Reduction of LH-RH pituitary and estradiol uterine binding sites by a superactive analog of luteinizing hormone-releasing hormone

E. Pedroza; J. A. Vilchez-Martinez; D. H. Coy; A. Arimura; A. V. Schally

doi:10.1016/0006-291X(80)91580-6

Reduction of LH-RH pituitary and estradiol uterine binding sites by a superactive analog of luteinizing hormone-releasing hormone

E. Pedroza, J. A. Vilchez-Martinez, D. H. Coy, A. Arimura, A. V. Schally

Research output: Contribution to journal › Article › peer-review

21 Scopus citations

Abstract

The ability of the Luteinizing Hormone-Releasing Hormone (LH-RH) analogs to displace LH-RH from its pituitary receptors was evaluated in vitro. The two superactive analogs tested showed higher potency than the antagonists and LH-RH itself, D-Trp⁶-LH-RH being the most potent. The LH-RH specific binding activity in the pituitary fluctuated throughout the age of the rats. The highest number of LH-RH binding sites were seen on day 35 of age (276 fmol x 10^-2/pit) and an increment was induced by 0.05 μg D-Trp⁶-LH-RH (400 fmol x 10^-2/pit). However, 1 μg D-Trp⁶-LH-RH reduced the binding of LH-RH at all the times studied. In the control animals the number of estradiol binding sites increased on day 42 of age, and 0.05 μg D-Trp⁶-LH-RH augmented them on day 35 of age. On the contrary, 1 μg D-Trp⁶-LH-RH diminished the estradiol uterine receptors at all the times studied. Similar results were obtained in the ovariectomized-hypophysectomized rats on day 35 of age. Our studies demonstrated a biphasic action of D-Trp⁶-LH-RH on LH-RH pituitary receptors and a direct effect on uterus which could be mediated through the uterine estradiol receptors.

Original language	English (US)
Pages (from-to)	1056-1062
Number of pages	7
Journal	Topics in Catalysis
Volume	95
Issue number	3
DOIs	https://doi.org/10.1016/0006-291X(80)91580-6
State	Published - 1980
Externally published	Yes

ASJC Scopus subject areas

Catalysis
Chemistry(all)
Biochemistry
Biophysics
Molecular Biology

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10.1016/0006-291X(80)91580-6

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title = "Reduction of LH-RH pituitary and estradiol uterine binding sites by a superactive analog of luteinizing hormone-releasing hormone",

abstract = "The ability of the Luteinizing Hormone-Releasing Hormone (LH-RH) analogs to displace LH-RH from its pituitary receptors was evaluated in vitro. The two superactive analogs tested showed higher potency than the antagonists and LH-RH itself, D-Trp6-LH-RH being the most potent. The LH-RH specific binding activity in the pituitary fluctuated throughout the age of the rats. The highest number of LH-RH binding sites were seen on day 35 of age (276 fmol x 10-2/pit) and an increment was induced by 0.05 μg D-Trp6-LH-RH (400 fmol x 10-2/pit). However, 1 μg D-Trp6-LH-RH reduced the binding of LH-RH at all the times studied. In the control animals the number of estradiol binding sites increased on day 42 of age, and 0.05 μg D-Trp6-LH-RH augmented them on day 35 of age. On the contrary, 1 μg D-Trp6-LH-RH diminished the estradiol uterine receptors at all the times studied. Similar results were obtained in the ovariectomized-hypophysectomized rats on day 35 of age. Our studies demonstrated a biphasic action of D-Trp6-LH-RH on LH-RH pituitary receptors and a direct effect on uterus which could be mediated through the uterine estradiol receptors.",

author = "E. Pedroza and Vilchez-Martinez, {J. A.} and Coy, {D. H.} and A. Arimura and Schally, {A. V.}",

year = "1980",

doi = "10.1016/0006-291X(80)91580-6",

language = "English (US)",

volume = "95",

pages = "1056--1062",

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T1 - Reduction of LH-RH pituitary and estradiol uterine binding sites by a superactive analog of luteinizing hormone-releasing hormone

AU - Pedroza, E.

AU - Vilchez-Martinez, J. A.

AU - Coy, D. H.

AU - Arimura, A.

AU - Schally, A. V.

PY - 1980

Y1 - 1980

N2 - The ability of the Luteinizing Hormone-Releasing Hormone (LH-RH) analogs to displace LH-RH from its pituitary receptors was evaluated in vitro. The two superactive analogs tested showed higher potency than the antagonists and LH-RH itself, D-Trp6-LH-RH being the most potent. The LH-RH specific binding activity in the pituitary fluctuated throughout the age of the rats. The highest number of LH-RH binding sites were seen on day 35 of age (276 fmol x 10-2/pit) and an increment was induced by 0.05 μg D-Trp6-LH-RH (400 fmol x 10-2/pit). However, 1 μg D-Trp6-LH-RH reduced the binding of LH-RH at all the times studied. In the control animals the number of estradiol binding sites increased on day 42 of age, and 0.05 μg D-Trp6-LH-RH augmented them on day 35 of age. On the contrary, 1 μg D-Trp6-LH-RH diminished the estradiol uterine receptors at all the times studied. Similar results were obtained in the ovariectomized-hypophysectomized rats on day 35 of age. Our studies demonstrated a biphasic action of D-Trp6-LH-RH on LH-RH pituitary receptors and a direct effect on uterus which could be mediated through the uterine estradiol receptors.

AB - The ability of the Luteinizing Hormone-Releasing Hormone (LH-RH) analogs to displace LH-RH from its pituitary receptors was evaluated in vitro. The two superactive analogs tested showed higher potency than the antagonists and LH-RH itself, D-Trp6-LH-RH being the most potent. The LH-RH specific binding activity in the pituitary fluctuated throughout the age of the rats. The highest number of LH-RH binding sites were seen on day 35 of age (276 fmol x 10-2/pit) and an increment was induced by 0.05 μg D-Trp6-LH-RH (400 fmol x 10-2/pit). However, 1 μg D-Trp6-LH-RH reduced the binding of LH-RH at all the times studied. In the control animals the number of estradiol binding sites increased on day 42 of age, and 0.05 μg D-Trp6-LH-RH augmented them on day 35 of age. On the contrary, 1 μg D-Trp6-LH-RH diminished the estradiol uterine receptors at all the times studied. Similar results were obtained in the ovariectomized-hypophysectomized rats on day 35 of age. Our studies demonstrated a biphasic action of D-Trp6-LH-RH on LH-RH pituitary receptors and a direct effect on uterus which could be mediated through the uterine estradiol receptors.

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Reduction of LH-RH pituitary and estradiol uterine binding sites by a superactive analog of luteinizing hormone-releasing hormone

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