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Bromocriptine and sulpiride competitively inhibit estrogen binding to its receptor in the adrenal gland

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  • Biochemistry and Biophysics, Metabolism, Neurobiology, Pharmacology
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Summary

Bromocriptine and sulpiride incubated simultaneously with [3H]-estradiol in the cytosol from adrenal glands of adult male rats, yielded curves typical of competitive inhibition as analyzed by Lineweaver-Burk plots. The inhibition constant for both drugs was approximately 108 M−1, only 10 times lower than the association constant for estradiol.

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Authors and Affiliations

  1. Instituto de Biologia y Medicina Experimental, Obligado 2490, 1428, Buenos Aires, Argentina

    I. A. Lüthy & R. S. Calandra

Authors
  1. I. A. Lüthy
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  2. R. S. Calandra
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Consejo Nacional de Investigaciones Cientificas y Técnicas.

Acknowledgments. The authors are deeply indebted to Mrs Diana Bas for her skillful technical assistance, and Mrs Elaine Leclerc, Mrs Dora Beatriz Destéfano for typing the manuscript, and to Dr James G. Chafouleas (CHUL, Quebec) and Dr Lawrence Crim (Newfoundland, Canada) for their helpful criticism.

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Lüthy, I.A., Calandra, R.S. Bromocriptine and sulpiride competitively inhibit estrogen binding to its receptor in the adrenal gland. Experientia 42, 136–138 (1986). https://doi.org/10.1007/BF01952433

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  • DOI: https://doi.org/10.1007/BF01952433

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