935481-06-4
Chemical Structure
PL37
Synonym(s): Debio-0827
- CAS No.: 935481-06-4
- Formula:C22H34N2O6S3
- Molecular Weight:518.71
IUPAC Name: 1-((ethoxycarbonyl)oxy)ethyl 2-((S)-3-(((S)-2-amino-4-(methylthio)butyl)disulfanyl)-2-benzylpropanamido)acetate
InChIKey: BJCNUZJDFWFVBY-VITQDTLGSA-N
SMILES: CSCC[C@H](N)CSSC[C@@H](CC1=CC=CC=C1)C(NCC(OC(C)OC(OCC)=O)=O)=O
Biological Activity: 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].
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PL37 | 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. | |||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Tesfaye S. PL37: a new hope in the treatment of painful diabetic neuropathy?[J]. Pain Management, 2016, 6(2): 129-132. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
Keywords
