Reversal of cognitive impairment by heptyl physostigmine, a long-lasting cholinesterase inhibitor, in primates.
Cholinergic replacement therapy for Alzheimer's disease using existing cholinesterase inhibitors is compromised by short duration, meagre benefits restricted to subgroups of patients, and peripheral toxicity. Heptyl physostigmine is a lipophilic carbamate derivative of physostigmine. In rhesus...
| Main Authors: | , , , , , |
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| Format: | Journal article |
| Language: | English |
| Published: |
1992
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| _version_ | 1797055615335399424 |
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| author | Rupniak, N Tye, S Brazell, C Heald, A Iversen, S Pagella, P |
| author_facet | Rupniak, N Tye, S Brazell, C Heald, A Iversen, S Pagella, P |
| author_sort | Rupniak, N |
| collection | OXFORD |
| description | Cholinergic replacement therapy for Alzheimer's disease using existing cholinesterase inhibitors is compromised by short duration, meagre benefits restricted to subgroups of patients, and peripheral toxicity. Heptyl physostigmine is a lipophilic carbamate derivative of physostigmine. In rhesus monkeys, heptyl physostigmine (0.2-0.9 mg/kg i.m.) fully reversed a scopolamine-induced cognitive impairment. Following oral administration in squirrel monkeys, heptyl physostigmine (8 mg/kg) induced long-lasting hypothermia (greater than or equal to 4 h), a centrally-mediated cholinergic effect. Erythrocyte acetylcholinesterase activity was inhibited by 86% at the time of peak hypothermia (180 min). Clinical trials with heptyl physostigmine will enable a more rigorous evaluation of cholinomimetic therapy for dementia. |
| first_indexed | 2024-03-06T19:12:24Z |
| format | Journal article |
| id | oxford-uuid:1733eaa0-4373-4d39-a814-cd5de6b76774 |
| institution | University of Oxford |
| language | English |
| last_indexed | 2024-03-06T19:12:24Z |
| publishDate | 1992 |
| record_format | dspace |
| spelling | oxford-uuid:1733eaa0-4373-4d39-a814-cd5de6b767742022-03-26T10:35:50ZReversal of cognitive impairment by heptyl physostigmine, a long-lasting cholinesterase inhibitor, in primates.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:1733eaa0-4373-4d39-a814-cd5de6b76774EnglishSymplectic Elements at Oxford1992Rupniak, NTye, SBrazell, CHeald, AIversen, SPagella, PCholinergic replacement therapy for Alzheimer's disease using existing cholinesterase inhibitors is compromised by short duration, meagre benefits restricted to subgroups of patients, and peripheral toxicity. Heptyl physostigmine is a lipophilic carbamate derivative of physostigmine. In rhesus monkeys, heptyl physostigmine (0.2-0.9 mg/kg i.m.) fully reversed a scopolamine-induced cognitive impairment. Following oral administration in squirrel monkeys, heptyl physostigmine (8 mg/kg) induced long-lasting hypothermia (greater than or equal to 4 h), a centrally-mediated cholinergic effect. Erythrocyte acetylcholinesterase activity was inhibited by 86% at the time of peak hypothermia (180 min). Clinical trials with heptyl physostigmine will enable a more rigorous evaluation of cholinomimetic therapy for dementia. |
| spellingShingle | Rupniak, N Tye, S Brazell, C Heald, A Iversen, S Pagella, P Reversal of cognitive impairment by heptyl physostigmine, a long-lasting cholinesterase inhibitor, in primates. |
| title | Reversal of cognitive impairment by heptyl physostigmine, a long-lasting cholinesterase inhibitor, in primates. |
| title_full | Reversal of cognitive impairment by heptyl physostigmine, a long-lasting cholinesterase inhibitor, in primates. |
| title_fullStr | Reversal of cognitive impairment by heptyl physostigmine, a long-lasting cholinesterase inhibitor, in primates. |
| title_full_unstemmed | Reversal of cognitive impairment by heptyl physostigmine, a long-lasting cholinesterase inhibitor, in primates. |
| title_short | Reversal of cognitive impairment by heptyl physostigmine, a long-lasting cholinesterase inhibitor, in primates. |
| title_sort | reversal of cognitive impairment by heptyl physostigmine a long lasting cholinesterase inhibitor in primates |
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