Doxofylline-d4 is the deuterium labeled Doxofylline. Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV[1][2].
Theophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) monohydrate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) monohydrate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) monohydrate induces apoptosis. Theophylline (1,3-Dimethylxanthine) monohydrate can be used for asthma and chronic obstructive pulmonary disease (COPD) research[1][2][3][4][5].
Xanthine amine congener (XAC) hydrochloride is a non-selective adenosine receptor antagonist. Xanthine amine congener hydrochloride induces convulsions in mice[1].
Inosine-2,8-d2 is the deuterium labeled Inosine. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors[1][2][3].
Enprofylline acts as a selective and competitive A2B receptor antagonist with the Ki of 7 μM. Enprofylline also acts as a phosphodiesterase inhibitor. Enprofylline can be used for the research of asthma, chronic obstructive pulmonary disease[1][2][3].
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research[1][2][3].
ST4206 is a potent adenosine A2A antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively.
LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.
KFM19 is a potent, selective Adenosine receptor (A1-receptor) antagonist, with an IC50 of 50 nM.
ZM 241385 is a selective and high affinity A2A adenosine receptor antagonist.
Adenosine 5'-monophosphate disodium is an orally active purine nucleotide, and participates in ATP metabolism. Adenosine 5'-monophosphate disodium is also a ligand for adenosine 2B receptor. Adenosine 5'-monophosphate disodium can activate AMPK in skeletal muscle, and ameliorates insulin resistance and impaired glucose metabolism. Adenosine 5'-monophosphate disodium can be used for research of diabetes[1][2][3].
Xanthine amine congener is a non-selective adenosine receptor antagonist[1]. Xanthine amine congener induces convulsions in mice[2].
Xanthine amine congener dihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2 receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model[1].
DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes[1][2][3].
KI-7 is an A2B adenosine receptor positive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC50=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2B adenosine receptor agonist BAY 60-6583 as well as by adenosine with EC50s of 2390 nM and 2550 nM, respectively[1][2].
Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
CD73-IN-1 is an inhibitor of CD73 which can be used in the treatment of cancer extracted from patent WO 2017153952 A1, example 80.
MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system[1]. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo[2].
(±)-5'-Chloro-5'-deoxy-ENBA is an agonist of A1AR. (±)-5'-Chloro-5'-deoxy-ENBA produces hypothermia in mice[1].
Dyphylline acts as an adenosine receptor antagonist and phosphodiesterase inhibitor, which is used in the treatment of respiratory disorders.Target: Adenosine Receptor; PDEDyphylline (trade names Dilor, Lufyllin), also known as diprophylline, is a xanthine derivative with bronchodilator and vasodilator effects. It is used in the treatment of respiratory disorders like asthma, cardiac dyspnea, and bronchitis. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor.
HEMADO is a potent and selective adenosine A3 receptor agonist with a Ki of 1.1 nM at the human A3 subtype[1].
Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.
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.
GP531 is a potent, second-generation adenosine regulating agent, is pharmacologically silent under basal conditions but increases localized endogenous adenosine during ischemia.
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].
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.
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]