Results 131 to 140 of about 10,564,162 (159)
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Journal of Molecular Neuroscience, 2006
It has been shown previously that the third extracellular loop (o3) and its vicinity play a critical role in allosteric modulation at muscarinic acetylcholine receptors (mAChRs) (Ellis et al., 1993; Krejçí and Tuçek, 2001; Buller et al., 2002). In this study interaction of four chemically related substances (strychnine, its dimethoxy derivate brucine ...
Jan, Jakubík, Vladimír, Dolezal
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It has been shown previously that the third extracellular loop (o3) and its vicinity play a critical role in allosteric modulation at muscarinic acetylcholine receptors (mAChRs) (Ellis et al., 1993; Krejçí and Tuçek, 2001; Buller et al., 2002). In this study interaction of four chemically related substances (strychnine, its dimethoxy derivate brucine ...
Jan, Jakubík, Vladimír, Dolezal
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Life Sciences, 1992
Piracetam, a nootropic drug, has been used for some time in Alzheimer's disease for its facilitatory effect on learning and memory. Rats treated with piracetam (500 mg/kg, p.o.) daily, during 1 and 2 weeks, showed a significant increase in muscarinic receptor number (Bmax) and in the dissociation constant values (Kd) in the cerebral motor cortex, in ...
G S, Viana, M M, Marinho, F C, Sousa
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Piracetam, a nootropic drug, has been used for some time in Alzheimer's disease for its facilitatory effect on learning and memory. Rats treated with piracetam (500 mg/kg, p.o.) daily, during 1 and 2 weeks, showed a significant increase in muscarinic receptor number (Bmax) and in the dissociation constant values (Kd) in the cerebral motor cortex, in ...
G S, Viana, M M, Marinho, F C, Sousa
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[3H]N-methylscopolamine binding to muscarinic receptors in intact adult rat brain cell aggregates
Biochemical Pharmacology, 1985Intact brain cell aggregates were dissociated from adult rat brains, by a simple sieving technique, and were used to study the binding characteristics of [3H]N-methylscopolamine to muscarinic acetylcholine receptors. The magnitude of binding of this ligand was related linearly to the amount of cell protein in the binding assay, with a high ratio of ...
J H, Lee, E E, el-Fakahany
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European Journal of Pharmacology, 1986
The effect of the irreversible acetylcholinesterase inhibitor diisopropylfluorophosphate (DFP) on mouse brain muscarinic acetylcholine receptors was assessed using the muscarinic antagonists [3H]N-methylscopolamine [( 3H]NMS) and [3H]quinuclidinyl benzilate [( 3H]QNB).
C L, Cioffi, E E, el-Fakahany
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The effect of the irreversible acetylcholinesterase inhibitor diisopropylfluorophosphate (DFP) on mouse brain muscarinic acetylcholine receptors was assessed using the muscarinic antagonists [3H]N-methylscopolamine [( 3H]NMS) and [3H]quinuclidinyl benzilate [( 3H]QNB).
C L, Cioffi, E E, el-Fakahany
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Comparative Biochemistry and Physiology Part C: Comparative Pharmacology, 1992
1. Binding characteristics of membrane preparations from four brain regions and heart (HT) right artria from mallard ducks were documented using the muscarinic ligand [3H]N-methylscopolamine([3H]NMS). 2. Brain regions used were: cerebellum (CL), medulla/pons (MP), corpus striatum (CS), and hippocampus (HI).
B.Thomas Marden +2 more
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1. Binding characteristics of membrane preparations from four brain regions and heart (HT) right artria from mallard ducks were documented using the muscarinic ligand [3H]N-methylscopolamine([3H]NMS). 2. Brain regions used were: cerebellum (CL), medulla/pons (MP), corpus striatum (CS), and hippocampus (HI).
B.Thomas Marden +2 more
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Pharmacology & Toxicology, 1988
Abstract:W84 (hexamethylene‐bis‐[dimethyl‐(3‐phthalimidopropyl)‐ammonium bromide]) protects overadditively against an organophosphate‐intoxication when applied in combination with atropine. Further experimental evidence led to the hypothesis that W84 exerted an allosteric effect on muscarinic acetylcholine receptors.
K, Jepsen +3 more
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Abstract:W84 (hexamethylene‐bis‐[dimethyl‐(3‐phthalimidopropyl)‐ammonium bromide]) protects overadditively against an organophosphate‐intoxication when applied in combination with atropine. Further experimental evidence led to the hypothesis that W84 exerted an allosteric effect on muscarinic acetylcholine receptors.
K, Jepsen +3 more
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Molecular Pharmacology, 2008
Muscarinic MT7 toxin is a highly selective and potent antagonist of the M(1) subtype of muscarinic receptor and acts by binding to an allosteric site. To identify the molecular determinants by which MT7 toxin interacts with this receptor in its free and NMS-occupied states, the effect on toxin potency of alanine substitution was evaluated in ...
Fruchart-Gaillard, Carole +5 more
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Muscarinic MT7 toxin is a highly selective and potent antagonist of the M(1) subtype of muscarinic receptor and acts by binding to an allosteric site. To identify the molecular determinants by which MT7 toxin interacts with this receptor in its free and NMS-occupied states, the effect on toxin potency of alanine substitution was evaluated in ...
Fruchart-Gaillard, Carole +5 more
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Journal of Receptor Research, 1986
Gallamine inhibited the binding of both (3H)N-Methylscopolamine ((3H)NMS) and (3H)Pirenzepine ((3H)PZ) in the hippocampus, striatum and cortex of rat brain. Competition curves between gallamine and (3H)PZ suggested that gallamine recognized an homogeneous class of receptors (Hill coefficient close to 1) whereas competition curves, using (3H)NMS as ...
Gillard, Michel +2 more
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Gallamine inhibited the binding of both (3H)N-Methylscopolamine ((3H)NMS) and (3H)Pirenzepine ((3H)PZ) in the hippocampus, striatum and cortex of rat brain. Competition curves between gallamine and (3H)PZ suggested that gallamine recognized an homogeneous class of receptors (Hill coefficient close to 1) whereas competition curves, using (3H)NMS as ...
Gillard, Michel +2 more
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Life Sciences, 1999
We previously demonstrated that brucine and some analogues allosterically enhance the affinity of ACh at muscarinic receptor subtypes M1, M3 or M4. Here we describe allosteric effects at human M1-M4 receptors of four stereoisomers of a pentacyclic structure containing features of the ring structure of brucine.
S, Lazareno +8 more
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We previously demonstrated that brucine and some analogues allosterically enhance the affinity of ACh at muscarinic receptor subtypes M1, M3 or M4. Here we describe allosteric effects at human M1-M4 receptors of four stereoisomers of a pentacyclic structure containing features of the ring structure of brucine.
S, Lazareno +8 more
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Characterization of 3H-N-methylscopolamine binding to intact rat thymocytes.
Endocrinologia experimentalis, 1990The binding parameters of muscarinic antagonists in intact rat thymocytes were determined from competitive binding experiments with 3H-N-methylscopolamine (3H-NMS). The muscarinic antagonists inhibited binding of 3H-NMS in a dose-dependent manner. Non-linear regression analysis of the displacement curves indicated the presence of two affinity states ...
I, Rinner, S, Porta, K, Schauenstein
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