Antagonistic activity of analogs of luteinizing hormone-releasing hormone (LH-RH) in vitro

D. H. Coy; F. Labrie; M. Savary; E. J. Coy; A. V. Schally

doi:10.1016/0303-7207(76)90083-6

Antagonistic activity of analogs of luteinizing hormone-releasing hormone (LH-RH) in vitro

D. H. Coy, F. Labrie, M. Savary, E. J. Coy, A. V. Schally

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

6 Scopus citations

Abstract

The ability of eighteen analogs of LH-RH to inhibit LH-RH-induced LH release was tested in primary cultures of rat anterior pituitary cells. [Des-His²]LH-RH, [Des-His², D-Leu⁶]LH-RH and [Des-His², D-Phe⁶]LH-RH inhibited 50% of LH-RH-induced LH release at molar ratios (MR₅₀s) of 3000, 500 and 60, respectively, while [D-Phe²]LH-RH, [D-Phe², D-Leu⁶]LH-RH and [D-Phe², D-Phe⁶]LH-RH had similar effects at MR₅₀s of 1000, 150 and 25, respectively. This indicates that substitution of D-phenylalanine for histidine at position 2 of LH-RH leads to compounds approximately 3-fold more potent than the corresponding [Des-His²]-analogs. [D-Phe², D-Phe⁶]LH-RH, the most potent antagonist tested has however a slight agonistic activity (0.003% that of LH-RH itself). [D-Phe², D-Phe⁶, Phe⁷]LH-RH, [D-Phe², Phe³, D-Phe⁶]-LH-RH and [D-Phe², Phe⁵, D-Phe⁶]LH-RH inhibit 50% of LH-RH action at MR₅₀s of 400, 100 and 75, respectively. All of the analogs mentioned in the last group have LH-releasing activities below 1/100,000 that of LH-RH itself.

Original language	English (US)
Pages (from-to)	201-208
Number of pages	8
Journal	Molecular and Cellular Endocrinology
Volume	5
Issue number	3-4
DOIs	https://doi.org/10.1016/0303-7207(76)90083-6
State	Published - 1976
Externally published	Yes

Keywords

antagonistic analogs
cell culture
LH
pituitary

ASJC Scopus subject areas

Endocrinology
Endocrinology, Diabetes and Metabolism

UN SDGs

This output contributes to the following Sustainable Development Goal(s)

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title = "Antagonistic activity of analogs of luteinizing hormone-releasing hormone (LH-RH) in vitro",

abstract = "The ability of eighteen analogs of LH-RH to inhibit LH-RH-induced LH release was tested in primary cultures of rat anterior pituitary cells. [Des-His2]LH-RH, [Des-His2, D-Leu6]LH-RH and [Des-His2, D-Phe6]LH-RH inhibited 50% of LH-RH-induced LH release at molar ratios (MR50s) of 3000, 500 and 60, respectively, while [D-Phe2]LH-RH, [D-Phe2, D-Leu6]LH-RH and [D-Phe2, D-Phe6]LH-RH had similar effects at MR50s of 1000, 150 and 25, respectively. This indicates that substitution of D-phenylalanine for histidine at position 2 of LH-RH leads to compounds approximately 3-fold more potent than the corresponding [Des-His2]-analogs. [D-Phe2, D-Phe6]LH-RH, the most potent antagonist tested has however a slight agonistic activity (0.003% that of LH-RH itself). [D-Phe2, D-Phe6, Phe7]LH-RH, [D-Phe2, Phe3, D-Phe6]-LH-RH and [D-Phe2, Phe5, D-Phe6]LH-RH inhibit 50% of LH-RH action at MR50s of 400, 100 and 75, respectively. All of the analogs mentioned in the last group have LH-releasing activities below 1/100,000 that of LH-RH itself.",

keywords = "antagonistic analogs, cell culture, LH, pituitary",

author = "Coy, {D. H.} and F. Labrie and M. Savary and Coy, {E. J.} and Schally, {A. V.}",

note = "Funding Information: of the Medical Research Council of Canada",

year = "1976",

doi = "10.1016/0303-7207(76)90083-6",

language = "English (US)",

volume = "5",

pages = "201--208",

journal = "Molecular and Cellular Endocrinology",

issn = "0303-7207",

publisher = "Elsevier Ireland Ltd",

number = "3-4",

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TY - JOUR

T1 - Antagonistic activity of analogs of luteinizing hormone-releasing hormone (LH-RH) in vitro

AU - Coy, D. H.

