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First published online June 15, 2006
Journal of Experimental Biology 209, 2525-2534 (2006)
Published by The Company of Biologists 2006
doi: 10.1242/jeb.02274
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Pharmacological characterization of the ergot alkaloid receptor in the salivary gland of the ixodid tick Amblyomma hebraeum
Department of Biological Sciences, University of Alberta, Edmonton, Alberta, T6G 2E9, Canada
* Author for correspondence (e-mail: reuben.kaufman{at}ualberta.ca)
Accepted 18 April 2006
Female ticks of the family Ixodidae osmoregulate by secreting the excess
fluid of the blood meal back into the host's circulation via the
salivary glands. At least three receptors control salivary fluid secretion in
the tick Amblyomma hebraeum: (1) dopamine (DA) stimulates fluid
secretion via a DA receptor, (2) ergot alkaloids (ErAs) stimulate
fluid secretion via an ErA-sensitive receptor (the natural ligand of
which has not been identified), and (3) a GABA receptor potentiates the action
of DA and ErAs. Here we present some pharmacological properties of the
ErA-sensitive receptor. Of the 11 ErAs we tested, (i) four were complete
agonists (approximate concentration eliciting 50% maximum response is given in
parentheses): dihydroergotamine (0.02 µmol l1),
ergonovine (ErN; 0.06 µmol l1), methylergonovine (0.1
µmol l1) and
-ergocriptine (0.9 µmol
l1); (ii) three were `incomplete agonists' (approximate
concentration eliciting 20% maximum response is given in parentheses):
ergocorninine (3.5 µmol l1), ergocristinine (7.5 µmol
l1) and ergocristine (10 µmol l1); (C)
three were partial agonists (approximate concentration eliciting the
respective maximum response in parentheses): ergocornine (50% maximum by 1
µmol l1), methysergide (28% maximum by 10 µmol
l1) and bromocriptine (22% maximum by 10 µmol
l1); and (D) one had no activity up to 1 mmol
l1: ergothioneine. Bromocriptine and methysergide did not
antagonize the action of DA, but were effective competitive antagonists of
ErN, with Kis of
0.3 µmol l1 and
11 µmol l1, respectively. Ergothioneine was not an
antagonist at either the DA- or ErA-sensitive receptor. The putative protein
kinase C activators, 1-oleoyl-2-acetyl-sn-glycerol (OAG) and
1,2-dioctanoyl-sn-glycerol (DiC8), neither stimulated
salivary fluid secretion nor potentiated the action of DA or ErN. The putative
protein kinase C inhibitors, bisindolymaleimide (BIM) and calphostin C did not
inhibit the action of DA or ErN, although low concentrations of calphostin C
(10 nmol l1) appeared to potentiate the action of DA but not
ErN. The ion transport inhibitors, furosemide and amiloride (both up to 1 mmol
l1), had no significant effect on DA-stimulated or
ErN-stimulated fluid secretion.
Key words: Amblyomma hebraeum, bromocriptine, dihydroergotamine, ergocornine, ergocorninine, ergocristine, ergocristinine, ergocryptine, ergonovine, ergothioneine, ergot alkaloids, methylergonovine, methysergide, tick salivary gland
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