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Guanine nucleotide regulation of dopamine receptor agonist affinity states in rat estradiol-induced pituitary tumors
Authors:T Di Paolo  P Falardeau
Institution:1. Institute of Metabolism and Systems Research, University of Birmingham, Birmingham, UK;2. Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, UK;3. Department of Endocrinology, Queen Elizabeth Hospital, University Hospitals Birmingham NHS Foundation Trust, Birmingham, UK
Abstract:We have investigated dopamine (DA) receptor agonist high- and low-affinity states in female rat estradiol-induced prolactin (PRL)-secreting pituitary tumors and intact pituitary tissue. Estradiol treatment increased the anterior pituitary weight 9-fold and plasma prolactin levels 74-fold and these measures are correlated (R = 0.745, n = 73, p less than 0.001). Competition for 3H]-spiperone binding to the DA receptor by apomorphine was compared in normal and adenomatous pituitary tissue. The inhibition constants (Ki) and the proportions of the two apomorphine sites are unchanged in tumors compared to intact pituitary tissue. Guanosine 5'-beta-gamma-imino]triphosphate (Gpp(NH)p) causes complete conversion of the high into low affinity dopaminergic agonist site in normal pituitary and in tumors. These results suggest that rats with primary estradiol-induced pituitary tumors have normal and functional DA receptors.
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