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Evidence that LY-141865 specifically stimulates the D-2 dopamine receptor

Nature volume 292, pages 463–465 (1981)Cite this article

Abstract

Available evidence suggests the existence of multiple categories of dopamine receptor1–4. According to the classification scheme used here5, dopamine receptors can be divided into two general categories, D-l and D-2. The dopamine receptors in the bovine parathyroid gland6–8 and carp retina9,10 exemplify the former category, and the dopamine receptors on the mammotrophs11,12 and melanotrophs13,14 of the pituitary gland exemplify the latter. Stimulation of a D-1 receptor enhances the formation of cyclic AMP, whereas stimulation of a D-2 receptor does not4,5. The availability of dopaminergic agonists which specifically activate either a D-1 or a D-2 receptor would facilitate pharmacological investigation of the physiological responses to dopamine; however, to date, an agonist specific for the D-2 receptor has not been available. Dopamine and other catecholamines stimulate both types of receptor6–14; ergolines (such as lergotrile and lisuride) stimulate the D-2 receptor13–15 but antagonize the D-1 receptor8,16–18; some agonists acting on the D-2 receptor (such as apomorphine) both stimulate and block the D-1 receptor6,8. Although one report claims that S-584 may selectively stimulate the dopamine receptor on mammotrophs19, according to another, S-584 stimulates the striatal dopamine-sensitive adenylate cyclase20. Several recently synthesized compounds containing various portions of the ergoline ring system stimulate the D-2 receptor on mammotrophs21. We report here that one of these ergoline analogues, LY-141865 or ‘38, R = pro’21, stimulates the D-2 receptor in the intermediate lobe (IL) of the rat pituitary gland but does not interact with the D-1 receptor in carp retina.

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Authors and Affiliations

  1. Experimental Therapeutics Branch, NINCDS, National Institutes of Health, Bethesda, Maryland, 20205, USA

    K. Tsuruta, E. A. Frey, C. W. Grewe & T. E. Cote

  2. Laboratory of Clinical Science, NIMH, National Institutes of Health, Bethesda, Maryland, 20205, USA

    R. L. Eskay

Authors
  1. K. Tsuruta
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  2. E. A. Frey
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  3. C. W. Grewe
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  4. T. E. Cote
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  6. J. W. Kebabian
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Tsuruta, K., Frey, E., Grewe, C. et al. Evidence that LY-141865 specifically stimulates the D-2 dopamine receptor. Nature 292, 463–465 (1981). https://doi.org/10.1038/292463a0

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