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α‐FLUPENTHIXOL: AN ANTAGONIST OF DOPAMINE‐EVOKED FLUID SECRETION BY AN INSECT SALIVARY GLAND PREPARATION
Author(s) -
BREWARD J.,
HOUSE C.R.,
SMITH R.K.
Publication year - 1980
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1980.tb10891.x
Subject(s) - dopamine , antagonism , endocrinology , chemistry , medicine , antagonist , neurotransmitter , cockroach , competitive antagonist , pharmacology , dopamine receptor , receptor , biology , ecology
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 μ m ) 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.