Detail of "19875-60-6"

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Lisuride hydrogen maleate: evidence for a long lasting dopaminergic activity in humans

Lisuride hydrogen maleate: evidence for a long lasting dopaminergic activity in humans. Liuzzi, A.; Chiodini, P. G.; Oppizzi, G.; Botalla, L.; Verde, G.; De Stefano, L.; Colussi, G.; Graef, K. J.; Horowski, R. (Cent. Endocrinol., Osp. Maggiore Ca Granda, Milan, Italy). J. Clin. Endocrinol. Metab., 46(2), 196-202 (English) 1978. CODEN: JCEMAZ. ISSN: 0021-972X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) In 12 acromegalics a single oral dose of 0.2 mg lisuride hydrogen maleate (I) [19875-60-6] reduced plasma prolactin (PRL) [9002-62-4], but not growth hormone (GH) [9002-72-6] concns. Three-tenths milligram of the drug significantly reduced plasma levels of the 2 hormones. Four-tenths milligram of I did not augment this inhibitory effect. Plasma PRL levels were suppressed in all patients, whereas GH levels were reduced by >50% in only 7 patients who also responded to the administration of 2.5 mg bromocriptine (CB154). In the patients unresponsive to I, CB154 also failed to change GH levels. The suppressive effect of I started at 60 min (at 150 min for CB154) and plasma GH and PRL levels were still markedly suppressed at 300 min. Plasma GH and PRL concns. were consistently reduced in 2 acromegalic patients during 2 wk of chronic treatment with 0.3 mg I, 4 times a day. In normal subjects, TRH-induced PRL release was inhibited by pretreatment with 0.3 mg I. The similarity in the effects of I and CB154 suggests that the obsd. effects of I on GH and PRL are attributable to the known dopaminergic activity of the drug. This is supported by the data showing that pimozide effectively counteracted the inhibitory action of I on GH and PRL release. Thus, I may be of value in the medical treatment of acromegaly and hyperprolactinemic states.

Effect of lisuride and LSD on monoamine synthesis after axotomy or reserpine treatment in rat brain

Effect of lisuride and LSD on monoamine synthesis after axotomy or reserpine treatment in rat brain. Kehr, Wolfgang; Speckenbach, Wolfgang; Neumeister, Ruth (Dep. Neuropsychopharmakol., Schering A.-G., Berlin, Ger.). Naunyn-Schmiedeberg's Arch. Pharmacol., 301(3), 163-9 (English) 1978. CODEN: NSAPCC. ISSN: 0369-5565. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) The effect of LSD tartrate (I-tartrate) [17676-08-3] and lisuride hydrogen maleate (II-hydrogen maleate) [19875-60-6] on the synthesis of monoamines was evaluated in rat brain regions in vivo. I (50-1000 mg/kg, i.p.) caused a dose-dependent increase in dopa [59-92-7] formation and a slight elevation of tyrosine [60-18-4] and tryptophan [73-22-3] concns. in the intact rat forebrain; moreover, it reduced the accumulation of 5-hydroxytryptophan [56-69-9]. The increase in dopa formation in the terminal system of the rat forebrain following an axotomy of the ascending monoaminergic fiber system was antagonized by I at 0.5 mg/kg, i.p. Haloperidol (2 mg/kg, i.p.) counteracted the effect of I. The increase in dopa formation in corpus striatum and the dopamine-rich part of the limbic system following treatment with reserpine was antagonized by II as well as by I. However, II was at least 10 times as potent as I. In reserpinized animals I counteracted the inhibitory effect on dopa accumulation of the direct dopamine receptor stimulant apomorphine while II did not. The data suggest that I is a weak agonist at dopamine receptors in vivo with partial receptor blocking properties at higher doses, while the action of II on dopamine receptors is a potent, purely agonistic one.