| Autor: | Manoj C. Desai, E. Edward Mena |
|---|---|
| Rok vydání: | 1991 |
| Předmět: |
Pharmacology
biology Chemistry medicine.drug_class Organic Chemistry Pharmaceutical Science Acetylcholinesterase chemistry.chemical_compound Membrane Biochemistry Acetylcholinesterase inhibitor Enzyme inhibitor medicine biology.protein Molecular Medicine Pharmacology (medical) Binding site Receptor IC50 Acetylcholine Biotechnology medicine.drug |
| Zdroj: | Pharmaceutical Research. :200-203 |
| ISSN: | 0724-8741 |
| DOI: | 10.1023/a:1015840003630 |
| Popis: | Tetrahydroaminoacridine (THA), an acetylcholinesterase inhibitor that is reported to have significant effects on cognition and memory in Alzheimer’s disease patients, binds to rat brain membranes in a saturable and reversible manner. Computer analysis of the binding data revealed high- and low-affinity sites with Kd values of 97.8 nM and 4.65 µM and Bmax values of 4.13 and 114 pmol/mg protein. Autoradiographic studies show that these binding sites are not co-localized with acetylcholinesterase activity. The binding of [3H]THA to membranes does not appear to be related to receptors for several neurotransmitters/neuromodulators, including acetylcholine and other acetylcholinesterase inhibitors. Amiridin, a closely related acetylcholinesterase inhibitor, was able to block specific [3H]THA binding (IC50 = 1.05 µM). While the function of THA mediated by these sites is unknown, they may be responsible in part for the distinct clinical effects of tetrahydroaminoacridine compared to other acetylcholinesterase inhibitors. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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