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Chemical Compound Review

SureCN10641501     N,N,2-trimethyl-1-(3- phenylquinolin-2...

Synonyms: Ici-170,809, AR-1E5084, Ici 170809, AC1L35JH, AC1Q7E24, ...
 
 
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Disease relevance of ZM 170809

  • 3. In a second study with lower doses of drugs, ICI 170,809 (0.3 mg kg-1) and ICI 192,605 (0.3 mg kg-1 min-1) had no significant effects on reperfusion-induced arrhythmias either alone or in combination [1].
  • 2. In a study on reperfusion-induced arrhythmias, the only significant effect of ICI 170,809 (1 mg kg-1, i.v.) was a reduction in the number of ventricular premature beats (VPBs) [1].
 

Psychiatry related information on ZM 170809

  • As previously shown, the acute effect of ICI-170,809 was to increase latency to rapid eye movement sleep (REMS), decrease the number of REM periods (REMPs), suppress the cumulative amount of REMS over 12 h, and increase the duration of REMPs in the first 6 h, while having no effect on non-REM sleep (NREMS) [2].
 

High impact information on ZM 170809

  • RESULTS: In plasma, platelet aggregation induced by 5-HT (3 microM) in the presence of adrenaline (1 microM) was inhibited by more than 85% by ICI 170809 (3 microM, IC50 0.1 microM), a specific platelet 5-HT2 antagonist [3].
  • 6. These results indicate that the previously observed antiarrhythmic activity of combined administration of the higher doses of ICI 170,809 and ICI 192,605 is unlikely to be due to direct effects on cardiac muscle but could be a consequence of reduced platelet aggregation [4].
  • 5. In rat isolated ventricular muscle preparations, ICI 170,809 increased the effective refractory period; e.g. from 39 +/- 4 to 86 +/- 18 ms, 10 min after adding 30 microM to left papillary muscles [4].
  • 1. The effects of the 5-HT2 antagonist, ICI 170,809 and the thromboxane A2 antagonist, ICI 192,605, given alone and in combination (n = 12 per group), were examined in anaesthetized rats [1].
  • In human temporal artery preparations ICI 169,369 was shown to cause a progressive rightward shift of the 5-HT-response curve over the range 10(-7)-10(-5)M, while ICI 170,809 in these concentrations shifted the curve to the same degree (no dose dependency) [5].
 

Anatomical context of ZM 170809

 

Associations of ZM 170809 with other chemical compounds

  • The effects of the novel, highly selective serotonin-2 (5-HT2) antagonists, ICI 169,369 and ICI 170,809, on 24 h EEG sleep-wake activity were studied in the rat [6].
 

Gene context of ZM 170809

  • 3. Pretreatment with the 5-HT2/5-HT1C antagonist ICI 170,809 (0.25-5 mg kg-1) also enhanced the behavioural syndrome induced by 8-OH-DPAT or 5-MeODMT [7].

References

  1. Suppression of reperfusion-induced arrhythmias with combined administration of 5-HT2 and thromboxane A2 antagonists. Shaw, L.A., Coker, S.J. Br. J. Pharmacol. (1996) [Pubmed]
  2. Effects of chronic treatment with two selective 5-HT2 antagonists on sleep in the rat. Pastel, R.H., Echevarria, E., Cox, B., Blackburn, T.P., Tortella, F.C. Pharmacol. Biochem. Behav. (1993) [Pubmed]
  3. Collagen induced human platelet aggregation: serotonin receptor antagonism retards aggregate growth in vitro. Menys, V.C. Cardiovasc. Res. (1993) [Pubmed]
  4. Combined administration of 5-HT2 and thromboxane A2 antagonists: effects on platelet aggregation and isolated cardiac muscle. Shaw, L.A., Batey, A.J., Coker, S.J. Br. J. Pharmacol. (1997) [Pubmed]
  5. 5-hydroxytryptamine antagonistic effects of ICI 169,369, ICI 170,809 and methysergide in human temporal and cerebral arteries. Jansen, I., Blackburn, T., Eriksen, K., Edvinsson, L. Pharmacol. Toxicol. (1991) [Pubmed]
  6. Suppressant effects of selective 5-HT2 antagonists on rapid eye movement sleep in rats. Tortella, F.C., Echevarria, E., Pastel, R.H., Cox, B., Blackburn, T.P. Brain Res. (1989) [Pubmed]
  7. Behavioural evidence for a functional interaction between central 5-HT2 and 5-HT1A receptors. Backus, L.I., Sharp, T., Grahame-Smith, D.G. Br. J. Pharmacol. (1990) [Pubmed]
 
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