a2b adenosine receptor

A2B receptor antagonist 1 is a small molecule antagonist and an A2B adenosine receptor antagonist with potent antagonistic activity, and can be used for research on adenosine receptor-related diseases.

MRS 1754 is a selective antagonist radioligand for the A2B adenosine receptor, exhibiting very low affinity for A1 and A3 receptors in both humans and rats.

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.

GS-6201 (CVT-6883) is a selective antagonist of the adenosine A2B receptor, demonstrating high affinity and selectivity with a Ki of 22 nM for human adenosine A2B receptors.

LAS101057 is a novel orally available and potent and selective A2B receptor antagonist for the study of asthma.

human A2B adenosine receptor antagonist

LAS38096 is an A2B adenosine receptor antagonist (Ki : 17 nM) that is potent, selective and efficient .

Alloxazine (Isoalloxazine) is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor.

ISAM-140 is a potent and highly selective antagonist of A2B adenosine receptor.

A2B receptor antagonist 2 hydrochloride is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. It has immunomodulatory activity[1].

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.

Adenosine receptor agonist2 (Compound 10) is an agonist of the adenosine A2B receptor (A2BR) with an EC50 of 0.38 nM. It significantly inhibits the accumulation of cAMP and calcium ions. Adenosine receptor agonist2 is applicable in cardiovascular protection studies.

Enprofylline (Enprofilina), a bronchodilator, acts primarily as a competitive nonselective phosphodiesterase inhibitor. Enprofylline is used in asthma, chronic obstructive pulmonary disease, and in the management of sickle cell disease, diabetic neuropathy, and cerebrovascular insufficiency.

MIPS3526 is a potent and selective A2B adenosine receptor (A2BR) agonist, exhibiting a pEC50 value of 10.17 (with an EC50 of 58 pM). It demonstrates high receptor subtype selectivity against A1R, A2AR, and A3R. MIPS3526 mitigates the stimulatory effects of angiotensin II on cardiomyocytes and fibroblasts and is useful in studying cardiovascular diseases, particularly heart failure driven by cardiac remodeling.

8-(p-Sulfophenyl)theophylline (8-SPT) (compound 2) is an adenosine A2B receptor antagonist, exhibiting a Ki value of 1330 nM for human recombinant A2B receptors.

A2A and A2B adenosine receptor partial agonist

adenosine A2B receptor antagonist

PSB-603 is a selective antagonist of Adenosine A2B receptor(Ki = 0.553 nM) with anti-inflammatory effects.

AMP-579 is an adenosine A1 receptor agonist. AMP-579 also acts as a A2b-adenosine receptor agonist in human 293 cells and rabbit hearts.

ATL802 is an adenosine A2B Receptor antagonist.

Regadenoson (CVT-3146) is an adenosine derivative and selective A2A adenosine receptor agonist with coronary vasodilating activity. Upon administration, regadenoson selectively binds to and activates the A2A adenosine receptor, which induces coronary vasodilation. This leads to an increase in coronary blood flow and enhances myocardial perfusion. Compared to adenosine, regadenoson has a longer half-life and shows higher selectivity towards the A2A adenosine receptor. This agent is a very weak agonist for the A1 adenosine receptor and has negligible affinity for the A2B and A3 adenosine receptors.

Adenosine 3'-monophosphate (sodium salt hydrate) (3'-AMP) is a nucleotide and cAMP-generating agonist that elevates cAMP levels in NG108-15 cells. Adenosine 3'-monophosphate is converted to adenosine via the A2B receptor, thereby inhibiting vascular smooth muscle cell (VSMC) proliferation.