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).

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

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

MRS 1754 is a selective antagonist radioligand for the A2B adenosine receptor. It has a very low affinity for A1 and A3 receptors of both humans and rats.

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

human A2B adenosine receptor antagonist

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

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.

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

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.

Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR). It exhibits 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. Therefore, Adenosine receptor inhibitor 1 holds great promise for investigating cancer and neurodegenerative diseases [1].

A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist (Ki: 0.4 nM). receptor (Ki: 1467 nM).

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].

ATL802 is an adenosine A2B Receptor antagonist.

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.

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

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

Adenosine receptor antagonist 2 is an orally active A2a (IC50: 1 nM), A2b (IC50: 3 nM) adenosine receptor antagonist that exhibits antitumour effects.

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.

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

adenosine A2B receptor antagonist

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