Description
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].
Uses
Antagonist (bradykinin).
Definition
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.
brand name
Metastat (CollaGenex).
Biological Activity
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.
References
[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.
