By Frank J. Dixon (Ed.)
Meant for researchers in immunology, cellphone biology, virology and drugs, this publication presents info on such themes as cytokine gene rules, and animal versions for bought immunodeficiency syndrome.
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Extra info for Advances in Immunology, Vol. 52
G. ICs0 values) rather than rigorous K d estimates. Thus, comparison of absolute affinities between different systems is difficult. Nevertheless, the presence in a given cell type of two binding sites with different apparent affinities for a given receptor antagonist should be a reliable indicator of intraspecies homologs.
1992). , 1995; Hall and Geppetti, 1995). The regulation of B2 receptor expression, internalization and signal transduction are covered in Chapter 6. , 1981a,b). g. , 1981a). , 1994). , 1994). 2 . 2 . 1 and Fig. 1 show the structures and pseudonyms of some Bz receptor antagonists. , 1992a,b). , 1993; Fig. 1). With the advent of stable and selective antagonists, the role of B2 receptors in pathophysiology began to be explored, and examples of antagonists are currently in some stage of clinical trials.
Structural conformations of B2 receptor antagonists are discussed by Kyle (1994) and Kyle et al. (1991a,b). The first competitive antagonists of B2 receptors were BK analogs (Vavrek and Stewart, 1985). The key modification was the replacement of proline at position seven with D-phenylalanine (DPhe), and the prototype, [DPhe7]BK, proved to be a moderately potent and selective antagonist in guinea-pig ileum (pA2 ca 5) (Vavrek and Stewart, 1985). 1. 4) (Vavrek and Stewart, 1985). Other antagonists in this series include analogs with hydroxyproline residues substituted at positions 2 and/or 3 (see Stewart and Vavrek, 1991).
Advances in Immunology, Vol. 52 by Frank J. Dixon (Ed.)