a2a

A2A receptor antagonist 2 is a highly selective and potent antagonist of the adenosine A2Areceptor (IC50: 8.3 nM).

A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.

A2A/A1 AR antagonist-1 (compound 1a) has the potential for ischemic stroke research which is potent A 2A /A 1 AR dual antagonist with Ki s of 5.58 and 24.2 nM, respectively [1].

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

Compound 23, designated as A2A/A3 AR antagonist-1, is a dual fluorescent ligand targeting A2A and A3 adenosine receptors (AR), exhibiting dissociation constants (Ki) of 90 nM for hA2A AR and 31.8 nM for hA3 AR, respectively [1].

A2AR-agonist-1 (N-(2-(1H-Indol-3-yl)ethyl)adenosine) is a potent A2AR and ENT1 agonist (Ki: 4.39 and 3.47 for A2AR and ENT1. It targets the Adenosine A2A Receptor and Adenosine Transporter for Neuroprotection.

Istradefylline (KW-6002)(Ki of 2.2 nM) is a selective adenosine A2A receptor (A2AR) antagonist, which is under development in Phase 3 trails. It has been used in trials studying the treatment and basic science of Drug Abuse, Sleep Disorder, Hepatic Impairment, Parkinson's Disease, and Restless Legs Syndrome, among others.

Amp579 TFA is a novel adenosine A1/A2a receptor agonist that induces acute and delayed preconditioning against myocardial shock in vivo.

Apadenoson TFA is a potent adenosine A2A receptor (A2AR) agonist that can be used to improve survival in patients infected with SARS.

Evodenoson (ATL313) is a potent and selective adenosine A2a receptor (A2aR) agonist for the treatment of eye diseases, tumors, and immune system disorders, and may be used in studies of open-angle glaucoma and blood tumors.

RWJ-51204 is a selective adenosine A2A receptor antagonist and a partial agonist of GABA(A) receptor (IC50: 0.2-2 nM). It has neuroprotective and movement-improving effects and can be used in research related to Parkinson's disease.

Pyrazolo[1,5-a]pyrimidine 4h is a morpholine derivative that is a selective antagonist of the adenosine A2A receptor. It has been shown to be neuroprotective in animal models of Parkinson's disease and Huntington's chorea.

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

ST 1535 is a potent and orally active antagonist of A2A adenosine receptor with antiparkinsonian activity and antitremorigenic effects. ST 1535 exhibits the potential for the research of Parkinson’s disease.

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.

BAY 60-6583 is a potent, high-affinity adenosine A2B receptor agonist (EC50 = 3 nM) with affinity for A2B receptors that exceeds that for A1, A2A, and A3 receptors.BAY 60-6583 is cardioprotective in a model of myocardial ischemia.The Ki values for BAY 60-6583 binding to mouse, rabbit, and dog A2BAR were 750 nM, 340 nM, and 330 nM, respectively. The Ki values of BAY 60-6583 binding to A2BAR in mice, rabbits and dogs were 750 nM, 340 nM and 330 nM respectively.

A2AAR antagonist 1 (compound 21a) is an antagonist of A2AAR (adenosine A2A receptor) that shows high ligand efficiency with a Ki value of 20 nM. A2AAR antagonist 1 can be used in neurodegenerative disease research [1].

A2AR-antagonist-1 (compound 38), an orally active adenosine A2A receptor antagonist with an IC50 value of 29 nM, demonstrates anti-tumor properties and stability in mouse liver microsomes (t1/2 = 86.1 min). Additionally, it activates T cells by inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and promoting expression of effector molecules (GZMB, IFNG, and IL-2) [1].

A2AAR/HDAC-IN-2 is a potent dual A2AAR/HDAC inhibitor.A2AAR/HDAC-IN-2 shows good affinity for A2AAR (Ki:10.3 nM) and inhibits HDAC1 well (IC50:18.5 nM). A2AAR/HDAC-IN-2 can be used 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.

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

SERCA2a activator 1 is a sarco/endoplasmic reticulum Ca2+-dependent ATPase 2a activator. SERCA2a activator 1 decreases phospholamban inhibition and enhances the systolic and diastolic functions of the heart.

AZD4635 (HTL1071) is a new-type adenosine 2A receptor (A2AR) inhibitor(Ki=1.7 nM).

CGS 21680 is a chemical compound that acts as a selective agonist for both adenosine and its A2A receptor, demonstrating a binding affinity (K i) of 27 nM.

ZM-241385 is a high-affinity antagonist ligand selective for the adenosine A2A receptor.

SCH 58261 is a potent and selective A2a adenosine receptor antagonist.The Ki =2.3 nM for rat A2a and 2 nM is for bovine A2a.

