Comparative studies of new thienothiazine derivatives on heart and smooth muscle preparations of guinea pigs.
New thienothiazine derivatives which differ in their side chain on the nitrogen atom of the thienothiazine molecule were studied in guinea pig papillary muscles and terminal ilea using isometric contraction force measurements. Compounds with a heterocyclic ring in their side chain like MS 57 (pyrrolidinylethylcarboxamide side chain), MS 58 (piperidinoethylcarboxamide side chain) and MS 55 (morpholinoethylcarboxamide side chain) had the most potent negative inotropic effect on isolated papillary muscles. The relaxing effect on smooth muscle was more pronounced with compounds carrying an aromatic ring in their side chain like MS 25 (dimethoxyphenylethyl-N-aminopropionyl side chain), MS 24 (dimethoxyphenylethyl-N-methylaminoacetyl side chain) and MS 27 (dimethoxyphenyl-N-methylethylaminoethylcarboxamide side chain). Our results show a tissue selectivity of the thienothiazine compounds.
Studenik
C
C
Institute of Pharmacology and Toxicology, University of Vienna, Austria.
Lemmens-Gruber
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R
Heistracher
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P
D000818:Animals; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects / Q000502:physiology; D006571:Heterocyclic Compounds / Q000494:pharmacology*; D007082:Ileum / Q000187:drug effects / Q000502:physiology; D009130:Muscle, Smooth / Q000187:drug effects* / Q000502:physiology; D010210:Papillary Muscles / Q000187:drug effects / Q000502:physiology; D010276:Parasympatholytics / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013843:Thiazines / Q000737:chemistry / Q000494:pharmacology*
D006571:Heterocyclic Compounds; D010276:Parasympatholytics; D013843:Thiazines