Abstract
The imidazoline nucleus linked in position 2 via an oxyethylene bridge to a phenyl ring carrying an ortho substituent of moderate steric bulk provided alpha(2)-adrenergic (AR) ligands endowed with significant alpha(2C)-agonism/alpha(2A)-antagonism. Similar behavior was displayed by cirazoline (12). For their positive morphine analgesia modulation (due to alpha(2C)-AR stimulation) and sedation overcoming (due to alpha(2A)-AR antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine.
MeSH terms
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Adjuvants, Pharmaceutic / pharmacology
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Adrenergic alpha-2 Receptor Agonists*
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Adrenergic alpha-2 Receptor Antagonists
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Adrenergic alpha-Agonists / pharmacology*
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Adrenergic alpha-Antagonists / pharmacology*
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Analgesics / therapeutic use*
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Animals
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CHO Cells
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Clonidine / pharmacology
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Cricetinae
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Cricetulus
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Drug Discovery
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Humans
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Imidazoles / pharmacology
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Morphine / therapeutic use*
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Pain / drug therapy*
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Pain / metabolism
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Receptors, Adrenergic, alpha-2
Substances
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ADRA2A protein, human
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Adjuvants, Pharmaceutic
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Adrenergic alpha-2 Receptor Agonists
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Adrenergic alpha-2 Receptor Antagonists
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Adrenergic alpha-Agonists
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Adrenergic alpha-Antagonists
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Analgesics
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Imidazoles
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Receptors, Adrenergic, alpha-2
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Morphine
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Clonidine
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cirazoline