Transgenic rodents as animal models for modulation of B1 bradykinin receptor protein

摘要

Transgenic rats are generated which incorporate a primate B₁ bradykinin receptor transgene(s) into their genome. This B₁ bradykinin receptor gene is expressed in these transgenic rats, which results in binding of compounds which are selective for the primate form (such as the human form) of the receptor and not the rat form of the receptor. Therefore, the expressed transgenes within these transgenic lines mimic antagonist and agonist selectivity of the wild type primate B₁ bradykinin receptor. These transgenic animals are useful as a specific receptor occupancy model for modulators of the B₁ bradykinin receptor from the human or closely related species, as well as providing for an animal model system for assessment of the pharmacodynamic properties of such a B₁ bradykinin modulator(s).