Adenosine A₁ receptor (A₁R) Agonist

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 A_2A (A_2AR) receptors.

CCPA (2-Chloro-N6-cyclopentyladenosine) a highly selective A1 adenosine receptors agonist with a K_i of 0.4 nM. CCPA inhibits adenylate cyclase with an IC₅₀ of 33 nM. CCPA exhibits anti-seizure and cardiacprotective activity. CCPA can be used for the research of seizure and myocardial infarction.

MIPS521 is a positive allosteric modulator of adenosine A₁ receptor (A₁AR). MIPS521 also has a lower A₁R allosteric affinity (pK_B=4.95; K_B=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine.

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).

LUF5834 is a selective A_2B adenosine receptor (A2BR) partial agonist (EC₅₀ = 12 nM). LUF5834 is also a partial A₁/A_2A adenosine receptor agonist (lacking selectivity) with K_i values of 2.6 and 28 nM, respectively.

2-Chloro-3-deazaadenosine is agonists for adenosine receptor, with K_is of 0.3, 0.08, 25.5 and 1.9 μM, for A1, A2A, A2B, and A3 receptors, respectively.

GW-493838 is a potent Adenosine A1 (A1AR) agonist. GW-493838 has the potential for the research of neuropathic pain.

BW-534U87 is an orally active adenosine A1 receptor agonist and competitive adenosine deaminase (ADA) inhibitor (K_i=7 μM). BW-534U87 elevates brain adenosine levels and suppresses epileptiform activity. BW-534U87 demonstrate anticonvulsant efficacy in animal seizure models. BW-534U87 is promising for research of epilepsy and adenosine-related neuropsychiatric disorders.

MRS7469 is a highly selective A1 adenosine receptor (A1AR) agonist with over 2000-fold selectivity over other adenosine receptor subtypes. MRS7469 stably binds to the orthosteric binding site of A1AR, and exhibits extremely high affinity for both humans and mice (e.g., human pK_i is 8.67, mouse pK_i is 9.43). By activating central A1AR, MRS7469 significantly induces hypothermia, motor inhibition and psychomotor dysfunction, and can be widely used in research related to depression and other relevant fields.

Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) hydrochloride is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate hydrochloride has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases.

Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases.

MIPS3526 is a potent and selective A2B adenosine receptor (A2BR) agonist with a pEC₅₀ of 10.17 (EC₅₀ of 58 pM). MIPS3526 shows highly receptor subtype selective versus the A1R, A2AR, and A3R. MIPS3526 ameliorates angiotensin II stimulating effects in both cardiac myocytes and fibroblasts. MIPS3526 can be used for the study of cardiovascular disease including heart failure where cardiac remodeling is a major driver.

CVT-2759 analog (compound 15) is a partial agonist of A1 adenosine receptor (K_i=167 nM) and can be used for the study of cardiac arrhythmias.