Acetylseco hemicholinium-3, a new choline acetyltransferase inhibitor useful in neuropharmacological studies
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منابع مشابه
Acetylseco hemicholinium-3, a new choline acetyltransferase inhibitor useful in neuropharmacological studies.
Described are the synthesis and some aspects of the pharmacology of acetylseco hemicholinium-3 (acetylseco HC-3), the acetylated open ring analogue of hemicholinium-3 (HC-3). The effects of both compounds were determined in uiuo on rat brain acetylcholine (ACh), ‘Y-choline (14C-Ch) incorporation into 14C-acetylcholine (14C-ACh) and on one way jump box avoidance and escape behavior in naive and ...
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Human choline kinase (ChoK) catalyzes the first reaction in phosphatidylcholine biosynthesis and exists as ChoKalpha (alpha1 and alpha2) and ChoKbeta isoforms. Recent studies suggest that ChoK is implicated in tumorigenesis and emerging as an attractive target for anticancer chemotherapy. To extend our understanding of the molecular mechanism of ChoK inhibition, we have determined the high reso...
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The effect of hemicholinium (HC-3) on choline distribution was studied in aivo in the subcellular fractions of the canine caudate nucleus. Both HC-3 and choline were given intraventricularly to locally anesthetized, decamethonium-paralyzed dogs maintained on artificial ventilation. At various time intervals after intraventricular injection of methyl-W-choline alone and in various HC-3/methyl-W-...
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High, subcutaneous doses of the organophosphorus insecticide chlorpyrifos (CPF) in adult male rats can be well-tolerated despite extensive and persistent acetylcholinesterase (AChE) inhibition. We propose that changes in acetylcholine synthesis could modulate the toxicity associated with extensive AChE inhibition following CPF exposure. High-affinity choline uptake (HACU, the rate-limiting step...
متن کاملMolecular cloning and characterization of a murine hemicholinium-3-sensitive choline transporter.
In cholinergic neurons, a specific requirement for precursor choline in the biosynthesis of acetylcholine (ACh) is thought to be sustained by a presynaptic, hemicholinium-3 (HC-3)-sensitive choline transporter (CHT). This transporter exhibits micromolar affinity for choline and transport activity is Na(+)- and Cl(-)-dependent. Based on the sequence information available with the recent cloning ...
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ژورنال
عنوان ژورنال: Neuropharmacology
سال: 1973
ISSN: 0028-3908
DOI: 10.1016/0028-3908(73)90005-1