Captopril characterization

Chetty DJ, Chen LH, Chien YW (2001) Characterization of captopril sublingual permeation Determination of preferred routes and mechanisms. J Pharm Sci 90 1868-1877... 

As expected, this drug is very effective in renovascular, malignant, and essential hypertensives characterized by high renin levels. Surprisingly, however, it is also effective in patients with normal renin levels and even in some low renin patients. The doses of captopril used in these studies were 50-100 times those previously shown to be required to block the conversion of angiotensin I to angiotensin II, so inhibition of the CE may not completely account for its antihypertensive action. ... 

Early work with zinc metalloprotease inhibitors focused on the well-characterized agents captopril ((2S)-l-[(2S)-2-methyl-3-sulfanyl-propanoyl] pyrrolidine-2-carboxylic acid) and phos-phoramidon (/V-alpha-i,-rhamnopyranosyloxy[hydroxyphosphinyl -i,-leucyl-L-tryptophan). These compounds, however, were found to have little inhibitory activity against BoNT (Adler et al., 1994, 1999a). The poor efficacy of captopril was suggested to stem from unfavorable steric constraints in the binding of proline at the active site of BoNT (Schmidt and Stafford, 2002). 

Tc-MAG3 is used for the evaluation of nephrological and urological disorders, in particular for the study of renal perfusion, relative kidney function, and characterization of urinary flow. Renovascular hypertension is diagnosed after pharmacological intervention (captopril test) (Kletter 1988). 

Early work with zinc metalloprotease inhibitors focused on the well-characterized agents captopril and phosphoramidon. These were found to have little or no inhibitory activity against any BoNT serotype. Phosphoramidon analogs in which Leu-Trp was replaced by Phe-Glu to resemble the cleavage site of synaptobrevin exhibited little increase in inhibitory activity one analog was slightly more potent and two were significantly less potent than the parent compound. 

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