Tozadenant (SYN115) is an adenosine A2A receptor antagonist(Ki of 11.5 nM and 6 nM on human and rhesus,respectively)

PSB 0777 ammonium hydrate is a potent and selective adenosine A2A receptor full agonist, exhibiting K i values of 44.4 nM for rat A2A receptors and 360 nM for human A2A receptors. For rat and human A1 receptors, it shows significantly lower affinity with K i values of ≥10000 nM and 541 nM, respectively. The compound demonstrates poor brain penetration and is not orally absorbable. It is of interest in research related to inflammatory bowel disease (IBD) [1] [2] [3].

8-Bromotheophylline (Bromotheophylline) is the active moiety of pamabrom, a mixture of 2-amino-2-methyl-propanol and bromotheophylline. From this mixture, 8-Bromotheophylline acts as a weak diuretic that has been used along with some analgesics to relieve the symptoms of premenstrual syndrome

1-epi-Regadenoson is an α-isomer impurity of Regadenoson, a highly selective adenosine A2A receptor agonist [1].

adenosine A2A receptor full agonist

ST4206 is an antagonist of adenosine A2A. For adenosine A2A receptor and adenosine A1 receptor, the Kis values are 12 nM and 197 nM , respectively.

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

N6-Cyclopentyladenosine (CPA) is a selective agonist of the adenosine A1 receptor and can be used to mimic the action of the adenosine A1 receptor, with Ki's of 2.3 nM, 790 nM, and 43 nM for human A1, A2A, and A3 receptors, respectively.N6-Cyclopentyladenosine (CPA) can be used to modulate cellular signaling and neurotransmission and other biological processes. Cyclopentyladenosine (CPA) is used to regulate cell signaling, neurotransmitter release and other biological processes.

MRS5698 is a high affinity and selective agonist of A3 adenosine receptor (Ki ~ 3 nM) protects against chronic neuropathic pain. MRS5698 displays >1000-fold selectivity over A1 and A2A adenosine receptors

8-CSC is a dual agent endowed with good hMAO-B inhibitory activity (Ki: 235 nM in baboon liver mitochondria) and A2A affinity (Ki: 36 nM in rat brain striatal membranes receptor).

SCH442416 (SCH 442416) is an selective antagonist of adenosine A2A receptor. SCH442416 binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively).

IHCH-3064 is a tumour immunotherapeutic agent that targets both the adenosine A2A receptor and HDAC. IHCH-3064 effectively binds A2AR (Ki: 2.2 nM) and selectively inhibits HDAC1 (IC50: 80.2 nM). Prexasertib Mesylate

Proxyphylline (7-(2-Hydroxypropyl)theophylline) is a dual of adenosine A1/A2a receptor inhibitor and phosphodiesterase (PDE) inhibitor. Proxyphylline acts as a cardiac stimulant, vasodilator and bronchodilator.

Sch412348 is a potent competitive the human adenosine A2A receptor antagonist with Ki of 0.6 nM and has >1000-fold selectivity over all other adenosine receptors.

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].

adenosine A2A receptors antagonist

adenosine A2A receptor antagonist

PD 117519 (CI947) is an agonist of adenosine receptor

antagonist for the human adenosine A3 receptor

Ogerin is a selective GPR68 positive allosteric modulator (pEC50: 6.83). Ogerin blocks recall in fear conditioning in mice. Ogerin displays inverse agonist and antagonist activity (Ki, 220 nM) at A2A receptor and weak antagonist activity (Ki, 736 nM) at 5

Sipagladenant (Compound I) is an orally active inverse agonist targeting the adenosine receptor A2A [1]. It possesses potential for utilization in research pertaining to frontal lobe dysfunction [2].

Vipadenant (CEB-4520)(BIIB-014) is an adenosine A2a antagonist with Ki of 1.3 nM; less potent for A1(Ki=69 nM).

Preladenant (SCH-420814) is an orally bioavailable antagonist of the adenosine A2A receptor (Ki: 1.1 nM) and has >1000-fold selectivity over all other adenosine receptors.

CAY10680 is a dopamine-sparing, benzothiazinone compound that selectively inhibits both MAO-B activity (IC50 = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human). It demonstrates significantly less potent inhibitory values for other adenosine receptor subtypes (Kis > 1 μM) and MAO-A (IC50 ≥ 10 μM). At 1-20 μM, CAY10680 has been shown to abolish cAMP accumulation in CHO cells transfected with adenosine A2A receptors. In the central nervous system adenosine A2A receptor expression is localized to dopamine-innervated areas where heteromeric complexes are formed with dopamine D2 receptors. Because inhibition of adenosine A2A receptors has been shown to enhance D2 receptor function, the blockade of adenosine A2A receptors has emerged as a potential treatment for Parkinson's disease. An additional strategy in the treatment of Parkinson's disease has been to block the activity of monoamine oxidase B (MAO-B), the enzyme involved in dopamine catabolism.