α‐FLUPENTHIXOL: AN ANTAGONIST OF DOPAMINE‐EVOKED FLUID SECRETION BY AN INSECT SALIVARY GLAND PREPARATION

1 We have demonstrated inhibition of secretory responses of cockroach salivary glands to dopamine, adrenaline, noradrenaline and neurotransmitter by α‐flupenthixol. This inhibition was slow in onset (60 min) and in reversal (> 2 h). 2 Inhibition of responses to adrenaline and noradrenaline was no...

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Veröffentlicht in:British journal of pharmacology 1980-05, Vol.69 (1), p.123-129
Hauptverfasser: BREWARD, J., HOUSE, C.R., SMITH, R.K.
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Sprache:eng
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Zusammenfassung:1 We have demonstrated inhibition of secretory responses of cockroach salivary glands to dopamine, adrenaline, noradrenaline and neurotransmitter by α‐flupenthixol. This inhibition was slow in onset (60 min) and in reversal (> 2 h). 2 Inhibition of responses to adrenaline and noradrenaline was non‐competitive, since the maxima and slopes of dose‐response curves of these agonists were reduced. 3 Although at low concentrations (< 3 μm) the antagonism of responses to dopamine showed some characteristics of competitive inhibition, at higher doses non‐competitive inhibition was clearly demonstrated. 4 These results are explained in terms of different efficacies of the agonists for the receptors antagonized by α‐flupenthixol. 5 β‐Flupenthixol was shown to antagonize responses to dopamine; however it was 10 to 100 times less potent than α‐flupenthixol.
ISSN:0007-1188
1476-5381
DOI:10.1111/j.1476-5381.1980.tb10891.x