Pharmacology Ergolines

The technical aspect of 2-bromo-a-ergocryptine synthesis, including the characterisation and significance of the impurities obtained in the production process, were reviewed. In the continuation new ergolene and ergoline compounds were synthesized and tested for the pharmacological activity. 

In general, the introduction of bromine in ergolene or ergoline structure results in remarkable change in pharmacological activity of the parent compounds. After intensive research work of several research groups many useful methods for 2-bromination have been developed. Practically, all methods are accompanied with many side reactions. Therefore, the best attainable yields of product 2 are in the range of 60 - 70 % of the theory ... 

A series of corresponding ergoline and ergolene derivatives was synthesized. The ergotamine derivative showed an interesting antihypertensive activity. Unfortunately, the substance has very poor solubility and stability and therefore the further pharmacological evaluation was stopped (ref. 25). 

Other ergoline derivatives of potential pharmacological value that have been reported include the nitroso-compounds (49) and (50), which show some activity against L 1210 leukaemia in mice, and the elymoclavine-derived urethane (51),... 

Ergot Alkaloids.—A supplement to Pharmacology that is devoted to the ergot alkaloids is introduced by reviews on the history " and the general pharmacology " of this group of alkaloids. A third review is concerned with the ergolines as potential inhibitors of prolactin and of mammary tumours. 

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... 

Table 2 Pharmacological characterization of serotonin (5-HT) receptors by means of ergolines in functional and radioligand binding studies...

Nelson, D.L., Lucaites, V.L., Audia, J.E., Nissen, J.S. and Wainscott, D.B. (1993) Species differences in the pharmacology of the 5-hydroxytryptamine2 receptor structurally specific differentiation by ergolines and tryptamines./. Pharmacol. Exp. Then, 265, 1272-1279. 

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