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Endocrinology Vol. 139, No. 1 432-435
Copyright © 1998 by The Endocrine Society

ARTICLES

Identification of a Pituitary Growth Hormone-Releasing Peptide (GHRP) Receptor Subtype by Photoaffinity Labeling

H. Ong, N. McNicoll, E. Escher, R. Collu, R. Deghenghi, V. Locatelli, E. Ghigo, G. Muccioli, M. Boghen and M. Nilsson

Faculty of Pharmacy (H.O., N.McN.) and Ste-Justine Hospital (R.C.), University of Montréal, Montréal, Canada; Department of Pharmacology (E.E.), University of Sherbrooke, Sherbrooke, Canada; Europeptides (R.D.), Argenteuil, France; Department of Pharmacology (V.L.), University of Milan, Milan, Italy; Department of Internal Medecine (E.G.) and Department of Anatomy (G.M.), University of Turin, Turin, Italy; Pharmacia & Upjohn (M.B., M.N.), Stockholm, Sweden

Address all correspondence and requests for reprints to: Dr. Huy Ong, Université de Montréal, Faculté de Pharmacie, C.P. 6128, Succ. Centre-Ville, Montréal, Québec H3C 3J7, Canada.


   Abstract
Top
 Abstract
 
Hexarelin, an analogue of GHRP-6, in which D-Tryptophan has been replaced by its 2-methyl derivative, is known to release growth hormone (GH) in vivo and in vitro by direct action on receptors present in anterior pituitary cells. Measurement of second messengers (c-AMP, Ca++, IP3) upon somatotrophs stimulation, suggests the existence of more than one GHRP receptor subtype. In order to document such an hypothesis, we have used a new photoactivatable derivative of Hexarelin, Tyr-Bpa-Ala-Hexarelin. This derivative was shown to be fully active in the release of GH in vivo with neonate rats. Using this photoactivatable ligand, we have specifically labeled a protein with an apparent Mr of 57 000 in human, bovine and porcine anterior pituitary membranes. Hexarelin and the spiroindoline sulfonamide MK-0677 displaced the Mr -57 000 photolabeled band with an apparent ED50 of 6x10-7 M and 2x10-5 M respectively. Taking into account the high efficiency (>60%) of covalent incorporation of the Bpa residue, this photoactivatable Hexarelin derivative has allowed the identification of a pituitary GHRP receptor subtype, which is apparently distinct from the recently cloned GH secretagogue receptor.

Received July 16, 1997.




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This Article
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