adenosine A1 receptor agonist, selective and high-affinity
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||103626-26-2||SDF||Download SDF|
|Canonical SMILES||ClC[[email protected]]1O[[email protected]]([[email protected]@H]([[email protected]@H]1O)O)N2C(N=CN=C3N[[email protected]]4[[email protected]](CC5)C[[email protected]@H]5C4)=C3N=C2|
|Solubility||<37.98mg/ml in DMSO; <37.98mg/ml in ethanol||Storage||Store at -20°C|
|Physical Appearance||White solid||Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
(±)-5'-Chloro-5'-deoxy-ENBA is a selective and high-affinity adenosine A1 receptor agonist with Ki values of 0.51 .
Adenosine A1 receptor mediated neuroand cardioprotection (an antiarrhythmic effect), reduction of lipolysis in adipose tissue and reduction of neuropathic pain .
In mice injected with formalin at doses between 1 and 2mg/kg, (±)-5'-Chloro-5'-deoxy-ENBA inhibited the first and the second phases of the nocifensive response induced by formalin . In a mouse model of neuropathic pain (the Spared Nerve Injury (SNI) of the sciatic nerve), (±)-5'-Chloro-5'-deoxy-ENBA (0.5 mg/kg) reduced thermal hyperalgesia and mechanical allodynia 7 and 3 days post-SNI without significantly changed the motor coordination and arterial blood pressure. Also, (±)-5'-Chloro-5'-deoxy-ENBA chronic treatment reduced activated and hypertrophic microglia . In a Parkinson's disease (PD) mouse model, (±)-5'-Chloro-5'-deoxy-ENBA prevented the increase in sIPSC frequency and eIPSC amplitude produced by SKF. In mice with unilateral DA denervation, (±)-5'-Chloro-5'-deoxy-ENBA reduced the development of abnormal involuntary movements induced by L-DOPA .
. Franchetti P, Cappellacci L, Vita P, Petrelli R, et al. N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice. J Med Chem, 2009, 52(8): 2393-2406.
. Luongo L, Petrelli R, Gatta L, et al. 5'-Chloro-5'-deoxy-(±)-ENBA, a potent and selective adenosine A(1) receptor agonist, alleviates neuropathic pain in mice through functional glial and microglial changes without affecting motor or cardiovascular functions. Molecules, 2012, 17(12): 13712-13726.
. Mango D, Bonito-Oliva A, Ledonne A, et al. Adenosine A1 receptor stimulation reduces D1 receptor-mediated GABAergic transmission from striato-nigral terminals and attenuates l-DOPA-induced dyskinesia in dopamine-denervated mice. Exp Neurol, 2014, 261: 733-743.