TRANSGENIC RODENTS AS ANIMAL MODELS FOR MODULATION OF B1 BRADYKININ RECEPTOR PROTEIN

摘要

Transgenic rats are generated which incorporate a primate B1 bradykininreceptor transgene(s) into their genome. This B1 bradykinin receptor gene isexpressed in these transgenic rats, which results in binding of compoundswhich are selective for the primate form (such as the human form) of thereceptor and not the rat form of the receptor. Therefore, the expressedtransgenes within these transgenic lines mimic antagonist and agonistselectivity of the wild type primate B1 bradykinin receptor. These transgenicanimals are useful as a specific receptor occupancy model for modulators ofthe B1 bradykinin receptor from the human or closely related species, as wellas providing for an animal model system for assessment of the pharmacodynamicproperties of such a B1 bradykinin modulator(s).