Cysteinyl leukotriene receptor 1 (CysLT1) (CysLT1)

The Cysteinyl leukotriene receptor 1 (CysLT1) is a G protein-coupled receptor primarily expressed in human airway smooth muscle cells, airway macrophages, and other inflammatory cells such as eosinophils (UniProt: Q9Y271). It serves as a high-affinity receptor for cysteinyl leukotrienes, particularly leukotriene D4 (LTD4), which are potent inflammatory mediators derived from arachidonic acid (IUPHAR/BPS Guide to Pharmacology). Upon activation, CysLT1 triggers intracellular signaling pathways that lead to profound bronchoconstriction, increased vascular permeability, and enhanced mucus secretion (UniProt: Q9Y271; StatPearls: Montelukast). These physiological responses are central to the pathophysiology of asthma and allergic rhinitis (StatPearls: Montelukast). Pharmacological targeting of CysLT1 involves the use of selective antagonists, such as montelukast and zafirlukast, which effectively block the binding of leukotrienes to the receptor (IUPHAR/BPS Guide to Pharmacology). These drugs are widely used as maintenance therapies to reduce airway inflammation and improve pulmonary function in patients with chronic respiratory conditions (StatPearls: Montelukast). Recent clinical observations have highlighted important safety considerations, including potential neuropsychiatric side effects associated with CysLT1 antagonist therapy (FDA: Montelukast Boxed Warning).

Other names

CYSLTR1Cysteinyl leukotriene receptor type 1LTD4 receptorCysLTR1HGNC:2582

Selective competitive antagonism of the CysLT1 receptor (IUPHAR/BPS Guide to Pharmacology; StatPearls: Montelukast).