AU - Labrie, F.

AU - Savary, M.

AU - Coy, E. J.

AU - Schally, A. V.

N1 - Funding Information: of the Medical Research Council of Canada

PY - 1976

Y1 - 1976

N2 - The ability of eighteen analogs of LH-RH to inhibit LH-RH-induced LH release was tested in primary cultures of rat anterior pituitary cells. [Des-His2]LH-RH, [Des-His2, D-Leu6]LH-RH and [Des-His2, D-Phe6]LH-RH inhibited 50% of LH-RH-induced LH release at molar ratios (MR50s) of 3000, 500 and 60, respectively, while [D-Phe2]LH-RH, [D-Phe2, D-Leu6]LH-RH and [D-Phe2, D-Phe6]LH-RH had similar effects at MR50s of 1000, 150 and 25, respectively. This indicates that substitution of D-phenylalanine for histidine at position 2 of LH-RH leads to compounds approximately 3-fold more potent than the corresponding [Des-His2]-analogs. [D-Phe2, D-Phe6]LH-RH, the most potent antagonist tested has however a slight agonistic activity (0.003% that of LH-RH itself). [D-Phe2, D-Phe6, Phe7]LH-RH, [D-Phe2, Phe3, D-Phe6]-LH-RH and [D-Phe2, Phe5, D-Phe6]LH-RH inhibit 50% of LH-RH action at MR50s of 400, 100 and 75, respectively. All of the analogs mentioned in the last group have LH-releasing activities below 1/100,000 that of LH-RH itself.

AB - The ability of eighteen analogs of LH-RH to inhibit LH-RH-induced LH release was tested in primary cultures of rat anterior pituitary cells. [Des-His2]LH-RH, [Des-His2, D-Leu6]LH-RH and [Des-His2, D-Phe6]LH-RH inhibited 50% of LH-RH-induced LH release at molar ratios (MR50s) of 3000, 500 and 60, respectively, while [D-Phe2]LH-RH, [D-Phe2, D-Leu6]LH-RH and [D-Phe2, D-Phe6]LH-RH had similar effects at MR50s of 1000, 150 and 25, respectively. This indicates that substitution of D-phenylalanine for histidine at position 2 of LH-RH leads to compounds approximately 3-fold more potent than the corresponding [Des-His2]-analogs. [D-Phe2, D-Phe6]LH-RH, the most potent antagonist tested has however a slight agonistic activity (0.003% that of LH-RH itself). [D-Phe2, D-Phe6, Phe7]LH-RH, [D-Phe2, Phe3, D-Phe6]-LH-RH and [D-Phe2, Phe5, D-Phe6]LH-RH inhibit 50% of LH-RH action at MR50s of 400, 100 and 75, respectively. All of the analogs mentioned in the last group have LH-releasing activities below 1/100,000 that of LH-RH itself.

KW - antagonistic analogs

KW - cell culture

KW - LH

KW - pituitary

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U2 - 10.1016/0303-7207(76)90083-6

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C2 - 782958

AN - SCOPUS:0016987779

VL - 5

SP - 201

EP - 208

JO - Molecular and Cellular Endocrinology

JF - Molecular and Cellular Endocrinology

SN - 0303-7207

IS - 3-4

ER -

Antagonistic activity of analogs of luteinizing hormone-releasing hormone (LH-RH) in vitro

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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