Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1993-09-14
1996-06-04
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514561, 514567, A61K 31195, A61K 31215
Patent
active
055233236
ABSTRACT:
This invention concerns inhibitors of the tolerance and dependence induced by opiate analgesics. Excitatory amino acids control the action of the NMDA receptor through allosteric binding sites. Early studies showed that channel blockers and allosteric site antagonists of the NMDA receptor inhibited the development of tolerance to and dependence on opiate analgesics, but also produced their own undesirable side effects. Partial agonists of the NMDA allosteric sites tend to normalize NMDA receptor function and do not produce strong undesirable side effects. It has been discovered that partial agonists inhibit the development of tolerance to opiate analgesics, and it is taught that partial agonists also inhibit development of dependence on opiate analgesics. ACPC, 1-aminocyclopropanecarboxylic acid, in particular, is an exemplary partial agonist at the glysine site useful to treat opiate addiction. Compounds containing an opiate analgesic and a partial agonist, produce analgesia without inducing tolerance or dependence.
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