the adenosine A3 receptor antagonist, ...
more infohttp://www.patentsencyclopedia.com/app/20100105643
Adenozinski A3 receptor - Википедија, слободна енциклопедија  Adenozinski A3 receptor - Википедија, слободна енциклопедија
... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ... Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptor". Journal of Molecular ... N-dialkyluronamides as human A3 adenosine receptor antagonists". Bioorganic & Medicinal Chemistry Letters. 18 (5): 1612-6. PMID ... Entrez Gene: ADORA3 adenosine A3 receptor".. *^ Silverman MH, Strand V, Markovits D, Nahir M, Reitblat T, Molad Y, Rosner I, ...
more infohttps://sr.wikipedia.org/wiki/Adenozinski_A3_receptor
Nox4 Antibody (NB110-58849): Novus Biologicals  Nox4 Antibody (NB110-58849): Novus Biologicals
Renoprotective Effects of a Highly Selective A3 Adenosine Receptor Antagonist in a Mouse Model of Adriamycin-induced ... Critical role of X-box binding protein 1 in NADPH oxidase 4-triggered cardiac hypertrophy is mediated by receptor interacting ... Deletion of angiotensin II type 1 receptor gene or scavenge of superoxide prevents chronic alcohol-induced aortic damage and ... Glucagon-like peptide-1 receptor agonist ameliorates renal injury through its anti-inflammatory action without lowering blood ...
more infohttps://www.novusbio.com/products/nox4-antibody_nb110-58849
Antileukotriene Drugs: Clinical Application, Effectiveness and Safety | Bentham Science  Antileukotriene Drugs: Clinical Application, Effectiveness and Safety | Bentham Science
A3 Adenosine Receptor Antagonists. Mini-Reviews in Medicinal Chemistry. * The Many Faces of Glutathione Transferase Pi. Current ... By competitive binding to the Cys-LT1 receptor, leukotriene receptor antagonist drugs such as montelukast, zafirlukast, and ... By competitive binding to the Cys-LT1 receptor, leukotriene receptor antagonist drugs such as montelukast, zafirlukast, and ... Current Role of Leukotriene Receptor Antagonists in Preschool Asthma. Current Respiratory Medicine Reviews ...
more infohttp://www.eurekaselect.com/59600/article
Psoriasis and Psoriatic Arthritis: Harnessing the Potential of Targeted Therapies  Psoriasis and Psoriatic Arthritis: Harnessing the Potential of Targeted Therapies
Furthermore, other mechanisms of action (such as janus kinase [JAK] inhibitors and adenosine A3 receptor antagonists) are being ...
more infohttps://www.xcenda.com/insights/htaq-fall-2016-psoriasis-and-psoriatic-arthritis-targeted-therapies
Receptor Pharmacology and Signal Transduction - FIGON Dutch Medicines Days | 1-2 October, 2018  Receptor Pharmacology and Signal Transduction - FIGON Dutch Medicines Days | 1-2 October, 2018
Receptor Pharmacology and Signal Transduction Room: BACH 1-2Time: 10:30 - 12:30Chairs: Martine Smit, Amalia Dolga, Ingrid ... A covalent antagonist for the human adenosine A3 receptor. Xue Yang - Leiden University ... In this session the latest research in the field of receptor pharmacology and signal transduction will be presented. It is a ... Intracellular Irreversible Probes for GPCRs: A Covalent, Negative Allosteric Modulator for CC Chemokine Receptor 2 (CCR2) ...
more infohttps://www.figondmd.nl/blog/receptor-pharmacology-and-signal-transduction
Identification of a Potent and Selective Pharmacophore for Cdc25 Dual Specificity Phosphatase Inhibitors. | Molecular...  Identification of a Potent and Selective Pharmacophore for Cdc25 Dual Specificity Phosphatase Inhibitors. | Molecular...
4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists. J Med Chem 42:706-721. ... 1999) Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, ...
more infohttp://molpharm.aspetjournals.org/content/61/4/720?ijkey=0e998b2c5ed4658960f88418a62cee6748a4fa3c&keytype2=tf_ipsecsha
Browse by Authors and Editors - Nottingham ePrints  Browse by Authors and Editors - Nottingham ePrints
... of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor ... Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes. EMBO reports, 14 (8). ...
