Drugs online research references
Biochem Pharmacol. 1991 Jun 15;41(12):1963-6.
In vitro down-regulation predicts agonist efficacy at central muscarinic cholinergic receptors.
Stoll L, Muller WE.
Department of Psychopharmacology, Central Institute of Mental Health, Mannheim, Federal Republic of Germany.
Agonist induced short-term down-regulation of central muscarinic cholinergic receptors in mechanically dissociated cells of the mouse brain has been shown to predict the efficacy of agonists at muscarinic receptors. Pretreatment of cells with full agonists such as carbachol or oxotremorine M resulted in a loss of available muscarinic cholinergic receptors of about 30% using [3H]N-methylscopolamine [( 3H]NMS) as radioligand, whereas a second group of agonists e.g. RS 86 were only weakly active in this regard producing a significantly smaller loss of cell surface muscarinic cholinergic receptors. The magnitude of down-regulation of muscarinic receptors induced by pretreatment with several cholinergic drugs correlates fairly well with their ability to stimulate the phosphatidylinositol turnover. It seems that the agonist induced down-regulation of muscarinic cholinergic receptors on mechanically dissociated neurons of the mouse brain is a simple screening method to test for centrally acting cholinergic agonists.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2039547&dopt=Abstract
Psychopharmacology (Berl). 1981;73(4):388-90.
Modification of novelty preferences in rats by current and prior treatment with scopolamine and methylscopolamine.
Horsburgh RJ, Hughes RN.
Two experimental paradigms were adopted to compare effects of scopolamine and its quaternary derivative, methylscopolamine, on the behaviour of albino rats in an exploration box comprising novel and familiar halves. Subjects tested with the first paradigm were exposed to one of the halves, injected and then observed 20 min later. Although both drugs reduced preferences for the previously inaccessible novel half, only scopolamine decreased rearing and increased ambulation. With the second paradigm, behaviour was assessed without any current drug influence. On the 2 days prior to testing the rats had been exposed to one half of the apparatus while drugged. Prior treatment with both scopolamine and methylscopolamine reduced novelty preference to the extent that the familiar half of the apparatus was preferred. Both drugs also reduced rearing (for females only) and ambulation. It was concluded that the results with both paradigms provided some support for the view that reductions in novelty preference by anticholinergic drugs arise from their aversive peripheral actions.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6789363&dopt=Abstract
Alcohol Alcohol. 1990;25(1):3-7.
Reduction in ethanol preference following injection of centrally and peripherally acting antimuscarinic agents.
Rezvani AH, Overstreet DH, Janowsky DS.
Center for Alcohol Studies, University of North Carolina School of Medicine, Chapel Hill 27514.
Selectively bred alcohol-preferring (P) and alcohol non-preferring (NP) lines of rats were administered saline subcutaneously, and doses of 0.5 and 2.0 mg/kg of two antimuscarinic agents scopolamine (centrally acting) and methscopolamine (peripherally acting), twice daily respectively for a period of one day. Compared to saline, both doses of scopolamine and methscopolamine induced a significant reduction in ethanol consumption in the P line of rats, and both antimuscarinic agents significantly increased water intake. Thus, ethanol preference was dramatically reduced in these rats. In contrast, scopolamine had relatively little effect on either ethanol or water intake in the NP line of rats, while methscopolamine tended to suppress both ethanol and water intake. These findings suggest that peripheral muscarinic mechanisms may be involved in ethanol preference in P rats.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2334493&dopt=Abstract
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