Chemistry:AC-263093
From HandWiki
AC-263093 is a drug used in scientific research which acts as an agonist at the neuropeptide FF receptor NPFF2 and an antagonist for the closely related NPFF1 receptor. In animal studies it reduced tolerance to morphine but also produced hyperalgesia and anxiety.[1][2][3][4] Related compounds such as AC-099 with Cl or CF3 replacing the bromine substituents have similar activity as NPFF2 agonists or partial agonists but with relatively lower potency.[5]
References
- ↑ "Reversal of morphine tolerance by a compound with NPFF receptor subtype-selective actions". Neuroscience Letters 584: 141–145. January 2015. doi:10.1016/j.neulet.2014.10.018. PMID 25459291.
- ↑ "Altered nociception and morphine tolerance in neuropeptide FF receptor type 2 over-expressing mice". European Journal of Pain 20 (6): 895–906. July 2016. doi:10.1002/ejp.814. PMID 26648516.
- ↑ "Activation of NPFFR2 leads to hyperalgesia through the spinal inflammatory mediator CGRP in mice". Experimental Neurology 291: 62–73. May 2017. doi:10.1016/j.expneurol.2017.02.003. PMID 28179153.
- ↑ "NPFFR2 Activates the HPA Axis and Induces Anxiogenic Effects in Rodents". International Journal of Molecular Sciences 18 (8): 1810. August 2017. doi:10.3390/ijms18081810. PMID 28825666.
- ↑ "Nonpeptide small molecule agonist and antagonist original leads for neuropeptide FF1 and FF2 receptors". Journal of Medicinal Chemistry 57 (21): 8903–8927. November 2014. doi:10.1021/jm500989n. PMID 25268943.
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