Identification of a human delta opioid receptor: Cloning and expression

Richard J. Knapp, Ewa Malatynska, Lei Fang, Xiaoping Li, Elizabeth Babin, Michael Nguyen, Giovanna Santoro, Eva V. Varga, Victor J Hruby, William R Roeske, Henry I. Yamamura

Research output: Contribution to journalArticle

128 Citations (Scopus)

Abstract

The δ opioid receptor is an important target for analgesic drug development. This report describes the identification of δ opioid receptor clones from human cDNA libraries and the preparation of a human δ receptor cDNA in the pcDNA3 expression vector for transfection studies. The cDNA encodes a 372 amino acid protein that has 93% amino acid identity to mouse and rat δ receptors. COS-7 cells transfected with this clone express over 1.0 pmole receptor/mg protein when measured by saturation binding with [3H]naltrindole. The δ receptor selective ligands NTB, BNTX, [4′-Cl-Phe4]DPDPE and [D-Ala2, Glu4]deltorphin all have Ki values under 10 nM while the affinities of the μ and κ opioid receptor ligands CTAP and U-69593, respectively, are over 4.0 μM. Agonists show binding to multiple affinity states of the receptor consistent with the presence of G-protein coupled and uncoupled forms of the expressed receptor. The 8-fold higher affinity of NTB relative to BNTX suggests that the human δ receptor is of the δ2 subtype.

Original languageEnglish (US)
JournalLife Sciences
Volume54
Issue number25
DOIs
StatePublished - 1994

Fingerprint

Forensic Anthropology
delta Opioid Receptor
Cloning
Opioid Receptors
Organism Cloning
naltrindole
Complementary DNA
Clone Cells
D-Penicillamine (2,5)-Enkephalin
Ligands
Amino Acids
COS Cells
Gene Library
GTP-Binding Proteins
Transfection
Analgesics
Rats
Proteins

Keywords

  • cDNA library
  • endorphin receptors
  • radioligand binding
  • recombinant DNA

ASJC Scopus subject areas

  • Pharmacology

Cite this

Knapp, R. J., Malatynska, E., Fang, L., Li, X., Babin, E., Nguyen, M., ... Yamamura, H. I. (1994). Identification of a human delta opioid receptor: Cloning and expression. Life Sciences, 54(25). https://doi.org/10.1016/0024-3205(94)90138-4

Identification of a human delta opioid receptor : Cloning and expression. / Knapp, Richard J.; Malatynska, Ewa; Fang, Lei; Li, Xiaoping; Babin, Elizabeth; Nguyen, Michael; Santoro, Giovanna; Varga, Eva V.; Hruby, Victor J; Roeske, William R; Yamamura, Henry I.

In: Life Sciences, Vol. 54, No. 25, 1994.

Research output: Contribution to journalArticle

Knapp, RJ, Malatynska, E, Fang, L, Li, X, Babin, E, Nguyen, M, Santoro, G, Varga, EV, Hruby, VJ, Roeske, WR & Yamamura, HI 1994, 'Identification of a human delta opioid receptor: Cloning and expression', Life Sciences, vol. 54, no. 25. https://doi.org/10.1016/0024-3205(94)90138-4
Knapp, Richard J. ; Malatynska, Ewa ; Fang, Lei ; Li, Xiaoping ; Babin, Elizabeth ; Nguyen, Michael ; Santoro, Giovanna ; Varga, Eva V. ; Hruby, Victor J ; Roeske, William R ; Yamamura, Henry I. / Identification of a human delta opioid receptor : Cloning and expression. In: Life Sciences. 1994 ; Vol. 54, No. 25.
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