Norisoboldine is an isoquinoline alkaloid which acts as an AhR agonist, and enhances the function of the adenosine A1 receptor.
MRS1177 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 0.3 nM.
Danshenol B is a diterpenoid. Danshenol B has strong aldose reductase (AR) inhibitory activity with IC50 value of 0.042μM. Danshenol B can be used for the research of diabetic related complication resulted by metabolic abnormality, such as cataracts, retinopathy, neuropathy, and nephropathy[1].
N-[(4-Aminophenyl)methyl]adenosine is a adenosine receptor inhibitor, with Ki of 29 nM for Rat ecto-5′-Nucleotidase.IC50 value: 29.0 ± 1.7 nM (Ki) Target: Adenosine Receptor
Acefylline is an adenosine receptor antagonist.
Adenosine receptor antagonist 4 (compound 2) is an adenosine A1 receptor antagonist with a Ki of 101 nM for human A1 receptor[1].
Adenosine receptor antagonist 1 is a A2aR-selective antagonist with an IC50 of 0.29 nM and displays 14-fold more selective for A2aRthan A2bR.
GP531 is a potent, second-generation adenosine regulating agent, is pharmacologically silent under basal conditions but increases localized endogenous adenosine during ischemia.
Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment.Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450)[1].Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases[2].
LUF7690 (Compound 9) is a clickable and covalent affinity-based probe (AfBP) that targets the human A3AR (hA3AR). LUF7690 can be used in the detection and characterization of the hA3AR in different types of granulocytes, among other cell types[1].
Adenosine amine congener (ADAC) is a selective A1 adenosine receptor agonist, can ameliorate noise- and Cisplatin-induced cochlear injury. Adenosine amine congener also has neuroprotective effects[1][2].
AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors.
PSB11 hydrochloride is an antagonist with reverse excitatory activity for human A3 Adenosine Receptor with high affinity (Ki=2.3 nM)[1].
Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A1/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR[1].
A2AR-agonist-1 is a potent A2AR and ENT1 agonist with Ki of 4.39 and 3.47 for A2AR and ENT1.IC50 value: 4.39 and 3.47 (Ki) [1]Target: A2AR and ENT1A2AR-agonist-1 is a novel dual-action compound, targeting the Adenosine A2A Receptor and Adenosine Transporter for Neuroprotection.[1]
N6-Cyclopentyladenosine (CPA) is a selective Adenosine A1 receptor agonist, with Ki values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively[1][2].
N6-[2-(4-Aminophenyl)ethyl]adenosine is a potent, non-selective A3 adenosine receptor agonist.Target: Adenosine receptor agonist.in vitro: N6-[2-(4-Aminophenyl)ethyl]adenosine is a non-selective agonist of the adenosine A3 receptors, at the subprotective dose of 1 mg/kg against electroconvulsions, significantly potentiates the anticonvulsive action of phenobarbital, diphenylhydantoin and valproate against maximal electroshock, being ineffective at lower doses. N6-[2-(4-Aminophenyl)ethyl]adenosine (0.0039-1 mg/kg) also enhances the protective activity of carbamazepine. N6-[2-(4-Aminophenyl)ethyl]adenosine at low doses potentiates the protective activity of Carbamazepine most likely through the A subtype of adenosine receptors. At higher doses, N6-[2-(4-Aminophenyl)ethyl]adenosine seems to enhance the anticonvulsive effect of other antiepileptics via adenosine A1 receptors. [1]in vivo: N6-[2-(4-Aminophenyl)ethyl]adenosine (2-4 mg/kg) has no significant effect on seizure parameters (seizure severity, seizure duration and afterdischarge duration) in amygdala-kindled rats. N6-[2-(4-Aminophenyl)ethyl]adenosine is combined with antiepileptic drugs administered at doses ineffective in fully kindled rats.[2]
GR79236 is a highly potent and selective adenosine A1 receptor agonist (Ki = 3.1 nM) that has analgesic and anti-inflammatory actions in humans and animals.IC50 value: 3.1 nM(Ki)Target: adenosine A1 receptorin vitro: GR79236 is a highly potent and selective A1-receptor agonist that is originally developed for the treatment of Type 2 diabetes mellitus, as a cardioprotective agent and also for peripheral arterial occlusive diseases.in vivo: GR79236 has also been shown to have antinociceptive and anti-inflammatory properties in animal models. GR79236 inhibits the release of CGRP evoked by superior sagittal sinus (SSS) stimulation in the cat and inhibits trigeminal nucleus firing in the cat and rat. GR79236X has acute, short-term analgesic efficacy.
PSB-1115 is a selective A2B Adenosine Receptor antagonist. PSB-1115 inhibits the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced contraction inhibition of acetylcholine (ACh)[1].
Regadenoson is an A2A adenosine receptor agonist that is a coronary vasodilator that is commonly used in pharmacologic stress testing.Target: A2A adenosine receptorRegadenoson produces hyperemia quickly and maintains it for a duration that is useful for radionuclide myocardial perfusion imaging. The selective nature of the drug makes it preferable to other stress agents such as adenosine, which are less selective and therefore cause more side-effects.Regadenoson has a 2 to 3 minute biological half-life.[1]
Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline sodium glycinate inhibits PDE3 activity to relax airway smooth muscle. Theophylline sodium glycinate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline sodium glycinate induces apoptosis. Theophylline sodium glycinate can be used for asthma and chronic obstructive pulmonary disease (COPD) research[1][2][3][4][5].
2'-MeCCPA is a potent and selective A1 adenosine receptors (A1AR) agonist. 2'-MeCCPA efficiently inhibits cAMP modulation in both direct pathway medium spiny neurons (dMSNs) and indirect pathway medium spiny neurons (iMSNs)[1][2].
PSB-1901 is a potent A2B adenosine receptor (A2BAR) antagonist with Kis of 0.0835 nM and 0.131 nM for human and mouse A2BARs respectively. PSB-1901 can be used for the research of cancer[1].
A3AR antagonist 2 (compound 18) is a potent Human A3 adenosine receptor antagonist with an Ki value of 4.54 nM[1].
A2B receptor antagonist 1 is a potent A2B adenosine receptor antagonist extracted from patent WO 2009157938 A1 EXAMPLE 9B.
Capadenoson is a selective agonist of adenosine-A1 receptor.
SCH-202676 hydrobromide is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 hydrobromide has antiviral activity and inhibits 3CLpro in a time-dependent manner with an IC50 value of 0.655 μM[1][2][3][4].
A2A receptor antagonist 1 is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.
LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR). IC50 value: Target: A3 adenosine receptor LUF6000 was found to be an allosteric enhancer of Emax of structurally diverse agonists at the A3 AR, being more effective for low-Emax agonists than for high-Emax agonists. LUF6000 exerted an Emax-enhancing effect at a concentration of 0.1 microM or higher, and was shown to increase the Emax of Cl-IB-MECA and other low-efficacy agonists to a larger extent than that of the high-efficacy agonist NECA. Interestingly, LUF6000 converted a nucleoside A3 AR antagonist MRS542, but not a non-nucleoside antagonist MRS1220, into an agonist.
CGS 21680 is a specific adenosine A2A receptor agonist, used for treatment of neurological disease.