The interaction of eptazocine, a novel analgesic, with opioid receptors

Toshitaka Nabeshima, K. Matsuno, H. Kamei, T. Kameyama

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

The profile of action of eptazocine, a novel analgesic, on opioid receptors was investigated. Eptazocine caused a concentration-dependent inhibition against the [3H]-naloxone ([3H]-NLX) specific binding to rat brain synaptic membrane in the absence of sodium cation and GTP (IC50; 7.83 ± 1.57 μM). The ratios of IC50 values between the absence to the presence of sodium cation alone or sodium cation and GTP were 3.89 and 4.35, respectively. In addition, eptazocine (10 μM) also produced the significant decrease of [3H]-NLX specific binding in the mouse brain synaptic membrane. Moreover, the same dose eptazocine significantly decreased the [3H]-ethylketacyclazocine ([3H]-EKC) specific binding, but not [3H]-phencyclidine ([3H]-PCP). These results suggest that eptazocine interacts with opioid receptor, and is classified as one of the opiate agonist-antagonist analgesics.

Original languageEnglish
Pages (from-to)173-181
Number of pages9
JournalResearch Communications in Chemical Pathology and Pharmacology
Volume48
Issue number2
Publication statusPublished - 01-01-1985
Externally publishedYes

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Opioid Receptors
Analgesics
Cations
Synaptic Membranes
Sodium
Guanosine Triphosphate
Inhibitory Concentration 50
Opiate Alkaloids
Brain
Membranes
Phencyclidine
Naloxone
Rats
eptazocine

All Science Journal Classification (ASJC) codes

  • Pathology and Forensic Medicine
  • Toxicology
  • Pharmacology
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

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The interaction of eptazocine, a novel analgesic, with opioid receptors. / Nabeshima, Toshitaka; Matsuno, K.; Kamei, H.; Kameyama, T.

In: Research Communications in Chemical Pathology and Pharmacology, Vol. 48, No. 2, 01.01.1985, p. 173-181.

Research output: Contribution to journalArticle

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