Abstract
The proposal that 3H-cis(Z)flupenthixol (3H-FPT) preferentially binds to striatal dopamine receptors associated with adenylate cyclase activity (D-1), distinct from dopamine receptors to which 3H-haloperidol (3H-hal) binds (D-2), has been investigated further. The dopamine agonists bromocriptine and ergotamine were 60-times more potent as displacers of 3H-hal than 3H-FPT binding. Other dopamine agonists (ergometrine, dopamine, apomorphine, 2-amino-6,7-dihydroxy-tetralin (ADTN), and ergocornine) also shared this profile, although a smaller ratio was found for these compounds. Substituted benzamides (clebopride greater than sultopride greater than sulpiride greater than metoclorpramide greater than tiapride) displace 3H-hal but have only a very slight displacing effect towards 3H-FPT, and did not inhibit dopamine-stimulated adenylate cyclase activity. The same pattern is shared by oxiperomide and molindone. Together, these results support the idea that 3H-FPT labels another class of dopamine receptors than does 3H-hal, and that the former class most likely is associated with adenylate cyclase.
MeSH Terms
Adenylyl Cyclases/metabolism
Animals
Corpus Striatum/metabolism
Flupenthixol/metabolism
In Vitro Techniques
Rats
Receptors, Dopamine/drug effects,metabolism
Thioxanthenes/metabolism
Chemicals
Receptors, Dopamine
Thioxanthenes
Adenylyl Cyclases
Flupenthixol
Authors & Affiliations
1 authors, click to expand affiliations / ORCID
Hyttel J
References (10)
10 references, click to expand
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