Functional alpha(1)-adrenoceptor subtypes in human submandibular glands.

alpha(1)-Adrenoceptor has been discovered to exist in many human tissues and mediates important physiological functions. The purpose of this study was to detect the expression, distribution, and function of alpha(1)-adrenoceptor subtypes in human submandibular glands. alpha(1A)- and alpha(1B)-Adrenoceptor mRNAs were identified by reverse-transcription/polymerase chain-reaction (RT-PCR), and their proteins were detected by Western blotting. No expression of the alpha(1D)-adrenoceptor mRNA and protein was found. By in situ hybridization and immunohistochemistry, alpha(1A)- and alpha(1B)-adrenoceptor mRNAs and proteins were shown to be widespread in both ductal and acinar cells. By confocal microscopy, phenylephrine (stimulating both alpha(1A)- and alpha(1B)-adrenoceptors) or A61603 (alpha(1A)-selective agonist) induced an increase in intracellular calcium by 2.33 +/- 0.18-fold and 1.81 +/- 0.43-fold, respectively, while 5-methylurapidil (alpha(1A)-selective antagonist) partly blocked calcium mobility stimulated by phenylephrine. The results indicated that functional alpha(1A)- and alpha(1B)-adrenoceptors were expressed in human submandibular glands, and might contribute to the regulation of saliva synthesis and secretion.