Hoe 140 (D-Arg-[Hyp3, Thi5, D-Tic7, Oic8]-bradykinin), on bradykinin- and platelet-activating factor (PAF)-induced bronchoconstriction and airway microvascular leakage in anesthetized guinea pigs. Hoe 140 is highly potent and long-acting in inhibiting BK-induced hypotensive responses in the rat. Four hours after s.c. administration of 20nmol kg-1, inhibition still amounted to 60% whereas the effect of 200nmol kg-1 of d-Arg-[Hyp2, Thi5,8, d-Phe7]BK was not significant[1-2].
ChEBI: A ten-membered synthetic oligopeptide consisting of D-Arg, Arg, Pro, Hyp, Gly, Thi, Ser, D-Tic, Oic, and Arg residues joined in sequrence. A bradykinin receptor antagonist used as its acetate salt for the treatment of acut
attacks of hereditary angioedema in adult patients.
Hoe 140 is highly potent and long-acting in inhibiting BK-induced hypotensive responses in the rat. Four hours after s.c. administration of 20 nmol kg?1, inhibition still amounted to 60%, whereas the effect of 200 nmol kg?1 of d-Arg—[Hyp2, Thi5,8, d-Phe7]BK was not significant. In receptor binding studies in guinea-pig ileum preparations, Hoe 140 showed an IC50 of 1.07 × 10?9mol l?1 and a KI value of 7.98 × 10?10 mol l?1.
[1] K. Wirth. “Hoe 140 a new potent and long acting bradykinin-antagonist: in vivo studies.” British Journal of Pharmacology 102 3 (1991): 774–777.
[2] T Sakamoto. “Effect of Hoe 140, a new bradykinin receptor antagonist, on bradykinin- and platelet-activating factor-induced bronchoconstriction and airway microvascular leakage in guinea pig.” European journal of pharmacology 213 3 (1992): 367–73.
