Identification of neurotensin receptors associated with calcium channels and prolactin release in rat pituitary

M. Memo, L. Castelletti, A. Valerio, C. Missale, P. F. Spano

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Neurotensin (NT) is now reasonably well established as a neurotransmitter or neuromodulator candidate in the CNS. In the present study, we characterized the NT receptors in dispersed cells from the anterior love of rat pituitary and investigated the involvement of both cyclic AMP and calcium in the release of prolactin (PRL) induced by NT receptor stimulation. The [3H]NT binding to membranes from anterior pituitary dispersed cells was found saturable and stereospecific. Scatchard analysis of the data gave a straight line indicating a B(max) value of 121 ± 11 fmol/mg protein and a K(D) value of 1.4 ± 0.2 nM. The calculated IC50 values for [3H]NT binding were 5.8 nM for NT, 7.8 nM for L-Phe-NT, and 3,000 nM for the pharmacologically inactive form D-Phe-NT. NT, up to a concentration of 1 μM, did not affect the cyclic AMP generating system in homogenates of anterior pituitary from male or lactating female rats. The same pattern of results was obtained for cyclic AMP formation in intact cells. NT and its analogs stereospecifically enhanced the influx of calcium into dispersed cells from rat anterior pituitary. The effect was time-and dose-dependent. It appeared to be associated with neurotransmitter-operated calcium channels since: (1) preincubation of the cells with tetrodotoxin did not affect the increase in calcium influx induced by NT; (2) concentrations of verapamil that counteract the influx of calcium induced by potassium lacked the capacity to modify the influx of calcium induced by NT; and (3) NT lost its capacity to release PRL in the absence of extracellular calcium. The significant correlation of the effective concentrations of NT and its analogs for binding and biological activities indicates that occupancy of NT receptors in anterior pituitary modifies calcium channel permeability of the cell membranes, resulting in an accumulation of intracellular calcium that participates in the cascade of events that are ultimately expressed as an enhanced release of PRL.

Original languageEnglish
Pages (from-to)1682-1688
Number of pages7
JournalJournal of Neurochemistry
Issue number6
Publication statusPublished - 1986

ASJC Scopus subject areas

  • Biochemistry
  • Cellular and Molecular Neuroscience


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