a1

Adenosine A1 receptor activator T62 is an allosteric enhancer of the adenosine A1 receptor, producing antinociception in animal models of acute pain and reducing hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].

N6-(2-Phenylethyl)adenosine (N6-Phenethyladenosine) is an adenosine derivative and adenosine receptor agonist with Ki values of 11.8 nM for rat A1 receptors and 30.1 nM for human A1 receptors.

BAY 60-6583 is a potent, high-affinity adenosine A2B receptor agonist (EC50 = 3 nM) with affinity for A2B receptors that exceeds that for A1, A2A, and A3 receptors.BAY 60-6583 is cardioprotective in a model of myocardial ischemia.The Ki values for BAY 60-6583 binding to mouse, rabbit, and dog A2BAR were 750 nM, 340 nM, and 330 nM, respectively. The Ki values of BAY 60-6583 binding to A2BAR in mice, rabbits and dogs were 750 nM, 340 nM and 330 nM respectively.

KFM19 is a potent and selective adenosine receptor (A1-receptor) antagonist (IC50 : 50 nM) for the study of neurological disorders.

Tonapofylline is an orally active and selective antagonist of the A1 adenosine receptor (Ki: 7.4 nM for human A1). Tonapofylline can be used in studies about heart failure.

GW-493838 is a potent adenosine A1A receptor agonist for the treatment of dyslipidemia and neuropathic pain, with analgesic effects on post-herpetic neuralgia or peripheral nerve damage caused by trauma or surgery.

Sulmazole (AR-L 115-BS) is a small molecule Sulmazole is a small molecule cGMP-PDE inhibitor.Sulmazole is a competitive inhibitor of A1 adenosine receptors.Sulmazole has been shown to improve cardiac index, low pulmonary capillary wedge pressure, and can be used in the study of heart failure.Sulmazole is a small molecule cGMP-PDE inhibitor.

N 0861 is a selective adenosine A1 receptor antagonist that attenuates renal insufficiency during adenosine-controlled hypotension in rats.

Acefylline (Theophylline-7-acetic acid), a stimulant drug of the xanthine chemical class, acts as an adenosine receptor antagonist. It is combined with diphenhydramine in the pharmaceutical preparation Etanautine to help offset its stimulant effects

Proxyphylline (7-(2-Hydroxypropyl)theophylline) is a dual of adenosine A1/A2a receptor inhibitor and phosphodiesterase (PDE) inhibitor. Proxyphylline acts as a cardiac stimulant, vasodilator and bronchodilator.

2'-MeCCPA is a potent and highly selective A1 adenosine receptor (A1AR) agonist with a K-value of 1.8 nM for AR. 2'-MeCCPA inhibits trichostatin-stimulated adenylate cyclase activity with an IC value of 13.1 nM, exhibits analgesic activity, and can be used in the study of HCV.

VPC171 is a novel adenosine A1 receptor positive allosteric modulator (PAM).

Trabodenoson (INO-8875) is a selective and potent adenosine A1 receptor agonist, an adenosine analog, for the study of primary open-angle glaucoma.

Cirsimarin (Cirsitakaoside) is a flavonoid isolated from Microtea debilis. It shows a potent antilipogenic effect and decreases adipose tissue deposition in mice. Cirsimarin has antagonist activity on the adenosine A1 receptor and inhibitory effect on phosphodiesterase.

N6-Cyclohexyladenosine (CHA) is a selective agonist of A1 receptor with EC50 of 8.2 Nm. N6-Cyclohexyladenosine exerts anticonvulsant effects and protects against neuronal death. CHA was also found to inhibit the pressor effects of lumbar sympathetic nerve stimulation in rats.

CGS 15943 is an orally bioavailable non-xanthine antagonist of the Adenosine Receptor. In transfected CHO cells, its Ki values for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM, respectively.

MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1, and A3 receptors respectively. MRS-1706 is an effective and selective adenosine A2B receptor inverse agonist.

N6-Cyclopentyladenosine (CPA) is a selective agonist of the adenosine A1 receptor, mimicking its action with Ki values of 2.3 nM, 790 nM, and 43 nM for human A1, A2A, and A3 receptors, respectively. CPA is used to modulate cellular signaling, neurotransmission, and other biological processes.

Rolofylline (KW-3902) is a selective adenosine A1 receptor antagonist utilized in research on acute congestive heart failure, renal dysfunction, and neurodegenerative disorders.

Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.

CCPA (2-chloro-N(6)cyclopentyladenosine) is a potent and selective agonist of adenosine A1 receptor

DPCPX (PD 116948) is an A1 adenosine receptor antagonist

SDZ WAG 994 is an A1 adenosine receptor agonist.

Vipadenant (CEB-4520)(BIIB-014) is an adenosine A2a antagonist with Ki of 1.3 nM; less potent for A1(Ki=69 nM).