Ba 679 BR, A novel long-acting anticholinergic bronchodilator
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2018, Pulmonary Pharmacology and TherapeuticsCitation Excerpt :Many studies suggest that the longevity of the antagonist-receptor complex is the cause of insurmountable antagonism, although the phenomenon has also been explained either by the presence of allosteric binding sites on the receptor or by the partitioning of the antagonist into (and slow removal from) tissue compartments or the matrix surrounding the receptor, which allows sustained release of the antagonist and increases the likelihood of rebinding to the receptor [35,36]. Several in vitro studies have found that the dissociation half-life at the human M3 muscarinic receptor (hM3R) is much longer for LAMAs that for ipratropium [9,10,12,19,37]. However, the experimental conditions in the in vitro evaluation of a drug's kinetic properties are less physiologically authentic than in an organ bath; tiotropium and glycopyrronium dissociate much more quickly from the hM3R at a physiological temperature and salt concentration (46 and 11 min, respectively) than in the receptor binding studies (462 and 173 min, respectively) [9,19].
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