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Abstract

Partial dopamine-agonistic and atypical neuroleptic properties of the amino-ergolines SDZ 208-911 and SDZ 208-912.

D M Coward, A K Dixon, S Urwyler, T G White, A Enz, M Karobath and G Shearman
Journal of Pharmacology and Experimental Therapeutics January 1990, 252 (1) 279-285;
D M Coward
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A K Dixon
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S Urwyler
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T G White
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A Enz
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M Karobath
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G Shearman
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Abstract

The aminoergolines SDZ 208-911 [N-[(8-alpha)-2,6-dimethylergoline-8-yl]-2,2- dimethylpropanamide] and SDZ 208-912 [N-[8-alpha)-2-chloro-6-methylergoline-8-yl]- 2,2-dimethylpropanamide] exhibit nonclassical, neuroleptic-like properties in rodents. Thus, they are equipotent to haloperidol as inhibitors of apomorphine-induced gnawing behavior and conditioned avoidance responding, but are essentially devoid of cataleptogenic activity. In addition, they show high affinity for central D-2 receptors in vitro and elevate striatal homovanillic acid levels. In contrast to haloperidol, however, SDZ 208-911 and 208-912 strongly inhibit prolactin secretion and induce contralateral circling behavior in 6-hydroxydopamine-lesioned animals. These profiles are consistent with the drugs exhibiting varying degrees of partial agonistic activity at dopamine D-2 receptors, with SDZ 208-911 being considerably more agonistic than SDZ 208-912. Support for this contention stems from the ability of SDZ 208-911 to reduce the elevation of striatal L-dopa formation induced by gamma-butyrolactone, and SDZ 208-912's partial reversal of apomorphine's inhibitory action on gamma-butyrolactone activity. SDZ 208-911's effects are reduced after the partial alkylation of D-2 receptors with N-ethoxy-carbonyl-2-ethoxy-1,2-dihydroquinoline, confirming its partial agonistic properties. SDZ 208-911 and SDZ 208-912 could be effective against both the positive and negative symptoms of schizophrenia, while exhibiting a reduced incidence of dystonic and parkinsonian side-effects. In addition, their clinical testing might throw more light on the central dopaminergic status of schizophrenic subjects.

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Journal of Pharmacology and Experimental Therapeutics
Vol. 252, Issue 1
1 Jan 1990
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Abstract

Partial dopamine-agonistic and atypical neuroleptic properties of the amino-ergolines SDZ 208-911 and SDZ 208-912.

D M Coward, A K Dixon, S Urwyler, T G White, A Enz, M Karobath and G Shearman
Journal of Pharmacology and Experimental Therapeutics January 1, 1990, 252 (1) 279-285;

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Abstract

Partial dopamine-agonistic and atypical neuroleptic properties of the amino-ergolines SDZ 208-911 and SDZ 208-912.

D M Coward, A K Dixon, S Urwyler, T G White, A Enz, M Karobath and G Shearman
Journal of Pharmacology and Experimental Therapeutics January 1, 1990, 252 (1) 279-285;
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