ABSTRACT
The transient receptor potential (TRP) superfamily of cation channels has emerged as cellular sensors of various extra-and intracellular environmental changes.1 The 28 or so TRP members in mammals and their counterparts in other animal classes are involved in diverse cellular functions, many of which are mentioned and some of which are discussed in detail in subsequent chapters of this book. However, the biggest challenge that TRP channel researchers face nowadays is the lack of pharmacological tools. With a few exceptions, for instance, TRPV1, high-af—nity speci—c agonists and/or antagonists are lacking for the mammalian TRP channels. Despite this de—ciency, active research has revealed a large number of natural and synthetic compounds having stimulatory or inhibitory effects on various TRP channels. However, even some of the more commonly used drugs, e.g., menthol, 2-aminoethoxydiphenyl borate (2-APB), allyl isothiocyanate (mustard oil), and 1-oleoyl-acetyl-sn-glycerol (OAG), may lack the speci—city required for more rigorous studies, and the concentrations employed are typically in high micromolar ranges,2-5 limiting their use in physiological experiments when the identity of the channel(s) is ambiguous. Thus there are unmet needs for more speci—c and potent activators and/or inhibitors for many TRP channels.
