Zafirlukast is the first-approved LTR antagonist with anti-asthmatic and potential capsular contracture-preventing activities.

Montelukast Sodium is a potent, selective and competitive LTR1 antagonist with IC50 value < 5 nM, possesssing anti-inflammatory and bronchodilating activities.

Pranlukast 是一种选择性的 CysLT1 受体拮抗剂，对 CysLT1 受体具有高亲和力，IC50 值为 0.5 nM。Pranlukast 具有抗过敏和抗哮喘作用，可用于过敏性疾病和哮喘的研究。