The enhancement of dopamine D1 receptor desensitization by adenosine A1 receptor activation.

 attenuated dopamine D(1) receptor desensitization.

Adenosine inhibits basolateral ClC-K2/b chloride channel in the collecting duct intercalated cells.

 on ClC-K2/b was abolished in the presence of A1R blocker, 

Inhibition of the hypercapnic ventilatory response by adenosine in the retrotrapezoid nucleus in awake rats

 on breathing was blunted by prior RTN injection of a broad spectrum adenosine receptor blocker (8‐PT) or a selective A1‐receptor blocker (

Endogenous adenosine release is involved in the control of heart rate in rats.

injections of (i) atropine, (ii) propranolol, (iii) caffeine, (iv) 8 cyclopentyl-1,3-dipropylxanthine 

), or (v) dipyridamole to increase the plasma concentration of 

Would calcium or potassium channels be responsible for cardiac arrest produced by adenosine and ATP in the right atria of Wistar rats?

, a selective adenosine A1 receptor antagonist.

A1 adenosine receptor modulation of chemically and electrically evoked lumbar locomotor network activity in isolated newborn rat spinal cords

 depressed this reflex and pulse train-evoked bouts of alternating fictive locomotion; this inhibition was reversed by 1 μM 

Absence of adenosine A1 receptors unmasks pulses of insulin release and prolongs those of glucagon and somatostatin.

 was counteracted by 100 nM of the A(1)R antagonist 

Adenosine A1 and A2a receptors modulate insulinemia, glycemia, and lactatemia in fetal sheep.

 (n = 6) augmented the glycemic and lactatemic responses of 

Selective Deletion of the A1 Adenosine Receptor Abolishes Heart-Rate Slowing Effects of Intravascular Adenosine In Vivo

Moreover, pre-treatment with a specific A1AR antagonist 

) attenuated the heart-rate slowing effects of 

 in wild-type, A2AAR−/−, or A2BAR−/− mice, but did not alter hemodynamic responses of A1AR−/− mice.

Suppression of GABA input by A1 adenosine receptor activation in rat cerebellar granule cells

 (DPCPX), but not by other P1 and P2 receptor antagonists, indicating that it was mediated by activation of A1 adenosine receptors.

Adenosine modulates excitatory synaptic transmission and suppresses neuronal death induced by ischaemia in rat spinal motoneurones

 significantly decreased the frequency of miniature excitatory postsynaptic currents (mEPSCs) in almost all neurones examined that could be mimicked by an A1 receptor agonist, N6-cyclopentyladenosine (CPA), and inhibited by an A1 receptor antagonist, 8-cyclopentyl-1, 3-dipropylxanthine (

 increased mEPSC frequency in the presence of 

Developmental changes of purinergic control of intestinal motor activity during metamorphosis in the African clawed frog, Xenopus laevis.

 induced relaxation before, during, and after metamorphosis, which was blocked by the A(1)-receptor antagonist 1,3-dipropyl-8-cyclopentylxanthine (

Role of adenosine receptor subtypes in rat jejunum in unfed state versus glucose-induced hyperemia.

 (DPCPX) (200 nm), and the A2b receptor antagonist, alloxazine (… and reactivity of the inflow and premucosal arterioles to 

, whereas the selective A2a receptor antagonist 8-(3-chlorostyryl)caffeine (CSC) (200 nm) … arteriole diameter and only slightly reduced the premucosal arteriolar sensitivity to adenosine.

[Action of AMP579 and adenosine on potassium or sodium ionic channels in isolated rat and guinea pig ventricular myocytes].

 (PD116948), can abolish the effects of AMP579 and 

 on I(to), demonstrating that the effect is mediated by adenosine A1 receptor.

[Adenosine reduces intracellular free calcium concentration in guinea pig ventricular myocytes].

 (1 micromol/L) significantly reduced the effects of 

 (100 micromol/L) in high K+ Tyrode's solution.

Evidence for both adenosine A1 and A2A receptors activating single vagal sensory C‐fibres in guinea pig lungs

 (0.1 μm) or the selective A2A antagonist SCH 58261 (0.1 μm) partially inhibited the nodose C‐fibre activation by 

, and the combination of both antagonists almost completely inhibited the response.

