Adenosine Receptor Agonist

Adenosine monophosphate-¹³C₁₀ (AMP-¹³C₁₀) dilithium is ¹³C-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction.

GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a K_is of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions.

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.

N6-(4-Hydroxybenzyl) adenosine (Para-topolin riboside) is an equilibrative nucleoside transporter 1 (ENT1) inhibitor and a selective agonist of adenosine A_2a receptor (A_2aR), and also exhibits activity against P2Y12 receptor. N6-(4-Hydroxybenzyl) adenosine reduces ethanol intake and preference, attenuates operant conditioning-induced ethanol place preference, decreases the value of ethanol-related rewards, and inhibits collagen-induced platelet aggregation. N6-(4-Hydroxybenzyl) adenosine can be used in studies related to alcohol use disorder.

Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full α1A-adrenergic receptor (α1A-AR) agonist (K_i=120 nM) and only a partial agonist at α1B-AR (K_i= 960 nM) and α1D-AR (K_i=660 nM).

(-)-N6-phenylisopropyl adenosine (L-Phenylisopropyladenosine) is a selective A1 adenosine receptor agonist. (-)-N6-phenylisopropyl adenosine inhibits K⁺-induced Ca²⁺ uptake with an IC₅₀ value of 0.5 µM. (-)-N6-phenylisopropyl adenosine protects against ischemia-induced ventricular arrhythmias and atrial fibrillation, and exacerbates ethanol withdrawal symptoms. (-)-N6-phenylisopropyl adenosine also has analgesic effects.

A2AR-agonist-1 is a potent A2AR agonist and ENT1 inhibitor with Ki of 4.39 and 3.47 for A2AR and ENT1.

CV1808 (2-Phenylaminoadenosine) is a non-selective A2 adenosine receptor (A2 AR) agonist with K_is of 76 and 1450 nM for A2A and A3 adenosine receptor subtypes, respectively.

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).

Evodenoson is a selective agonist of the A_2A adenosine receptor. Evodenoson’s primary actions include reducing inflammatory responses, decreasing intestinal fluid secretion, edema, tissue damage, and neutrophil infiltration induced by Clostridium difficile toxin A. Evodenoson’s protective effect is achieved by reducing myeloperoxidase (MPO) and adenosine deaminase (ADA) activities, and by lowering the production of tumor necrosis factor-alpha (TNF-α).

Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis.

Apadenoson is an adenosine analog with selective agonist activity for the adenosine A_2a receptor and induces coronary vasodilatation.

AB-MECA is a high affinity A₃ adenosine receptor agonist with a binding K_i of 430.5 nM for human A₃ receptors in CHO cells. AB-MECA can enhance plasma histamine level.

GS-9667 (CVT 3619), a novel N⁶-5'-substituted adenosine analog, is a selective, partial agonist of the A₁ adenosine receptor (A₁AdoR). GS-9667 binds to adipocyte membranes with high (K_H=14 nM) and low (K_L=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC₅₀ values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA).

Adenosine monophosphate-¹³C₁₀,¹⁵N₅(AMP-¹³C₁₀,¹⁵N₅) is the ¹³C-labeled and ¹⁵N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction.

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.

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.

Binodenoson (MRE-0470) is a potent and selective A2A adenosine receptor agonist (K_D=270 nM). Binodenoson is being developed as a short-acting coronary vasodilator as an adjunct to radiotracers for use in myocardial stress imaging.

LUF6000 is an orally active allosteric modulator of the A3 adenosine receptor. LUF6000 has potent anti-inflammatory effect.

Adenosine monophosphate-d₁₂ (AMP-d₁₂) dilithium is deuterium labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction.