AI Article Synopsis
- Carbamylcholine, a muscarinic agonist, significantly increased amylase secretion and ion efflux in rat parotid acini, indicating a strong activity on various cellular processes.
- The study found that the effectiveness of carbamylcholine varied based on concentration, with EC50 values suggesting a limited relationship between phospholipase C activation and amylase secretion.
- Muscarinic antagonists inhibited the effects of carbamylcholine according to their potency, with atropine being the most effective, indicating that M2 subtype muscarinic receptors were primarily involved in these responses.
Article Abstract
The muscarinic agonist, carbamylcholine, stimulated amylase secretion in rat parotid acini 6-fold, the 86Rb efflux 5-fold, the 45Ca efflux 5-fold and the accumulation of inositol monophosphate, bisphosphate, trisphosphate and tetrakisphosphate 4-, 4-, 3- and 3-fold, respectively. The EC50 of carbamylcholine on these parameters were 0.4, 0.5, 1.3, 12, 12, 6 and 9 microM, suggesting spareness between phospholipase C activation and amylase secretion. These muscarinic responses were inhibited by four muscarinic antagonists with an order of potency on all parameters and on receptor occupancy (using N-[methyl-3H]scopolamine as a tracer): atropine greater than hexahydrosiladifenidol greater than pirenzepine greater than AF-DX 116. The pA2 of these antagonists on carbamylcholine-stimulated amylase secretion were 9.72 for atropine, 8.14 for hexahydrosiladifenidol, 7.16 for pirenzepine and 6.22 for AF-DX 116, indicating that the parotid muscarinic receptors were of an M2 subtype 83-fold more sensitive to hexahydrosiladifenidol than to AF-DX 116.
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| http://dx.doi.org/10.1016/0014-2999(88)90539-0 | DOI Listing |
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