Milestones in the development of CysLT1 therapeutic antagonists
| • 1938, identification of SRS (Feldberg and Kellaway, 1938) |
| • 1951, SRS-A generated by the human lung (Schild et al., 1951) |
| • 1973, SRS-A antagonist (Augstein et al., 1973) |
| • 1976–1980, structures and synthetic pathways for the leukotrienes (Corey et al., 1980;Samuelsson, 1983) |
| • 1980–1990, CysLT selective antagonists (Laboratories: Merck, Smith Kline & French, Abbott, Eli Lilly) |
| • 1985–1995, existence of two receptors in the human lung: a single CysLT1 receptor in airways responsible for smooth muscle contraction (Buckner et al., 1986) and a CysLT2 receptor in the human pulmonary vasculature associated with vasoconstriction (Labat et al., 1992) |
| • 1995, first CysLT1 antagonist marketed (Pranlukast) |
| • 1999, hCysLT1 receptor cloned expressed and characterized (Lynch et al., 1999;Sarau et al., 1999) |
| • 2000, hCysLT2 receptor cloned expressed and characterized (Heise et al., 2000; Nothacker et al., 2000; Takasaki et al., 2000). |