Abstract:
:Rat pheochromocytoma PC12W cell membranes have previously been shown to exclusively contain the AT2 receptor subtype. The present study extended these binding data and explored the functional expression of these binding sites. Our binding competition studies show a potency series of Ang II = Ang III greater than saralasin greater than Ang I = PD123177 much greater than Ang II(1-7) much much greater than losartan. PD123177 (1 microM) completely eliminated [125I]Ang II binding to PC12W cells. Competitive displacement of [125I]Ang II with Ang II shows a dissociation equilibrium constant (Kd) of 1.79 nM and a binding site maximum (Bmax) of 3.97 fmol/mg protein. Investigating several Ang II signal transduction pathways on these cells, we found that Ang II (10(-8) to 10(-6) M) does not affect basal cAMP, cGMP, arachidonic acid release, prostacyclin release, intracellular Ca2+ mobilization or thymidine incorporation in the PC12W cells. Nerve growth factor, cAMP, 5-fluorouridine deoxyriboside modulation of the number of AT2 receptor sites in PC12W cells failed to unmask any Ang II effects on basal cAMP, cGMP and intracellular Ca2+ mobilization. In conclusion, the present study confirms the exclusive presence of AT2 binding sites in the PC12W cells. However, these binding sites are not functionally coupled to common signal transduction pathways.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Leung KH,Roscoe WA,Smith RD,Timmermans PB,Chiu ATdoi
10.1016/0922-4106(92)90143-jkeywords:
subject
Has Abstractpub_date
1992-09-01 00:00:00pages
63-70issue
1eissn
0014-2999issn
1879-0712journal_volume
227pub_type
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journal_title:European journal of pharmacology
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