PMID: 8460121Mar 15, 1993Paper

A method for evaluation of activity of antagonistic analogs of growth hormone-releasing hormone in a superfusion system

Proceedings of the National Academy of Sciences of the United States of America
Z Rekasi, A V Schally

Abstract

Antagonistic analogs of growth hormone-releasing hormone (GHRH) are being synthesized in our laboratory for various clinical applications, including treatment of certain endocrine disorders and insulin-like growth factor I-dependent tumors. To evaluate the endocrine effect of these GHRH antagonists, a sensitive dynamic in vitro system has been developed. The concentration causing 50% inhibition (IC50) of the standard GHRH antagonist human [N-Ac-Tyr1,D-Arg2]GHRH-(1-29)-NH2 is 4.5 x 10(-8) M in our dispersed pituitary cell superfusion system. This value is 11 times less than that measured in earlier static pituitary cell cultures. This reliable dynamic system is simple, fast, and inexpensive and not only makes it possible to obtain quantitative data on the inhibitory capacity of the antagonists but also provides information about the intrinsic GHRH activity of the analog. The dynamic interactions of the GHRH antagonist, the GHRH receptors, and GH release can also be evaluated by this superfusion system. The pulsatile GH release induced by 10(-9) M human GHRH-(1-29)-NH2 was inhibited by two modes of application, preincubation and simultaneous administration of the GHRH antagonist (10(-9) to 10(-6) M). The reduction in GHRH-stimula...Continue Reading

References

Jan 1, 1978·Annual Review of Biochemistry·A V SchallyC A Meyers
Jun 17, 1992·Journal of the National Cancer Institute·M PollakR Bell
Feb 28, 1990·Biochemical and Biophysical Research Communications·K SatoN Ling
Feb 21, 1990·Journal of the National Cancer Institute·M N PollakM Richard
Feb 1, 1985·Journal of Medicinal Chemistry·D H CoyV A Lance
Dec 1, 1982·Proceedings of the National Academy of Sciences of the United States of America·P BrazeauR Guillemin

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Citations

Nov 5, 1999·Trends in Endocrinology and Metabolism : TEM·A V Schally, J L Varga
Dec 6, 1994·Proceedings of the National Academy of Sciences of the United States of America·M ZarandiA V Schally
Feb 3, 2004·Proceedings of the National Academy of Sciences of the United States of America·Jozsef L VargaMarta Zarandi
Jan 20, 1999·Proceedings of the National Academy of Sciences of the United States of America·J L VargaZ Rékási
Mar 27, 1998·The Journal of Peptide Research : Official Journal of the American Peptide Society·K TothA V Schally

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