Ishii T, Shimo Y
Eur J Pharmacol. 1987 Feb 10;134(2):137-43. doi: 10.1016/0014-2999(87)90159-2.
Experiments were designed to determine the effect of cooling on the contractile response of rat tracheal strip-chain preparation to the partial agonist pilocarpine. The preparation was suspended in an organ bath containing Krebs bicarbonate solution for isometric tension recording. A decrease of the bath temperature from 37 to 30, 20 or 10 degrees C (cooling) did not affect or inhibited the contractile response of the trachea caused by pilocarpine (1-100 microM), while it augmented the carbachol (0.1-1 microM)-induced response. At 37 degrees C, the pilocarpine (3-100 microM)-induced contraction was relatively resistant to removal of extracellular Ca2+ or to the Ca2+ entry blocker, verapamil (1 microM). Similar results were also obtained for the carbachol (0.3-10 microM)-induced response. On the other hand, the affinity of pilocarpine for the tracheal muscarinic receptors, determined from its dissociation constant (KA), was significantly decreased at a lower temperature. It is concluded from these observations that cooling-induced subsensitivity of the rat tracheal muscle to pilocarpine is mainly associated with a decrease in the affinity of the agonist for muscarinic receptors.