a2b receptor antagonist

A2B receptor antagonist 1 (EXAMPLE 9B) is a potent A2B adenosine receptor antagonist.

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).

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

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.

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.

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.

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.

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.

adenosine A2B receptor antagonist

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

ATL-801 is anselective antagonist of A2B receptor with herapeutic activity for colitis.

ATL802 is an adenosine A2B Receptor antagonist.

Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR), exhibiting exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties, holding great promise for investigating cancer and neurodegenerative diseases [1].

Adenosine receptor antagonist 2 is an orally active A2a (IC50: 1 nM) and A2b (IC50: 3 nM) adenosine receptor antagonist with antitumor properties.

A2A receptor antagonist 3 (Example 92) is an adenosine A2A receptor antagonist (Ki: 0.4 nM) and a receptor (Ki: 1467 nM).

M1069 is a selective, orally active A2A A2B diadenosine receptor antagonist that is more than 100-fold more selective than subtypes A1 and A3. M1069 antagonizes the immunosuppressive mechanisms induced by adenosine and exhibits antitumor effects.

PSB-1901 is a potent A2B Adenosine Receptor Antagonist with Picomolar Potency (Ki 0.0835 nM, KB 0.0598 nM, human A2BAR) with >10 000-fold selectivity versus all other AR subtypes. PSB-1901 was similarly potent and selective at the mouse A2BAR, making it a promising tool for preclinical studies.

CELT-327 is a potent, selective fluorescent hA2B/A3 adenosine receptor antagonist, exhibiting K_i values of 35.6 nM at A2B and 45.7 nM at A3 receptors. It efficiently labels HCT116 cells expressing A2B adenosine receptors in a dose-dependent manner, demonstrating rapid, uniform spread and integration of fluorescence within cell monolayers. In live HCT116 spheroids, it achieves consistent staining throughout, penetrating even the deepest layers. As a fluorescent adenosine receptor probe, CELT-327 is ideal for applications in fluorescence binding assays, live cell imaging, flow cytometry, and fluorescence polarization assays, serving as an effective alternative to GPCR radiolabeling ligands. Its excitation and emission peaks are at 589 nm and 616 nm, respectively, making it suitable for TR-FRET assays as an acceptor dye, particularly in combination with the CoraFlor1 TR-FRET donor.

PSB-1115 potassium salt, a selective A2B Adenosine Receptor antagonist, inhibits the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced contraction inhibition of acetylcholine (ACh) [1].

BAY-545 is an antagonist of A2B adenosine receptor(IC50 : 59 nM).