Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors.
Science
; 279(5347): 77-81, 1998 Jan 02.
Article
em En
| MEDLINE
| ID: mdl-9417028
ABSTRACT
Development of analgesic agents for the treatment of severe pain requires the identification of compounds that are devoid of opioid receptor liabilities. A potent (inhibition constant = 37 picomolar) neuronal nicotinic acetylcholine receptor (nAChR) ligand called ABT-594 was developed that has antinociceptive properties equal in efficacy to those of morphine across a series of diverse animal models of acute thermal, persistent chemical, and neuropathic pain states. These effects were blocked by the nAChR antagonist mecamylamine. In contrast to morphine, repeated treatment with ABT-594 did not appear to elicit opioid-like withdrawal or physical dependence. Thus, ABT-594 may be an analgesic that lacks the problems associated with opioid analgesia.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Azetidinas
/
Receptores Nicotínicos
/
Agonistas Nicotínicos
/
Analgésicos não Narcóticos
Tipo de estudo:
Etiology_studies
Idioma:
En
Ano de publicação:
1998
Tipo de documento:
Article