picumeterol

Picumeterol is a potent and highly selective beta2-adrenoceptor agonist, developed as the (R)-enantiomer of the racemic compound GR63411B. It acts by stimulating beta2-adrenoceptors on airway smooth muscle, leading to increased intracellular cyclic adenosine monophosphate (cAMP) and resulting in bronchodilation. Picumeterol was investigated primarily for inhalation use in asthma and related respiratory diseases. In preclinical studies, it demonstrated a longer duration of action than salbutamol but shorter than salmeterol, with about 40 times greater potency than its (S)-isomer. Clinical studies showed that while it produced significant bronchodilation, its effects were short-lasting in vivo despite long-lasting activity observed in vitro. The drug displayed dissociation between bronchodilator activity and protection against methacholine-induced bronchoconstriction, possibly due to low intrinsic activity[1][2][4][5][6][8].

Other names

picumeterol fumaratepicumeterolum130641-36-0