Binding of fentanyl and pethidine to muscarinic receptors in rat brain.

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Hustveit O

Binding of fentanyl and pethidine to muscarinic receptors in rat brain.

Jpn J Pharmacol. 1994 Jan;64(1):57-9.

PubMed ID

8164394 [ View in PubMed

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Abstract

Symptoms similar to the central anticholinergic syndrome are often seen after high dose fentanyl anesthesia. Therefore, the binding of fentanyl, alfentanil, pethidine and morphine to opioid and muscarinic receptors was investigated in rat brain homogenate with [3H]naloxone and [3H]QNB as the radioligands, respectively. Both pethidine and fentanyl inhibited [3H]QNB binding with Ki values in the micromolar range. Alfentanil and morphine had no affinity for muscarinic receptors. The ratio of the Ki values for muscarinic receptors versus opioid receptors was 2.5 for pethidine and 88 for fentanyl. It is concluded that binding of fentanyl to muscarinic receptors is likely to occur during high-dose fentanyl anesthesia.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Meperidine	Muscarinic acetylcholine receptor (Protein Group)	Protein group	Humans	Unknown	Binder	Details