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PMID: 6768074 Published · ppublish English Journal Article

Further evidence that 3H-cis(Z)flupenthixol binds to the adenylate cyclase-associated dopamine receptor (D-1) in rat corpus striatum.

Psychopharmacology ·Vol. 67 ·No. 1 ·1980-01-00 ·Pages 107-9

Hyttel J

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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Article Info
Journal
Psychopharmacology
Abbr.
Psychopharmacology (Berl)
ISSN
0033-3158
Published
1980-01-00
Pages
107-9
Language
English
Region
Germany
NLM ID
7608025
Subset
IM
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