Sakurada_2003_Neurochem.Res_28_1401

Reference

Title : Pralidoxime iodide (2-pAM) penetrates across the blood-brain barrier - Sakurada_2003_Neurochem.Res_28_1401
Author(s) : Sakurada K , Matsubara K , Shimizu K , Shiono H , Seto Y , Tsuge K , Yoshino M , Sakai I , Mukoyama H , Takatori T
Ref : Neurochem Res , 28 :1401 , 2003
Abstract :

The in vivo rat brain microdialysis technique with HPLC/UV was used to determine the blood-brain barrier (BBB) penetration of pralidoxime iodide (2-PAM), which is a component of the current nerve agent antidote therapy. After intravenous dosage of 2-PAM (10, 50, 100 mg/kg), 2-PAM appeared dose-dependently in the dialysate; the striatal extracellular/blood concentration ratio at 1 h after 50 mg/kg dosage was 0.093 +/- 0.053 (mean +/- SEM). This finding offered conclusive evidence of the BBB penetration of 2-PAM. We also examined whether the BBB penetration of 2-PAM was mediated by a certain specific transporter, such as a neutral or basic amino acid transport system. Although it was unclear, the neural uptake of 2-PAM was Na+ dependent. The mean BBB penetration by 2-PAM was approximately 10%, indicating the intravenous administration of 2-PAM might be to a degree effective to reactivation of the blocked cholinesterase in the brain.

PubMedSearch : Sakurada_2003_Neurochem.Res_28_1401
PubMedID: 12938863

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Citations formats

Sakurada K, Matsubara K, Shimizu K, Shiono H, Seto Y, Tsuge K, Yoshino M, Sakai I, Mukoyama H, Takatori T (2003)
Pralidoxime iodide (2-pAM) penetrates across the blood-brain barrier
Neurochem Res 28 :1401

Sakurada K, Matsubara K, Shimizu K, Shiono H, Seto Y, Tsuge K, Yoshino M, Sakai I, Mukoyama H, Takatori T (2003)
Neurochem Res 28 :1401