a1ar

A1AR antagonist 2 (compound 18h) is a potent antagonist of the A1 adenosine receptor (AR) with Ki values of 1.49, 10.2, and 50.1 nM for hA1, hA2A, and hA2B, respectively [1].

A1AR antagonist 6 (compound 15) is a potent and selective inhibitor of the A1 adenosine receptor (A1AR), exhibiting a pKi of 7.13 and a pIC50 of 6.38[1].

A1AR antagonist 1 (compound 18g) is a potent A1 adenosine receptor (AR) antagonist with Ki values of 2.08, 6.91, and 31.2 nM for hA1, hA2A, and hA2B, respectively [1].

A1AR antagonist 5 (compound 20) is a potent and selective inhibitor of the A1 adenosine receptor (A1AR) with a pKi of 6.11 and a pIC50 of 5.83 [1].

A1AR antagonist 4 (compound 22) is a potent and selective A1 adenosine receptor (A1AR) antagonist with a pIC50 value of 5.51 and a pKi value of 6.29 [1].

A1AR antagonist 3 (compound 13) is a selective adenylate 1 (A1) receptor antagonist with an affinity for human A1 (Ki: 9.69 nM) and rat A1 (Ki: 0.529 nM). It is suitable for research on neurological diseases.

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.

XU1(Benzo[c][1,8]naphthyridin-6(5h)-One) is an Aurora protein kinase inhibitor used for the treatment of diseases suitable for inhibition, regulation or modulation of kinase signaling.

N6-Ethyladenosine, an adenosine derivative, acts as an agonist of Adenosine receptors (hA1AR and hA3AR) with Ki values of 4.9 nM and 4.7 nM, respectively.

FSCPX is a potent and selective irreversible antagonist of the A1 adenosine receptor (A1AR), exhibiting low nanomolar binding potency. It can effectively decrease the interstitial adenosine level in the guinea pig atrium, thereby modifying the effect of [NBTI], a nucleoside transport inhibitor.

MIPS521 ({2-Amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone) is a positive allosteric modulator of the A1R.

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.

CPFPX is a highly selective radioactive ligand for the A1 adenosine receptor (A1AR).

The A1, A2A, A2B, and A3 adenosine receptors (ARs) are ubiquitous G protein-coupled receptors. The four AR subtypes have been implicated in several areas of therapeutic interest such as stroke and other ischemic conditions, as well as inflammation, neurodegenerative diseases, diabetes, and sleep regulation. A3 AR antagonists are of interest as therapeutic agents in glaucoma agents and inflammation. CAY10498 is a potent and selective A3 AR antagonist exhibiting a Ki of 37 nM with 60 and 200-fold selectivity over A1 and A2A adenosine receptors, respectively. CAY10498 is also a structural analog of reversine, a dedifferentiation agent of embryonic progenitor cells. However, no dedifferentiation effects or any connection between A3 AR antagonism and dedifferentiation have been demonstrated.

A2A A1 AR antagonist-1 (compound 1a) is a potent dual antagonist with Ki values of 5.58 nM and 24.2 nM for A2A and A1 AR, respectively, demonstrating potential for ischemic stroke research [1].

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 inhibitor 2 (compound 14b) is a potent inhibitor of AR (adenosine receptor), exhibiting dual affinity towards A1 A2A ARs with higher affinity for A1- than A2A AR, and Ki values of 52.2 nM for A1 AR and 167 nM for A2A AR.

A2AAR HDAC-IN-1 (compound 14c) is an orally active, balanced dual inhibitor of A2AAR (Ki: 163.5 nM) and HDAC1 (IC50: 145.3 nM).

A2AAR HDAC-IN-2 is a potent dual A2AAR HDAC inhibitor with good affinity for A2AAR (Ki: 10.3 nM) and effective HDAC1 inhibition (IC50: 18.5 nM). A2AAR HDAC-IN-2 is applicable in anti-tumour studies.

hA2A hCA XII modulator 1 is a potent antagonist of the hA2A adenosine receptor (hA2AAR), a triazolopyrazine that acts on hA2AAR (Ki: 6.4 nM), hA1AR (Ki: 4.819 μM), and hA3AR (Ki>30 μM). hA2A hCA XII modulator 1 Also a potent inhibitor of human carbonic anhydrase XII (hCA XII), capable of acting on hCA XII (Ki: 6.2 nM), hCA II (Ki: 46 nM), hCA IX (Ki: 466 nM) and hCA I (Ki: 8.351 μM). hA2A hCA XII modulator 1 exhibits potential for cancer research.

VCP-746 is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. VCP746 reduces hypertrophy in a rat neonatal cardiac myocyte model. VCP746 is a hybrid molecule consisting of an adenosine moiety linked to an adenosine A1 receptor (A1AR) allosteric modulator moiety. At the A1AR, VCP746 mediated cardioprotection in the absence of haemodynamic side effects such as bradycardia.