tcsc1813 Meptazinol (hydrochloride)

Meptazinol Hcl(WY-22811 Hcl) is a unique centrally active opioid analgesic.

IC50 Value: < 1 nM [1]

Target: Opioid Receptor

in vitro: Meptazinol inhibits a portion of 3H-labeled opiate and opioid peptide binding quite potently, with IC50 value under 1 nM [1].

in vivo: Given at equianalgesic doses, morphine (3.5 mg/kg i.v.) significantly lowers the pO2 over 20 mm Hg and raises the pCO2 over 10 mm Hg as measured in arterial blood samples, whereas meptazinol (10 mg/kg i.v.) has no significant effects on either [1]. The group receiving meptazinol demonstrated no cardiovascular changes although bispectral index dropped by an additional 19% when compared to 1 min after barbiturate injection [2]. Rapid and significant levels of MEP in plasma and CSF can be achieved after nasal administration whereas the oral administration resulted in considerably lower drug concentrations [3].