The ligand-selectivity of cloned human and rat opiate mu receptors studied with [125I]IOXY-AGO

Richard B. Rothman; Heng Xu; Jia Bel Wang; John S. Partilla; Hiroshi Kayakiri; Kenner C. Rice; George R. Uhl

doi:10.1016/0167-0115(94)90483-9

The ligand-selectivity of cloned human and rat opiate mu receptors studied with [¹²⁵I]IOXY-AGO

Richard B. Rothman, Heng Xu, Jia Bel Wang, John S. Partilla, Hiroshi Kayakiri, Kenner C. Rice, George R. Uhl

Research output: Contribution to journal › Article › peer-review

1 Scopus citations

Abstract

The recent molecular cloning of μ, δ and κ opiate receptors (1-5) has created new opportunities for the study of opiate receptors. The recent cloning of the human μ receptor (6) has shown that there is a high homology between the predicted human and rat μ receptor sequences, but also some differences in sequence. We therefore sought significant changes in the ligand-selectivity profile of these two receptors expressed in the COS and CHO cell lines under identical assay conditions. We used the novel agonist ligand [¹²⁵I]IOXY-AGO (6β-[¹²⁵Iodo]-3,14-dihydroxy-17-methyl-4,5α-epoxymorphinan) since its high specific activity (2200 Ci/mmol) and high affinity for μ opioid receptors generated a high signal-to-noise ratio with use of relatively few expressing cells. (7). The results indicate substantial similarities in ligand-selectivity profile of the human and rat μ receptors, but also modest differences.

Original language	English (US)
Pages (from-to)	249-250
Number of pages	2
Journal	Regulatory Peptides
Volume	54
Issue number	1
DOIs	https://doi.org/10.1016/0167-0115(94)90483-9
State	Published - Nov 10 1994
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Endocrinology
Physiology
Neuroscience(all)

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title = "The ligand-selectivity of cloned human and rat opiate mu receptors studied with [125I]IOXY-AGO",

abstract = "The recent molecular cloning of μ, δ and κ opiate receptors (1-5) has created new opportunities for the study of opiate receptors. The recent cloning of the human μ receptor (6) has shown that there is a high homology between the predicted human and rat μ receptor sequences, but also some differences in sequence. We therefore sought significant changes in the ligand-selectivity profile of these two receptors expressed in the COS and CHO cell lines under identical assay conditions. We used the novel agonist ligand [125I]IOXY-AGO (6β-[125Iodo]-3,14-dihydroxy-17-methyl-4,5α-epoxymorphinan) since its high specific activity (2200 Ci/mmol) and high affinity for μ opioid receptors generated a high signal-to-noise ratio with use of relatively few expressing cells. (7). The results indicate substantial similarities in ligand-selectivity profile of the human and rat μ receptors, but also modest differences.",

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AU - Rothman, Richard B.

AU - Xu, Heng

AU - Wang, Jia Bel

AU - Partilla, John S.

AU - Kayakiri, Hiroshi

AU - Rice, Kenner C.

AU - Uhl, George R.

PY - 1994/11/10

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N2 - The recent molecular cloning of μ, δ and κ opiate receptors (1-5) has created new opportunities for the study of opiate receptors. The recent cloning of the human μ receptor (6) has shown that there is a high homology between the predicted human and rat μ receptor sequences, but also some differences in sequence. We therefore sought significant changes in the ligand-selectivity profile of these two receptors expressed in the COS and CHO cell lines under identical assay conditions. We used the novel agonist ligand [125I]IOXY-AGO (6β-[125Iodo]-3,14-dihydroxy-17-methyl-4,5α-epoxymorphinan) since its high specific activity (2200 Ci/mmol) and high affinity for μ opioid receptors generated a high signal-to-noise ratio with use of relatively few expressing cells. (7). The results indicate substantial similarities in ligand-selectivity profile of the human and rat μ receptors, but also modest differences.

AB - The recent molecular cloning of μ, δ and κ opiate receptors (1-5) has created new opportunities for the study of opiate receptors. The recent cloning of the human μ receptor (6) has shown that there is a high homology between the predicted human and rat μ receptor sequences, but also some differences in sequence. We therefore sought significant changes in the ligand-selectivity profile of these two receptors expressed in the COS and CHO cell lines under identical assay conditions. We used the novel agonist ligand [125I]IOXY-AGO (6β-[125Iodo]-3,14-dihydroxy-17-methyl-4,5α-epoxymorphinan) since its high specific activity (2200 Ci/mmol) and high affinity for μ opioid receptors generated a high signal-to-noise ratio with use of relatively few expressing cells. (7). The results indicate substantial similarities in ligand-selectivity profile of the human and rat μ receptors, but also modest differences.

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The ligand-selectivity of cloned human and rat opiate mu receptors studied with [¹²⁵I]IOXY-AGO

Abstract

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