Adenosine reverses the stimulatory effect of angiotensin II on the renal Na+-ATPase activity through the A2 receptor

Incubation of Ang II-stimulated enzyme with 10(-6)M

, in the presence of the A1 receptor antagonist 

 (10(-6)M), completely reverses the Ang II-induced effect bringing the Na+-ATPase activity to the basal level.

: 1) the inhibitory effect of Ado is abolished by the A2 receptor selective antagonist DMPX (10(-8)M); 2) the effect induced by Ado …(-6)M cAMP; 4) Ado stimulates PKA activity; 5) the inhibitory effect induced by this nucleoside is reversed by the PKA inhibitor peptide.

Novel Mitogenic Effect of Adenosine on Coronary Artery Smooth Muscle Cells: Role for the A1 Adenosine Receptor

 is mimicked by NECA, CCPA, and R-PIA, but not by CGS21680 and 2-Cl-IB-MECA, and is inhibited by 

, indicating a prominent role for the A1 receptor.

Pharmacological characterisation of the adenosine receptor mediating increased ion transport in the mouse isolated trachea and the effect of allergen challenge

 concentration–effect curve only at 1 μM. The mixed A2A/A2B receptor antagonist 4‐(2‐[7‐amino‐2‐(2‐furyl)[1,2,4]triazolo[… 241385) also caused rightward shift of the adenosine concentration–effect curve, again only at micromolar concentrations, suggestive of the involvement of A2B receptors.

Adenosine A1-receptor modulation of glutamate-induced calcium influx in rat retinal ganglion cells.

 (10 microM) inhibited calcium channel currents by 43%, and again this effect was blocked by 

 was blocked by the A(1)-R antagonist 8-cyclopentyl-1,3-dipropylxanthine (

), but not by the A(2)-R antagonist 3,7-dimethyl-1-propargylxanthine (DMPX).

Adenosine acting via A1 receptors, controls the transition to status epilepticus-like behaviour in an in vitro model of epilepsy

, acting via its A1 receptor, exerted powerful inhibitory effects to prevent the spontaneous progression to LRDs while the potent A1 receptor antagonist, 

, accelerated the progression in a concentration dependent manner.

Effects of adenosine on optic nerve head circulation in rabbits.

Co-administration of the specific adenosine A(1) receptor antagonist,

 (DPCPX, 10 nmol) significantly suppressed (P=0.006, ANOVA) the increase in the ONH blood flow induced by 

Modulatory Role of Adenosine Receptors in Insect Motor Nerve Terminals

Stable adenine nucleotides inhibit [3H]-noradrenaline release in rabbit brain cortex slices by direct action at presynaptic adenosine A1-receptors

 (DPCPX, 10 nmol/l) shifted the concentration-response curves of 

, ATPyS, β,γ-imido-ATP and β,γ-methylene-ATP to the right by very similar degrees.

The receptor mechanism mediating the contractile response to adenosine on lung parenchymal strips from actively sensitised, allergen-challenged Brown Norway rats

 and theophylline, at concentrations which inhibit the A1 A2A and/or A2B receptors but have negligible affinity for the rat A3 receptor, inhibited responses to 

, but high concentrations were required and blockade was incomplete.

 were partially blocked by the 5-HT receptor antagonist, methysergide, or the A1 receptor antagonist, 

, and abolished in the presence of both antagonists.

Convergent control of synaptic GABA release from rat dorsal horn neurones by adenosine and GABA autoreceptors

 were blocked by the A1 receptor antagonist 8‐cyclopentyl‐1,3‐dipropylxanthine (

Endogenous adenosine reduces glutamatergic output from rods through activation of A2-like adenosine receptors.

 (DPCPX), and A2A antagonist, ZM-241385, but not the A3 antagonist, VUF-5574, inhibited effects of 

Adenosine inhibits calcium channel currents via A1 receptors on salamander retinal ganglion cells in a mini‐slice preparation

 on calcium channel current … antagonist 8‐cyclopentyltheophylline (

, 1–10 µm), but not by the A2 antagonist 3‐7‐dimethyl‐1‐propargylxanthine (DMPX, 10 µm), and was mimicked … N 6‐cyclohexyladenosine (CHA, 1 µm) but not by the A2 agonist 5′‐(N‐cyclopropyl) carbox‐amidoadenosine (CPCA, 1 µm).

