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- W2025551502 abstract "To examine the response to ß-adrenergic receptor agonists (ß-agonists) following prolonged activation of the stimulatory G protein of adenylyl cyclase (G<sub>s</sub>), relaxation by isoproterenol (isoprenaline, CAS 949-36-0) and formoterol (CAS 73573-87-2), a long-acting ß-agonist, after exposure to formoterol was measured in human tracheal smooth muscle, using isometric tension records. Prior exposure to formoterol (0.3-30 nmol/l) for 45 min reduced the subsequent relaxation induced by this drug in a concentration-dependent manner, but only modestly reduced that induced by isoproterenol. Next, the effects of cholera toxin (CTX, CAS 9012-63-9) an irreversible direct activator of G<sub>s</sub> and formoterol on the reduced responsiveness to isoproterenol after continuous and repeated exposure to isoprotenerol were examined. Preincubation with cholera toxin (0.02-2 µg/ml) caused concentration-dependent inhibition of the desensitization induced by isoproterenol, but preincubation with formoterol did not. These results indicate that prolonged activation of G<sub>s</sub> via ß-adrenergic receptors does not cause cross-desensitization to short-acting ß-agonists. However, it also fails to inhibit the desensitization of ß-adrenergic receptors after excessive exposure to short-acting ß-agonists. Activation of G<sub>s</sub> via a pathway that bypasses the receptors may be beneficial for the prevention of this phenomenon." @default.
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- W2025551502 date "2011-12-26" @default.
- W2025551502 modified "2023-10-16" @default.
- W2025551502 title "Effects of Direct and Indirect Activation of G Protein of Adenylyl Cyclase on the Subsequent Response to ß-Adrenergic Receptor Agonists in Human Trachealis" @default.
- W2025551502 doi "https://doi.org/10.1055/s-0031-1299971" @default.
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