PZM21

A μ-opioid receptor agonist

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1mg

￥650.00

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5mg

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1130.00

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10mg

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50mg

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100mg

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Background

PZM21 is a μ-opioid receptor agonist (K_i = 1.1 nM).¹ It is selective for μ- over κ- and δ-opioid receptors (K_is = 18 and 506 nM, respectively). PZM21 induces G_i/o signaling (EC₅₀ = 4.6 nM in HEK293T cells expressing human receptors) but has no detectable activity in a β-arrestin2 recruitment assay. In vivo, PZM21 (10, 20, and 40 mg/kg) induces analgesia in the hot plate test and reduces formalin-induced paw licking in mice when administered at a dose of 40 mg/kg.

1.Manglik, A., Lin, H., Aryal, D.K., et al.Structure-based discovery of opioid analgesics with reduced side effectsNature537(7619)185-190(2016)

Protocol

Animal experiment:

Mice: PZM21 is dissolved in 0.9% sodium chloride. Mice are injected with either vehicle, morphine (5 mg/kg, or 10 mg/kg), TRV130 (1.2 mg/kg) or PZM21 (10 mg/kg; 20 mg/kg; or 40 mg/kg). After injection of drug, the analgesic effect expressed as percentage maximum possible effect (%MPE) is measured at 15, 30, 60, 90 and 120 min after drug treatment[1].

参考文献:

[1]. Manglik A, et al. Structure-based discovery of opioid analgesics with reduced side effects. Nature. 2016 Sep 8;537(7619):185-190.
[2]. Kostic M, et al. Biasing Opioid Receptors and Cholesterol as a Player in Developmental Biology.
[3]. Araldi D, et al. Mu-opioid Receptor (MOR) Biased Agonists Induce Biphasic Dose-dependent Hyperalgesia and Analgesia, and Hyperalgesic Priming in the Rat. Neuroscience. 2018 Oct 17;394:60-71.