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Specific Effect of CV 205-502, a Potent Nonergot Dopamine Agonist, During a Combined Anterior Pituitary Function Test^*

Clinique Médicale et Division d’Endocrinologie, Department of Medicine, University Hospital CH-1211 Geneva 4
Clinical Research, Sandoz Ltd. (K.A., J.B.) CH-4002 Basel, Switzerland

Address all correspondence and requests for reprints to: Dr. R. C. Gaillard, M.D., Clinique Medicale, University Hospital, CH-1211 Geneva 4, Switzerland.

CV 205–502, an octahydrobenzo[g]quinoline, is a dopamine agonist compound that is not an ergot or ergoline derivative. To investigate the site of action of CV 205-502, three groups of five men were given single daily doses of CV 205–502 (0.04, 0.06, or 0.08 mg/day, doses that suppress plasma PRL by 60–80% for 24 h) for 5 days; on day 6 a combined anterior pituitary function test using iv administration of four hypothalamic releasing hormones (TRH, 200 µg; GHRH, 100 µg; CRH, 100 µg; LHRH, 100 ng) was performed. One month later the challenge tests were repeated to obtain control values. The following hormones were measured by RIA in plasma: TSH, ACTH, cortisol, PRL, GH, LH, FSH, and testosterone. With the exception of plasma PRL levels, basal and releasing hormone-stimulated values were similar after CV 205–502 administration and after the 1-month washout period. Basal plasma PRL was lower after CV 205–502 administration, and the response to TRH was attenuated by all three doses of CV 205–502 (the mean percent inhibition values were 76%, 93%, and 94%, respectively). All three doses of CV 205–502 were well tolerated, and another group of men well tolerated 0.1 mg daily. The results confirm that CV 205–502 is a potent dopamine agonist, which directly inhibits lactotropic cells but has no effect on other pituitary cell types.

^* This work was supported by the Swiss NSF (Grants 3.814.084 and 3.091.087) and Sandoz Ltd. (Basel, Switzerland).

Received January 21, 1988.

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