
CAS
863513-91-1
Formulation
A solid
Purity
≥98%
MW
378,482463
Shipment
-20
Long Term Storage
-20
Shelf Life
1460
Description
An agonist of nociceptin-, µ-, ĸ-, and δ-opioid receptors (Kis = 0.9, 0.7, 2.6, and 18 nM, respectively); >100-fold selective for these receptors over a panel of more than 100 ion channels, neurotransmitter transporters, receptors, and enzymes, but does bind to the 5-HT5A receptor (Ki = 8.7 nM); inhibits nociceptin-, DAMGO-, and SNC 80-induced GTPɣS binding in CHO cells expressing nociceptin-, µ-, and δ-opioid receptors, respectively (EC50s = 13, 1.2, and 110 nM, respectively), as well as U69,593-induced GTPɣS binding in HEK293 cells expressing the ĸ-opioid receptor (EC50 = 17 nM); increases the paw withdrawal threshold in rat models of bone cancer pain and streptozotocin-induced diabetic neuropathy (ED50s = 3.6 and 0.5 µg/kg, respectively, i.v.); increases paw weight bearing on the ipsilateral side in a rat model of arthritis induced by complete Freund's adjuvant (CFA) and M. tuberculosis (ED50 = 5.5 µg/kg, i.v.)
ESCLUSIVAMENTE PER USO DI RICERCA (RUO) e non per uso terapeutico o diagnostico su uomini o animali. Il prodotto NON è un Dispositivo Medico o un Diagnostico in Vitro.
PRODUCT FOR RESEARCH USE ONLY (RUO) and not for therapeutic or diagnostic use on humans or animals. The product is NOT a Medical Device or an In-Vitro Diagnostic (IVD).