Effect of purinergic agonists and antagonists on insulin secretion from INS-1 cells (insulinoma cell line) and rat pancreatic islets.

 (100 microM), an adenosine (A1) receptor antagonist, inhibited the inhibitory effects of both 

[The activation of A1 adenosine receptors attenuates myocardial stunning in the rabbit].

 was given in presence of an A1 receptor selective antagonist (

), LVDP reached 50 +/- 2% (P < 0.05 vs. control).

Adenosine A(1) and A(2A) receptors modulate sleep state and breathing in fetal sheep.

 and ZM-241385 eliminated the inhibitory effects of 

Adenosine A3 agonist cardioprotection in isolated rat and rabbit hearts is blocked by the A1 antagonist DPCPX.

The A1 antagonist 8-cyclopentyl-1,3-dipropylxanthine 

, 100 nM) blocked the beneficial effects of Cl-IB-MECA (51 +/- 5%) and 

Ameliorative effects of paeoniflorin, a major constituent of peony root, on adenosine A1 receptor-mediated impairment of passive avoidance performance and long-term potentiation in the hippocampus.

, at the concentration (0.1 microM) that had no effect on PS amplitudes or LTP induction, significantly reversed the suppressive effects of 

[Adenosine inhibits spontaneous and glutamate induced discharges of hippocampal CA1 neurons].

2) Both Ado non selective receptor antagonist 8 phenyltheophylline (8-PT, 0.5 mmol/L) and Ado selective A1 receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine 

, 50 nmol/L), completely blocked the inhibitory effects of 

 (200 nmol/L) and Gli (7 mmol/L) were all capable of abolishing the inhibiting effect of 

Adenosine modulates the (Na(+)+K(+))ATPase activity in malpighian tubules isolated from Rhodnius prolixus.

 decreases the (Na(+)+K(+)) ATPase specific activity by 88%, in a dose-dependent manner, with maximal effect at a concentration of 10(-9) M. …) at 10(-8) M, an agonist for A(1) adenosine receptor, and was reversed by 10(-9) M 8-cyclopentyl-1,3-dipropylxanthine (

Increased sensitivity of neonate atrial myocytes to adenosine A1 receptor stimulation in regulation of the L-type Ca2+ current.

 was antagonized by an A1 adenosine receptor antagonist, 

Adenosine receptor subtypes and vasodilatation in rat skeletal muscle during systemic hypoxia: a role for A1 receptors

 also reduced both the increase in FVC induced by hypoxia and that induced by 

; the control responses to these stimuli were comparable in magnitude and both were reduced by ∼50%.

Afferent arteriolar adenosine A2a receptors are coupled to KATP in in vitro perfused hydronephrotic rat kidney.

 elicited a transient vasoconstriction blocked by 

 (DPCPX), and 10-30 microM adenosine reversed KCl-induced vasoconstriction.

Effect of intracarotid administration of adenosine on the activity of area postrema neurons in barodenervated rats.

3) Selective A1 adenosine receptor antagonist,

 (DPCPX, 50 micrograms/kg), blocked the effect of 

Extracellular adenosine increases Na+/I− symporter gene expression in rat thyroid FRTL-5 cells

 on NIS mRNA levels, is mimicked by N6-(L-2-…) adenosine (PIA), an A1 adenosine receptor agonist, and inhibited by 

, an A1 adenosine receptor antagonist, suggesting that the effect is … via the A1 adenosine receptor stimulation in FRTL-5 cells.

Functional studies in atrium overexpressing A1‐adenosine receptors

 and R‐PIA in transgenic atria could be blocked by the A1‐adenosine receptor antagonist 

Sensitization of visceral afferents to bradykinin in rat jejunum in vitro

 was blocked by the A1 receptor antagonist 

 (10 μm) but remained unaffected by A2A receptor blockade with ZM241385 (10 μm).

