Identification of alpha 2-adrenergic receptors in chicken pineal gland using [3H]rauwolscine

The norepinephrine-induced inhibition of avian pineal N-acetyltransferase activity appears to be mediated by alpha 2-adrenergic receptors. In this study, alpha 2-adrenergic receptors in the chicken pineal gland were directly identified by radioligand binding. Membrane preparations of pineal glands f...

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Veröffentlicht in:Journal of neurochemistry 1988-07, Vol.51 (1), p.81-86
Hauptverfasser: Bylund, D B, Rudeen, P K, Petterborg, L J, Ray-Prenger, C
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container_issue 1
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container_title Journal of neurochemistry
container_volume 51
creator Bylund, D B
Rudeen, P K
Petterborg, L J
Ray-Prenger, C
description The norepinephrine-induced inhibition of avian pineal N-acetyltransferase activity appears to be mediated by alpha 2-adrenergic receptors. In this study, alpha 2-adrenergic receptors in the chicken pineal gland were directly identified by radioligand binding. Membrane preparations of pineal glands from chickens from 1 to 6 weeks of age were examined using [3H]rauwolscine, a selective alpha 2-adrenergic receptor antagonist, to characterize the binding sites. The results indicate no ontological change in either the affinity (KD) or density of receptor binding sites (Bmax) during the time span examined. The binding was saturable and of high affinity with a mean KD of 0.27 +/- 0.01 nM and a mean Bmax of 242 +/- 12 fmol/mg protein. Further characterization of these binding sites indicated that the alpha 2-adrenergic receptor is of the alpha 2A subtype, since prazosin and ARC-239 bound with low affinities and oxymetazoline bound with high affinity.
doi_str_mv 10.1111/j.1471-4159.1988.tb04838.x
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subjects Adrenergic alpha-Antagonists
Animals
Brimonidine Tartrate
Cell Membrane - metabolism
Chickens - metabolism
Circadian Rhythm
Female
Isoquinolines - metabolism
Isoquinolines - pharmacology
Male
Pindolol - metabolism
Pineal Gland - metabolism
Piperazines
Quinoxalines - metabolism
Quinoxalines - pharmacology
Receptors, Adrenergic, alpha - drug effects
Receptors, Adrenergic, alpha - metabolism
Tritium
Yohimbine - metabolism
Yohimbine - pharmacology
title Identification of alpha 2-adrenergic receptors in chicken pineal gland using [3H]rauwolscine
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