Abstract:
:(5R,6R)-6-(3-Propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[ 3.2.1]octane (PTAC) is a selective muscarinic receptor ligand. The compound exhibits high affinity for central muscarinic receptors with partial agonist mode of action at muscarinic M(2) and M(4) and antagonist mode of action at muscarinic M(1), M(3) and M(5) receptor subtypes. The compound was earlier reported to exhibit functional dopamine receptor antagonism in rodents despite its lack of affinity for dopamine receptors. In the present study, we report that PTAC, as well as the muscarinic receptor agonists pilocarpine and oxotremorine, dose-dependently decreased rates of intravenous self-administration (fixed ratio 1) of the indirect dopamine receptor agonist cocaine in drug naive mice. Similar decreases in cocaine self-administration rates were obtained with the dopamine receptor antagonists olanzapine, clozapine, risperidone, fluphenazine and haloperidol. These findings suggest that compounds with partial muscarinic receptor agonist mode of action may be used in the medical treatment of cocaine abuse.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Rasmussen T,Sauerberg P,Nielsen EB,Swedberg MD,Thomsen C,Sheardown MJ,Jeppesen L,Calligaro DO,DeLapp NW,Whitesitt C,Ward JS,Shannon HE,Bymaster FP,Fink-Jensen Adoi
10.1016/s0014-2999(00)00442-8keywords:
subject
Has Abstractpub_date
2000-08-25 00:00:00pages
241-6issue
3eissn
0014-2999issn
1879-0712pii
S0014299900004428journal_volume
402pub_type
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