Irreversible Inhibition of Angiotensin II Activity on the Rat Uterus by an Alkylating Angiotensin Derivative

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Abstract
An alkylating analogue of angiotensin II (AII) containing a nitrogen mustard group (p-[N, N-bis(2-chloroethyl) aminojphenylbutyryl at the N-terminus ([Chi1]-All) was shown to be an irreversible specific inhibitor of the action of AII on the isolated rat uterus. The inhibition was observed when the Ca++ concentration in the medium was 0.18 mM, and was more intense in calcium-free medium. It was not observed in the presence of 1 mM Ca++. It is concluded that a site near (but not on) the AII receptor is alkylated by [Chi1 ]-AII, and the properties of this site suggest that it is the same one involved in the phenomenon of tachyphylaxis.

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