Adenosine A1 receptor‐mediated excitation of nociceptive afferents innervating the normal and arthritic rat knee joint

The A1 antagonist 8‐cyclopentyl‐1,3‐dipropylxanthine 

, CPA, and the delayed increase seen after ATP, indicating that excitation of the nociceptive afferents was mediated via adenosine A1 receptors.

Adenosine and ADP prevent apoptosis in cultured rat cerebellar granule cells

 is partly inhibited by …-cyclopentyl-1,3-dipropylxanthine (

) and is mimicked by the A1AR agonist 2-chloro-N6-cyclopentyladenosine (CCPA), while ADP effect, that is completely blocked by … noncompetitive antagonist suramine, is restored in the presence of the selective P2x purinoceptors agonist beta, gamma-methylene-L-ATP.

Adenosine receptor-mediated inhibition of neurite outgrowth from cultured sensory neurons is via an A1 receptor and is reduced by nerve growth factor.

The antagonist studies revealed that activation of A1 adenosine receptors is primarily … effect on neuritogenesis since the inclusion of 1 or 10 microM

 (8-cyclopentyl-1,3-dipropyl … prevented the inhibitory activity of 

 or CHA whereas DMPX (3,7-dimethyl-… xanthine) did not prevent inhibition by CHA.

[Effects of intraventricular injection of adenosine on renal sympathetic nerve activity].

The renal sympathoexcitatory response to intraventricular injection of

 was completely inhibited by pretreatment with a selective A1-receptor antagonist (

Effector mechanism of adenosine in acute ischemic preconditioning of skeletal muscle against infarction.

Endogenous Adenosine Mediates the Presynaptic Inhibition Induced by Aglycemia at Corticostriatal Synapses

The presynaptic inhibitory effects induced by

 and aglycemia were both antagonized either by the nonselective adenosine receptor antagonist caffeine (2.5 mm) or by the A1 receptor antagonists 8-cyclopentyl-1,3-dimethylxanthine (CPT, 1 μm) and 

Evidence against a major role of adenosine in oxygen-dependent regulation of erythropoietin in rats.

, rats were treated with the non-specific … theophylline, the selective ADO A1 receptor blockers 

 and KW-3902, the selective ADO A2 receptor blocker DMPX, and AOPCP, an inhibitor of …'-ectonucleotidase, an ADO generating enzyme that is expressed on the surface of EPO producing cells.

Presynaptic GABAB and adenosine A1 receptors regulate synaptic transmission to rat substantia nigra reticulata neurones

 (1 mm) completely blocked the inhibitory effects of 

Adenosine uptake and deamination regulate tonic A2a receptor facilitation of evoked [3H]acetylcholine release from the rat motor nerve terminals

 (30 microM) reduction of evoked [3H]acetylcholine release was prevented after pretreatment with 

 (2.5 nM); when applied at high concentrations (100-500 microM), adenosine consistently increased evoked [3H]acetylcholine release in a PD 115,199 (25 nM)-sensitive manner.

Concentration-response relationships for adenosine agonists during preconditioning of rabbit cardiomyocytes.

 produced a broad concentration-protection curve which was displaced to the right by 

Pharmacological probes for A1 and A2 adenosine receptors in vivo in feline pulmonary vascular bed.

The selective A1 adenosine receptor … xanthine amine congener (XAC) and

 (DP-CPX) significantly antagonize … vasoconstrictor responses of 

 and R-PIA at low baseline PV tone while having less effect on … vasodilator responses of adenosine, 2-CADO, and R-PIA at elevated PV tone.

Purinergic agonists stimulate the secretion of endothelin‐1 in rat thyroid FRTL‐5 cells

 was inhibited by the P1‐receptor antagonist 8‐cyclopentyl‐1,3‐dipropylxanthine (

), and in the presence of adenosine deaminase the adenosine‐ and ATP‐mediated ET‐1 secretion was abolished.

Adenosine activates A2 receptors to inhibit neutrophil adhesion and injury to isolated cardiac myocytes.

In contrast, inhibition of cell adhesion by

 (IC50 = 4 +/- 1 nM) and attenuated by N6-cyclopentyladenosine, suggesting that occupancy of A1 receptors can conversely increase cell adhesion.

