| Bioactivity | PL37 (Debio-0827) is an orally active Enkephalinase dual inhibitor (dual inhibition refers to the simultaneous inhibition of Neutral Endopeptidase and Aminopeptidase N activities). PL37 exerts its anti-hyperalgesic effects by activating μ-opioid receptors (µ-opioid receptors), with an ED50 value of 13.4 mg/kg for analgesic effects in mice. PL37 can be used to study diabetic neuropathic pain[1][2][3][4]. |
| CAS | 935481-06-4 |
| Formula | C22H34N2O6S3 |
| Molar Mass | 518.71 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Menéndez L, et al. Inhibition of osteosarcoma-induced thermal hyperalgesia in mice by the orally active dual enkephalinase inhibitor PL37. Potentiation by gabapentin. Eur J Pharmacol. 2008 Oct 31;596(1-3):50-5. [2]. Tesfaye S. PL37: a new hope in the treatment of painful diabetic neuropathy?[J]. Pain Management, 2016, 6(2): 129-132. [3]. González-Rodríguez S, et al. Involvement of enkephalins in the inhibition of osteosarcoma-induced thermal hyperalgesia evoked by the blockade of peripheral P2X3 receptors. Neurosci Lett. 2009 Nov 20;465(3):285-9. [4]. Descheemaeker A, et al. Dual enkephalinase inhibitor PL37 as a potential novel treatment of migraine: evidence from a rat model. Brain. 2022 Aug 27;145(8):2664-2670. |