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Chloro- and methyl-substituted 10H-pyrazino[2,3-b][1,4]benzothiazines were prepared and their structures determined by 13C NMR and X-ray crystallographic analysis. Alkylation afforded the 10-[3-(dimethylamino)-1-propyl] derivatives, which were compared to chlorpromazine in receptor-binding assays, in vivo behavioral tests, and electrochemical oxidation studies. In this series, the 2-chloro compound, 4c, proved to be the most effective derivative in displacing [3H]siperone, [3H]apomorphine, and [3H]prazosin radioligands from binding sites, being approximately as potent as chlorpromazine in this respect. However, none of the 10H-pyrazino[2,3-b][1,4]benzothiazines of this study were as active as chlorpromazine in in vivo tests predictive of neuroleptic activity.
W S Saari, and
D W Cochran, and
Y C Lee, and
E L Cresson, and
J P Springer, and
M Williams, and
J A Totaro, and
G G Yarbrough
August 1980,
Journal of medicinal chemistry,
W S Saari, and
D W Cochran, and
Y C Lee, and
E L Cresson, and
J P Springer, and
M Williams, and
J A Totaro, and
G G Yarbrough
June 2004,
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W S Saari, and
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J P Springer, and
M Williams, and
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G G Yarbrough
March 1977,
Il Farmaco; edizione scientifica,
W S Saari, and
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M Williams, and
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G G Yarbrough
March 2009,
Acta crystallographica. Section E, Structure reports online,
W S Saari, and
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E L Cresson, and
J P Springer, and
M Williams, and
J A Totaro, and
G G Yarbrough
July 2002,
Chemical & pharmaceutical bulletin,
W S Saari, and
D W Cochran, and
Y C Lee, and
E L Cresson, and
J P Springer, and
M Williams, and
J A Totaro, and
G G Yarbrough
April 1953,
Annales medico-psychologiques,
W S Saari, and
D W Cochran, and
Y C Lee, and
E L Cresson, and
J P Springer, and
M Williams, and
J A Totaro, and
G G Yarbrough
April 1963,
Medicina,
W S Saari, and
D W Cochran, and
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E L Cresson, and
J P Springer, and
M Williams, and
J A Totaro, and
G G Yarbrough
September 2009,
Acta crystallographica. Section E, Structure reports online,
W S Saari, and
D W Cochran, and
Y C Lee, and
E L Cresson, and
J P Springer, and
M Williams, and
J A Totaro, and
G G Yarbrough
January 1974,
Indian journal of physiology and pharmacology,
W S Saari, and
D W Cochran, and
Y C Lee, and
E L Cresson, and
J P Springer, and
M Williams, and
J A Totaro, and
G G Yarbrough
May 1976,
Il Farmaco; edizione scientifica,
