Thermodynamic parameters for [D-Pen2,5]enkephalin at δ-opioid receptors in the mouse isolated vas deferens

Robert B. Raffa, Kenneth D. Wild, Henry I. Mosberg, Frank Porreca

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

Dissociation constants (KA) for [D-Pen2,5]enkephalin (DPDPE) inhibition of the electrically evoked twitch of the mouse isolated vas deferens preparations (MVD) were calculated at five temperatures (25, 30, 34, 37 and 40°C). These values were determined from the equiactive concentrations obtained before (A) and after (A′) partial irreversible blockade of a fraction of the receptor population by β-chlornaltrexamine (β-CNA) plotted as ( 1 A) against ( 1 A′) where KA = slope - 1)/intercept. The values of KA tended to increase (approximately doubled) over this temperature range, indicating that the affinity of DPDPE for the opioid δ receptor is an inverse function of temperature. From these results, thermodynamic parameters were calculated from a Van 't Hoff plot of 1n(KA) against 1 T. The relative magnitudes of the change in enthapy (ΔH°′ = -6.67 kcal mol-1), the change in entropy (ΔS°′ = +0.009 kcal mol-1 °K-1) and the change in free energy (ΔG°′ = -9.43 kcal mol-1) suggest that the interaction between DPDPE and the δ-opioid receptor in MVD is an exothermic exergonic reaction, predominantly enthalpy-driven and results in an increase in the entropy of the system.

Original languageEnglish (US)
Pages (from-to)231-238
Number of pages8
JournalEuropean Journal of Pharmacology: Molecular Pharmacology
Volume244
Issue number3
DOIs
StatePublished - Feb 15 1993

Keywords

  • DPDPE ([D-Pen,D-Pen]enkephalin)
  • Mouse vas deferens
  • Thermodynamics
  • δ-Opioid receptors

ASJC Scopus subject areas

  • Pharmacology

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