Dihydroisohistrionicotoxin inhibits acetylcholine receptor-dependent 22Na+ uptake of cultured chick muscle cells with a KI of 0.2 micrometer. The inhibition is noncompetitive with respect to agonists. The toxin enhances desensitization of the receptor by agonists which is accompanied by a ...

Ligand binding studies with nicotinic acetylcholine receptor on the fiber optic biosensor indicate K (sub i) values for antagonists were similar to those obtained in membrane binding assays. The agonists appear much less potent. This may be due to the ina...

The regulation of muscarinic acetylcholine receptors by short-term exposure to agonists was investigated in intact mouse neuroblastoma (clone N1E-115) cells, using the hydrophilic ligand (tritium)N-methylscopolamine. It was found that preincubation of cel...

... for Aedes taeniorhynchus females after 24-h exposure. Neonicotinoid insecticides are agonists of the nicotinic acetylcholine receptor and ... and J.-M. Hougard. 2004. Dinotefuran: A potential neonicotino...

-mutant animals to the paralytic effects of aldicarb, an acetyl- cholinesterase inhibitor, and levamisole, an acetylcholine receptor agonist. Resistance to these agents, particularly to levamisole, is a telltale sign

... principal piece of human and mouse sperm [49]. Physostigmine, an AChE inhibitor (and thus an indirect agonist ... ...

... The role of classical neurotransmitters including acetylcholine and norepinephrine in regulating myometrial contractility has been well studied; ... Although the classical neurotransmitters such as acetyl...

... W. and Berman, JD (1989) Mechanism of agonist-induced down-regulation and subsequent recovery of muscarinic acetylcholin receptors in a ...

1 The potentiating effect of a low concentration of various vascular contractile agonists on the response of rabbit aortic strips to acetylcholine was examined. 2 A marked parallel displacement to the left (potentiation; not additive effect) of the dose-response curve for acetylcholine was observed when 5-hydroxytryptamine (5-HT), ...

Pretreatment of {alpha}-bungarotoxin ({alpha}-Bgt) binding sites from rat brain with cholinergic agonists causes transformation of sites to a high-affinity form toward agonist over a time course of minutes, consistent with identity of those sites as central nicotinic acetylcholine receptors (nAChR). This ...

Nicotinic acetylcholine receptors are pentameric ligand-gated ion channels, which are involved in a wide range of neuronal functions. During the past decade, a large number of nicotinic acetylcholine receptor subunits have been cloned and showed a discreet yet overlapping distribution pattern. Recently, several ...

... Title : Turnover of Acetylcholine Receptors: Mechanisms of Regulation. ... Acetylcholine receptors, RA5 Neuromuscular junctions, Motor nerves. ...

Acetylcholine release stimulated by nicotinic agonists was measured as radioactivity released from perfused synaptosomes prepared from mouse interpeduncular nucleus (IPN) that had been loaded with [ 3 H]choline. Agonist-stimulated release was dependent upon external calcium and over 90% of released radioactivity was ...

Partial contents include: Light-activated channels in limulus ventral photoreceptors; Paramagnetic hydrophobic ions as probes for electrically active conformational transitions in Ion channels; Acetylcholine receptor. Dynamic properties; Acetylcholine-activated channel current-voltage relations in symmetrical Na(+) solutions; A ...

Intact rat brain cells were dissociated and used to study the regulation of muscarinic acetylcholine receptors upon exposure to muscarinic receptor agonists. Incubation of cells with carbamylcholine resulted in a time-dependent decrease in subsequent (/sup 3/H)N-methylscopolamine specific binding, an effect which ...