2. Signaling Pathways
  3. GPCR/G Protein
  4. Adenosine Receptor
  5. Adenosine A1 receptor (A1R) Isoform

Adenosine A1 receptor (A1R)

 

Adenosine A1 receptor (A1R) Related Products (50):

Cat. No. Product Name Effect Purity
  • HY-N0092
    Inosine
    		Agonist 99.94%
    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.
  • HY-14858
    Derenofylline
    		Antagonist 99.93%
    Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.
  • HY-103185
    CCPA
    		Agonist 99.77%
    CCPA (2-Chloro-N6-cyclopentyladenosine) a highly selective A1 adenosine receptors agonist with a Ki 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.
  • HY-103175
    PSB36
    		Antagonist 99.94%
    PSB36 is a highly selective A1 adenosine receptor antagonist, with a Ki of 0.12 nM and a Kd of 0.7 nM. Systemic administration of PSB36 reduces formalin- and Carrageenan (HY-125474)-induced edema in mice and decreases pain-related behaviors, with no local paw activity. PSB36 prolongs the APD90 of rat and human atria, produces a frequency-dependent prolongation of rat atrial ERP, increases the diastolic threshold of rat atria, and shortens the duration of atrial fibrillation episodes. PSB36 can be used in research related to inflammatory pain, inflammatory hyperalgesia, edema and atrial fibrillation.
  • HY-116800
    FR194921
    		Antagonist 98.10%
    FR194921 is a potent, selective and orally active and cross the blood-brain barrier Adenosine A1 antagonist with Ki value of 6.6, 5400 nM for A1, A2A, respectively. FR194921 shows cognitive-enhancing and anxiolytic activity.
  • HY-115525
    NBUMP
    		Ligand
    NBUMP is a 5-HT1A receptor ligand with a 5-HT1A receptor Ki of 0.1 nM, α1-adrenergic receptor Ki of 46 nM, and a 5-HT1A receptor-to-α1-adrenergic receptor selectivity ratio of 460.NBUMP binds to the 5-HT1A receptor with high affinity.NBUMP binds to the α1-adrenergic receptor with lower affinity.
  • HY-182340
    KF20274
    		Antagonist
    KF20274 is an orally active adenosine A1 receptor antagonist. KF20274 increases the fecal pellet output in rats, and does not affect small intestinal propulsion or gastric emptying at defecation-increasing doses. KF20274 does not induce diarrhea at defecation-increasing doses. KF20274 can be used for the research of constipation.
  • HY-182518
    MDL-102234
    		Inhibitor
    MDL-102234 is a potent and selective adenosine A1 receptor antagonist with a Ki value of 23.2 nM at the adenosine A1 receptor. MDL-102234 can be used for the study of cognition enhancement-related neural functions.
  • HY-139644
    MIPS521
    		Agonist 98.21%
    MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95; KB=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine.
  • HY-147907
    Adenosine receptor inhibitor 1
    		Inhibitor 98.29%
    Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases.
  • HY-P2259
    TAT-GluA2 3Y
    		Inhibitor 99.93%
    TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction.
  • HY-103180
    2'-MeCCPA
    		Agonist 99.80%
    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).
  • HY-147908
    Adenosine receptor inhibitor 2
    		Inhibitor 99.08%
    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.
  • HY-103174
    MRS1334
    		Antagonist 98.93%
    MRS1334 is a potent and selective human adenosine A3 receptor antagonist with Kis of 2.69 nM, >100 nM, >100 nM for hA3, rA1, rA2A, respectively. MRS1334 blocks the protective effect of Cl-IB-MECA leading to significant bradycardia and elevated ST segment. MRS1334 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-103170
    LUF5834
    		Agonist 99.8%
    LUF5834 is a selective A2B adenosine receptor (A2BR) partial agonist (EC50 = 12 nM). LUF5834 is also a partial A1/A2A adenosine receptor agonist (lacking selectivity) with Ki values of 2.6 and 28 nM, respectively.
  • HY-147545
    A1AR antagonist 6
    		Antagonist 98.13%
    A1AR antagonist 6 (compound 15) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 6.38 and a pKi of 7.13.
  • HY-W004425
    DMPX
    		Antagonist 99.66%
    DMPX (3,7-Dimethyl-1-propargylxanthine) is a selective A2A adenosine receptor (A2A AR) antagonist that crosses the blood-brain barrier, with a Ki of 11 μM for rat A2 adenosine receptor and a Ki of 45 μM for rat A1 adenosine receptor. By blocking A2A receptors in specific brain regions, DMPX protects dopaminergic and GABAergic neurons from mitochondrial dysfunction. DMPX is applicable to research related to depression, Parkinson's disease and Huntington's disease.
  • HY-148076
    A2A receptor antagonist 3
    		Antagonist 99.46%
    A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a Ki of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with Kis of 37, 107 and 1467 nM, respectively.
  • HY-147544
    A1AR antagonist 5
    		Antagonist
    A1AR antagonist 5 (compound 20) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 5.83 and a pKi of 6.11.
  • HY-106186
    GW-493838
    		Agonist
    GW-493838 is a potent Adenosine A1 (A1AR) agonist. GW-493838 has the potential for the research of neuropathic pain.