186141-75-3
Chemical Structure
A-134974
- CAS No.: 186141-75-3
- Formula:C11H14IN5O2
- Molecular Weight:375.17
IUPAC Name: (1S,2R,3S,5R)-3-amino-5-(4-amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol
InChIKey: NSXJHIFQIZKLGF-LWIVVEGESA-N
SMILES: O[C@H]1[C@@H](C[C@@H]([C@H]1O)N)N2C3=NC=NC(N)=C3C(I)=C2
Biological Activity: A-134974 is a selective adenosine kinase (ADK) inhibitor, with an IC50 of 0.06 nM and 45 nM in rat brain cytoplasmic ADK enzyme assays and intact IMR-32 cells, respectively. A-134974 inhibits adenosine phosphorylation and elevates intracellular and extracellular adenosine levels, alleviates neuropathic tactile allodynia and inflammatory thermal hyperalgesia via endogenous adenosine signaling in the spinal cord, and shows favorable dose separation between its analgesic effects and motor function impairment. A-134974 can be used in research on neuropathic pain, inflammatory pain, RNA silencing and thermoregulation[1][2][3][4].
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A-134974 | A-134974 is a selective adenosine kinase (ADK) inhibitor, with an IC50 of 0.06 nM and 45 nM in rat brain cytoplasmic ADK enzyme assays and intact IMR-32 cells, respectively. A-134974 inhibits adenosine phosphorylation and elevates intracellular and extracellular adenosine levels, alleviates neuropathic tactile allodynia and inflammatory thermal hyperalgesia via endogenous adenosine signaling in the spinal cord, and shows favorable dose separation between its analgesic effects and motor function impairment. A-134974 can be used in research on neuropathic pain, inflammatory pain, RNA silencing and thermoregulation. | |||||||||||||||||||||
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- [1]. Zhu CZ, et al. A-134974: a novel adenosine kinase inhibitor, relieves tactile allodynia via spinal sites of action in peripheral nerve injured rats. Brain research. 2001 Jun 29;905(1-2):104-10. [Content Brief]
- [2]. Wang H, et al. Adenosine kinase inhibition and suppression of RNA silencing by geminivirus AL2 and L2 proteins. Journal of virology. 2005 Jun;79(12):7410-8. [Content Brief]
- [3]. Eisner C, et al. Profound hypothermia after adenosine kinase inhibition in A1AR-deficient mice suggests a receptor-independent effect of intracellular adenosine. Pflugers Archiv : European journal of physiology. 2017 Feb;469(2):339-347. [Content Brief]
- [4]. Jarvis MF, et al. Comparison of the ability of adenosine kinase inhibitors and adenosine receptor agonists to attenuate thermal hyperalgesia and reduce motor performance in rats. Pharmacology, biochemistry, and behavior. 2002 Oct;73(3):573-81. [Content Brief]
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