Effects of the nootropic agents adafenoxate, meclofenoxate and the acetylcholine precursor citicholine on the brain muscarinic receptors (experiments on rats). 1987

V D Petkov, and J S Popova
Institute of Physiology, Bulgarian Academy of Sciences, Sofia.

The effect of adafenoxate (Af), meclofenoxate (Mf) and citicholine on the brain muscarinic receptors was studied in groups of ten male Wistar rats. The compounds were administered in doses of 50 mg/kg body weight twice daily for 7 days. One hour after the last treatment the animals were killed and the frontal cerebral cortex striatum, the hypothalamus and the hippocampus were removed immediately. Af and Mf were found to diminish significantly and to an analogous extent the density (Bmax) of the muscarinic receptors in the cerebral cortex, striatum and the hippocampus. At the same time, however, the greater decrease of Kd induced by these two nootropic agents, i.e. the increased affinity of the muscarinic binding sites, exceeded considerably the decreased number of the binding sites. These differences in the effects on Bmax and Kd suggest that the functional capacity of the cerebral cholinergic system increases under the action of Mf and Af. The surprising increase in the number of muscarinic receptors in the striatum, observed in citicholine-treated animals, is assumed to be due to the great increase of the dopamine content in this structure, induced by this acetylcholine precursor, observed in other experiments. This increase would result in reduced acetylcholine production by the inhibited cholinergic neurones, with a subsequent increase in the number of the muscarinic receptors.

UI MeSH Term Description Entries
D008297 Male Males
D011869 Radioligand Assay Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders). Protein-Binding Radioassay,Radioreceptor Assay,Assay, Radioligand,Assay, Radioreceptor,Assays, Radioligand,Assays, Radioreceptor,Protein Binding Radioassay,Protein-Binding Radioassays,Radioassay, Protein-Binding,Radioassays, Protein-Binding,Radioligand Assays,Radioreceptor Assays
D011919 Rats, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding. August Rats,Inbred Rat Strains,Inbred Strain of Rat,Inbred Strain of Rats,Inbred Strains of Rats,Rat, Inbred Strain,August Rat,Inbred Rat Strain,Inbred Strain Rat,Inbred Strain Rats,Inbred Strains Rat,Inbred Strains Rats,Rat Inbred Strain,Rat Inbred Strains,Rat Strain, Inbred,Rat Strains, Inbred,Rat, August,Rat, Inbred Strains,Rats Inbred Strain,Rats Inbred Strains,Rats, August,Rats, Inbred Strain,Strain Rat, Inbred,Strain Rats, Inbred,Strain, Inbred Rat,Strains, Inbred Rat
D011976 Receptors, Muscarinic One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology. Muscarinic Acetylcholine Receptors,Muscarinic Receptors,Muscarinic Acetylcholine Receptor,Muscarinic Receptor,Acetylcholine Receptor, Muscarinic,Acetylcholine Receptors, Muscarinic,Receptor, Muscarinic,Receptor, Muscarinic Acetylcholine,Receptors, Muscarinic Acetylcholine
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D002504 Meclofenoxate An ester of DIMETHYLAMINOETHANOL and para-chlorophenoxyacetic acid. Centrophenoxine,Atsefen,Cerutil,Cetrexin,Helfergin,Meclofenoxate Hydrochloride
D002794 Choline A basic constituent of lecithin that is found in many plants and animal organs. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism. Bursine,Fagine,Vidine,2-Hydroxy-N,N,N-trimethylethanaminium,Choline Bitartrate,Choline Chloride,Choline Citrate,Choline Hydroxide,Choline O-Sulfate,Bitartrate, Choline,Chloride, Choline,Choline O Sulfate,Citrate, Choline,Hydroxide, Choline,O-Sulfate, Choline
D003566 Cytidine Diphosphate Choline Donor of choline in biosynthesis of choline-containing phosphoglycerides. CDP Choline,Citicoline,Cidifos,Citicholine,Cyticholine,Cytidine 5'-Diphosphocholine,5'-Diphosphocholine, Cytidine,Choline, CDP,Choline, Cytidine Diphosphate,Cytidine 5' Diphosphocholine,Diphosphate Choline, Cytidine
D006016 Glycolates Derivatives of ACETIC ACID which contain an hydroxy group attached to the methyl carbon. 2-Hydroxyacetates,Glycolate Ethers,Hydroxyacetate Ethers,Hydroxyacetates,Hydroxyacetic Acids,2 Hydroxyacetates,Acids, Hydroxyacetic,Ethers, Glycolate,Ethers, Hydroxyacetate
D000109 Acetylcholine A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system. 2-(Acetyloxy)-N,N,N-trimethylethanaminium,Acetilcolina Cusi,Acetylcholine Bromide,Acetylcholine Chloride,Acetylcholine Fluoride,Acetylcholine Hydroxide,Acetylcholine Iodide,Acetylcholine L-Tartrate,Acetylcholine Perchlorate,Acetylcholine Picrate,Acetylcholine Picrate (1:1),Acetylcholine Sulfate (1:1),Bromoacetylcholine,Chloroacetylcholine,Miochol,Acetylcholine L Tartrate,Bromide, Acetylcholine,Cusi, Acetilcolina,Fluoride, Acetylcholine,Hydroxide, Acetylcholine,Iodide, Acetylcholine,L-Tartrate, Acetylcholine,Perchlorate, Acetylcholine

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