Prolactin inhibitors

In the search for new prolactin inhibitors, several 6-alkyl-derivatives of (d-8-ergolin-l-yl)acetamide have been made,46" together with several bis(ergolin-2- yl)alkanes,466 the latter being the products of acid-catalysed condensation of ergoline with ketones. 

Prolactin inhibitors. Dopamine released from hypothalamic neurosecretory nerve cells inhibits the secretion of prolactin from the adenohypophysis (p. 238). Prolactin promotes production of breast milk during the lactation period moreover it inhibits the secretion of gonadorelin. D2 receptor agonists prevent prolactin secretion and can be used for weaning and the treatment of fe-... 

Khalfallah Y, Claustrat B, Grochowicki M, Flocard F, Horlait S, Serusclat P, Sassolas G. Effects of a new prolactin inhibitor, CV 205-502, in the treatment of human macroprolactinomas. J Clin Endocrinol Metab 1990 71(2) 354-9. 

G02C B Prolactin inhibitors Bromocryptine is a semisynthetic ergot alkaloid, 2-bromoergo-cryptine and acts as an dopamine-agonist (i.e. has the same effect as dopamine) with a long duration and is an inhibitor of prolactin and growth hormone. For the indication inhibition and cessation of lactation one starts with a low dose 2.5 mg taken with food for two weeks. 

Acid maleate, CnH Oj, Cuvafir, Dopergin, Eunal, Lysenyl. Prisms from ethanol, mp 200 (dec). [a]f,° +288" (c = 0.5 in methanol), uv max (methanol) 313 nm. LDVI i.v in mice 14.4 mg/kg (Votava, Lamplova). therap cat Anti migraine prolactin inhibitor. 

New ergoline derivatives prepared for pharmacological evaluation include several urethanes of general formula (63), several N-alkylated N-norelymo-clavines," of which the Af-propyl derivative (64) proved to be as active as the most potent prolactin inhibitor reported to date, further examples of modified dihydrolysergic acid derivatives in which a substituent has been introduced into... 

The preparation of bromocryptine (2-bromo-a-ergocryptine), by the bromination of pure a-ergocryptine by means of iV-bromosuccinimide, has been described, together with details of 2-bromo-a-ergocryptine methanesulphonate, the clinically useful prolactin inhibitor. ... 

Table 1. Effect of prolactin inhibitor bromocriptine on the percent of... 

Gonadotropin-releasing hormone Growth hormone-releasing hormone Corticotropin-releasing hormone Prolactin inhibitor factor Amine... 

Pergolide (53a) is one of the strongest dopamine agonists and prolactin inhibitors. It is metabolised into four products resulting from oxidation and N-6 dealkylation (Clemens etal, 1993 Kerr etal., 1981). Pergolide sulfoxide (53b)... 

Cabergoline (58a) is another modern prolactine inhibitor with prolonged effect (Figure 20). This drug is metabolised in human organism similarly as the above... 

Therapeutical use dopamine agonist, antiparkinsonian, prolactine inhibitor, treatment of acromegaly 1975... 

Structurally closely related to LSD, Lisuride (226) is a compound having a 3,3-dimethylureido substituent, at die 9-position of the ergoline skeleton, and was first prepared in 1960 as a dopamine Dj-receptor agonist (98). Lisuride, as its acid maleate, is commercially available under Ae names of Cuvalit, Dopergin, Eunal, or Lysenyl, and is used clinically as an antimigraine and also as a prolactin inhibitor. The pharmacological activi and toxicity of lisuride were... 

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