more infohttp://eprints.nottingham.ac.uk/view/people/Corriden=3ARoss=3A=3A.html
  • As a consequence of the progress in the area of kinin receptors, specific kinin receptor antagonists will be available in near future in order to provide more selective therapeutic modalities for the treatment of diseases such as asthma, cardiovascular diseases, inflammation, pain, etc. (eurekaselect.com)
  • These two receptors also have important roles in the brain, regulating the release of other neurotransmitters such as dopamine and glutamate, while the A2B and A3 receptors are located mainly peripherally and are involved in processes such as inflammation and immune responses. (wikipedia.org)
  • Heteromers consisting of adenosine A1/A2A, dopamine D2/A2A and D3/A2A, glutamate mGluR5/A2A and cannabinoid CB1/A2A have all been observed, as well as CB1/A2A/D2 heterotrimers, and the functional significance and endogenous role of these hybrid receptors is still only starting to be unravelled. (wikipedia.org)
  • The A2A receptor is also expressed in the brain, where it has important roles in the regulation of glutamate and dopamine release, making it a potential therapeutic target for the treatment of conditions such as insomnia, pain, depression, drug addiction and Parkinson's disease. (wikipedia.org)
  • As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. (wikipedia.org)
  • Nociceptin is thought to be an endogenous antagonist of dopamine transport that may act either directly on dopamine or by inhibiting GABA to affect dopamine levels. (wikipedia.org)
  • In contrast, Beta-1 adrenergic receptors are coupled only to Gs, and stimulation of these results in a more diffuse cellular response. (wikipedia.org)
  • Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists. (nih.gov)
  • They exert important pharmacological effects by interaction with at least two different receptors: Cys-LT1 and Cys-LT2. (eurekaselect.com)
  • As these "classical" opioid receptors were identified 30 years earlier in the mid-1960s, the physiological and pharmacological characterization of NOP as well as therapeutic development targeting this receptor remain decades behind. (wikipedia.org)
  • A non-sedating ophthalmic antihistamine that antagonizes histamine H1 receptors (IC 50 = 1.58 nM) and prevents the release of pro-inflammatory mediators from mast cells and eosinophils. (thomassci.com)
  • Recent publications demonstrate that adenosine A3 receptor antagonists (SSR161421) could have therapeutic potential in bronchial asthma (17,18). (wikipedia.org)
  • Several commonly used opioid drugs including etorphine and buprenorphine have been demonstrated to bind to nociceptin receptors, but this binding is relatively insignificant compared to their activity at other opioid receptors in the acute setting (however the non-analgesic NOPr antagonist SB-612,111 was demonstrated to potentiate the therapeutic benefits of morphine). (wikipedia.org)
  • Through their Gβγ subunits, CB2 receptors are also known to be coupled to the MAPK-ERK pathway, a complex and highly conserved signal transduction pathway, which critically regulates a number of important cellular processes in both mature and developing tissues. (wikipedia.org)
  • Activation of NOP's canonical β-arrestin pathway causes receptor phosphorylation, internalization, and eventual downregulation and recycling. (wikipedia.org)
  • We applied this BiFC system to study example neuropeptide Y (NPY) Y1 receptor dimers. (aspetjournals.org)
  • The G i -coupled Y receptors for neuropeptide Y (NPY), peptide YY (PYY), and pancreatic polypeptide (PP) illustrate particular possibilities for heterodimers. (aspetjournals.org)
  • Recent research, however, led to find the mentioned specialty dubious, rising the possibility of it binding to other types of receptors, such as nicotinic ACh receptors -at micromolar concentrations- or adenosine A3. (wikipedia.org)
  • The primitive P2X receptors of unicellular organisms often share low sequence similarity with those in mammals, yet they still retain micromolar sensitivity to ATP. (wikipedia.org)
  • Beta-2 adrenergic receptor has been shown to interact with: AKAP12, OPRD1, Grb2, SNX27 and SLC9A3R1. (wikipedia.org)
  • As with the A1, the A2A receptors are believed to play a role in regulating myocardial oxygen consumption and coronary blood flow. (wikipedia.org)
  • The A2A receptor is responsible for regulating myocardial blood flow by vasodilating the coronary arteries, which increases blood flow to the myocardium, but may lead to hypotension. (wikipedia.org)
  • For instance, both A1 receptors and A2A play roles in the heart, regulating myocardial oxygen consumption and coronary blood flow, while the A2A receptor also has broader anti-inflammatory effects throughout the body. (wikipedia.org)
  • The A1, together with A2A receptors of endogenous adenosine play a role in regulating myocardial oxygen consumption and coronary blood flow. (wikipedia.org)
  • Stimulation of the A1 receptor has a myocardial depressant effect by decreasing the conduction of electrical impulses and suppressing pacemaker cell function, resulting in a decrease in heart rate. (wikipedia.org)
  • Adenosine is used as an adjunct to thallous (thallium) chloride TI 201 or Tc99m myocardial perfusion scintigraphy (nuclear stress test) in patients unable to undergo adequate stress testing with exercise. (wikipedia.org)
  • Although α receptors are less sensitive to epinephrine, when activated at pharmacologic doses, they override the vasodilation mediated by β-adrenoreceptors because there are more peripheral α1 receptors than β-adrenoreceptors. (wikipedia.org)
  • Originally it was thought that the CB2 receptor was only expressed in peripheral tissue while the CB1 receptor is the endogenous receptor on neurons. (wikipedia.org)
  • Initial investigation of CB2 receptor expression patterns focused on the presence of CB2 receptors in the peripheral tissues of the immune system and found CB2 receptor mRNA is found throughout tissues of the spleen, tonsils, and thymus gland. (wikipedia.org)
  • Presynaptically, it reduces synaptic vesicle release while post synaptically it has been found to stabilize the magnesium on the NMDA receptor. (wikipedia.org)
  • By competitive binding to the Cys-LT1 receptor, leukotriene receptor antagonist drugs such as montelukast, zafirlukast, and pranlukast, block the effects of Cys-LTs and alleviate the symptoms of many chronic diseases, especially bronchial asthma and allergic rhinitis. (eurekaselect.com)