Are negative chronotropic and inotropic responses to adenosine differentiated at the receptor or postreceptor levels in isolated dog hearts?

 (DPCPX, 10-300 nmol), dose-dependently inhibited the negative chronotropic and inotropic responses to 

, CAD and NECA in the isolated, perfused right atrium.

 also blocked the negative inotropic responses to 

, CAD and NECA in the isolated left ventricle.

Effects of adenosine on norepinephrine and acetylcholine release from guinea pig right atrium: Role of A1-receptors

 (10 nM) prevented the inhibitory effect of 

, indicating that A1-purinoceptors are involved in this action.

Endogenous adenosine reduces depression of cardiac function induced by beta-adrenergic stimulation during low flow perfusion.

The incidence of arrhythmias observed upon restoration of control flow was increased by ISO when the action of endogenous

Hypoxic changes in rat locus coeruleus neurons in vitro.

 did not alter the firing, but antagonized the effect of 

Effect of Ado A1- and A2-receptor activation on ventricular fibrillation during hypoxia-reoxygenation.

 (DPCPX, 1 microM), attenuated (from 100% to 20%) VF induced by 

Excitatory and Inhibitory Effects of A1 and A2A Adenosine Receptor Activation on the Electrically Evoked [3H]Acetylcholine Release from Different Areas of the Rat Hippocampus

 (5 µM) on [3H]ACh release was prevented by the A1 antagonist 1,3‐dipropyl‐8‐cyclopentylxanthine (

; 50 nM) in the three hippocampal areas and was converted in an excitatory effect in the CA3 and dentate gyrus areas.

Synergistic effects of angiotensin and adenosine in the renal microvasculature.

 to the bath significantly blunted the constrictor effect of angiotensin II (10(-8) M), 2) presence of the converting enzyme … by 10(-6) M adenosine, 3) simultaneous administration of submaximal constrictor doses of angiotensin II (10(-10) M) and 

 (10(-6) M) produced … effect in this preparation.

Characterization of the adenosine receptors of the rat superior cervical ganglion

 and PAA were antagonized by the A1‐selective antagonist, 8‐cyclopentyl‐1,3‐dipropylxanthine (

) but not by the A2‐selective antagonist, 3,7‐dimethyl‐1‐propargylxanthine (DMPX).

The P1-purinoceptors that mediate the prejunctional inhibitory effect of adenosine on capsaicin-sensitive nonadrenergic noncholinergic neurotransmission in the rat mesenteric arterial bed are of the A1 subtype.

In addition, the selective A1 receptor antagonist,

Comparison of the actions of adenosine at pre‐ and postsynaptic receptors in the rat hippocampus in vitro.

The A1 receptor antagonist 8‐cyclopentyl‐1,3‐dipropylxanthine 

, bath applied at 200 nM) blocked the pre‐ and postsynaptic actions of 

Contribution of adenosine to isoproterenol-stimulated prostacyclin production in rabbit heart.

 enhanced dP/dt(max) and HR and prevented the decrease by 

 and DCCA of the isoproterenol-induced increase in HR and dP/dt(max); the increase by DCCA but not the decrease by adenosine in 6-keto-PGF1 alpha output was abolished.

Differential effect of basolateral and apical adenosine on AVP-stimulated cAMP formation in primary culture of IMCD.

), an adenosine antagonist with selectivity for the A1 receptor, prevented the inhibitory effects of 

, CHA, and NECA on AVP-stimulated cAMP formation.(ABSTRACT TRUNCATED AT 250 WORDS)

Dual modulation by adenosine of gastrin release from canine G-cells in primary culture.

 was reversed by the preferential A1-receptor antagonist 1,3-dipropyl-8-cyclopentylxanthine (

) as well as by the nonselective adenosine receptor antagonist 8-phenyltheophylline (8-PT).

The effects of adenosine on the development of long-term potentiation

 (1,3-dipropyl-8-cyclopentyl-xanthine), a selective antagonist of adenosine A1 receptors, was present.

 (DPCPX), and 10-30 μM adenosine reversed KCl-induced vasoconstriction.

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Possible Interaction: Adenosine and 1,3-Dpcpx

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Adenosine

1,3-Dpcpx

Research Papers that Mention the Interaction