Partial and full agonism in endomorphin derivatives: Comparison by null and operational model

A. Rónai, M. Al-Khrasani, S. Benyhe, Imre Lengyel, László Kocsis, G. Orosz, Géza Tóth, Erzsébet Kató, L. Tóthfalusi

Research output: Contribution to journalArticle

17 Citations (Scopus)

Abstract

The partial μ-opioid receptor pool inactivation strategy in isolated mouse vas deferens was used to determine partial agonism of endomorphins and their analogs (endomorphin-1-ol, 2′,6′-dimethyltyrosine (Dmt)-endomorphin-1, endomorphin-2-ol and (d-Met2)-endomorphin-2) using morphine, normorphine, morphiceptin, (d-Ala2,MePhe4,Gly5-ol)-enkephalin (DAMGO) and its amide (DAMGA) as reference opioid agonists. Agonist affinities (KA) and efficacies were assessed both by the "null" and the "operational" method. The KA values determined by the two methods correlated significantly with each other and also with the displacing potencies against 3H-naloxone in the receptor binding assay in the presence of Na+. DAMGO and DAMGA were full agonist prototypes, morphine, endomorphin-1, endomorphin-1-ol, Dmt-endomorphin-1, endomorphin-2-ol and (d-Met2)-endomorphin-2 were found by both methods to be partial agonists whereas the parameters for normorphine, morphiceptin and endomorphin-2 were intermediate.

Original languageEnglish
Pages (from-to)1507-1513
Number of pages7
JournalPeptides
Volume27
Issue number6
DOIs
Publication statusPublished - Jun 2006

Fingerprint

Derivatives
Enkephalins
Amides
Morphine
Ala(2)-MePhe(4)-Gly(5)-enkephalin
Opioid Receptors
Naloxone
Vas Deferens
endomorphin 2
Opioid Analgesics
Assays
endomorphin 1
morphiceptin
normorphine

Keywords

  • β-Funaltrexamine
  • Endomorphin derivatives
  • Mouse vas deferens
  • Null and operational model
  • Partial agonism
  • Residual receptor fraction

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Physiology
  • Cellular and Molecular Neuroscience

Cite this

Partial and full agonism in endomorphin derivatives : Comparison by null and operational model. / Rónai, A.; Al-Khrasani, M.; Benyhe, S.; Lengyel, Imre; Kocsis, László; Orosz, G.; Tóth, Géza; Kató, Erzsébet; Tóthfalusi, L.

In: Peptides, Vol. 27, No. 6, 06.2006, p. 1507-1513.

Research output: Contribution to journalArticle

Rónai, A. ; Al-Khrasani, M. ; Benyhe, S. ; Lengyel, Imre ; Kocsis, László ; Orosz, G. ; Tóth, Géza ; Kató, Erzsébet ; Tóthfalusi, L. / Partial and full agonism in endomorphin derivatives : Comparison by null and operational model. In: Peptides. 2006 ; Vol. 27, No. 6. pp. 1507-1513.
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