Chiral pharmacokinetics and inversion of NG-nitro-arginine in rats / 中国药理学通报

ABSTRACT

Aim: To explore pharmacokinetics of NG-nitro-D-arginine (D-NNA)and NG-nitro-L-arginine (L-NNA)in conscious rats. Methods: The plasma concentration of D-NNA and L-NNA were determined by chiral ligand exchange method with capillary electrochromatography (CEC). Pharmacokinetic parameters were obtained using non-compartment model and were fitted using a computer program DAS. Results: The metabolism of D-NNA and L-NNA exhibited significant isomeric selectivity. The CL and T1/2 of D-NNA and D-NNA were(0.46 ± 0.02) ml·h-1·kg-1 vs (0.17 ± 0.03) ml·h-1·kg-1 (P < 0.05) and (1.44 ± 0.28) h vs (3.48 ± 0.41) h (P < 0.05), respectively. Unidirectional chiral conversion rate of D-NNA to L-NNA was (50.03 ± 8.5)%. Conclusion: The stereoselective pharmacokinetics of N G-nitro-arginine observed maybe due to the unidirectional chiral inversion of D-NNA to L-NNA.