Opioid receptor binding properties of analgesic analogues of cholecystokinin oceapeptide

Jirina Slaninova; Richard J. Knapp; Jinji Wu; Fang Su-Nan; Thomas Kramer; Thomas F. Burks; Victor J. Hruby; Henry I. Yamamura

doi:10.1016/0014-2999(91)90688-M

Opioid receptor binding properties of analgesic analogues of cholecystokinin oceapeptide

Jirina Slaninova, Richard J. Knapp, Jinji Wu, Fang Su-Nan, Thomas Kramer, Thomas F. Burks, Victor J. Hruby, Henry I. Yamamura

Chemistry and Biochemistry

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

33 Scopus citations

Abstract

Four analogues of cholecystokinin (CCK) octapeptide having analgesic activity after i.c.v. administration and high affinity for CCK-B receptors were studied for their ability to displace specific ligands,[³H]D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH₂. [³H]D-Pen², 4'-Cl-Phe⁴,D-Pen⁵]enkephalin and [³H]U-69,593. for μ-, δ- and κ-opioid receptors, respectively. None of the analogues tested have high affinity for either μ- or κ-receptors (IC₅₀ values > 0.7 μM), but their IC₅₀ values for δ-receptors range from 29 to 1023 nM. The results suggest a relationship between the ligand requirements of CCK-B and δ-opioid receptors which further implies a possible structural relationship between these receptors.

Original language	English (US)
Pages (from-to)	195-198
Number of pages	4
Journal	European Journal of Pharmacology
Volume	200
Issue number	1
DOIs	https://doi.org/10.1016/0014-2999(91)90688-M
State	Published - Jul 23 1991

Keywords

Analgesia
CCK analogues
CCK-B receptors
Cholecystokinin (CCK)
Opioid receptors
Radioligand binding

ASJC Scopus subject areas

Pharmacology

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10.1016/0014-2999(91)90688-M

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title = "Opioid receptor binding properties of analgesic analogues of cholecystokinin oceapeptide",

abstract = "Four analogues of cholecystokinin (CCK) octapeptide having analgesic activity after i.c.v. administration and high affinity for CCK-B receptors were studied for their ability to displace specific ligands,[3H]D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2. [3H]D-Pen2, 4'-Cl-Phe4,D-Pen5]enkephalin and [3H]U-69,593. for μ-, δ- and κ-opioid receptors, respectively. None of the analogues tested have high affinity for either μ- or κ-receptors (IC50 values > 0.7 μM), but their IC50 values for δ-receptors range from 29 to 1023 nM. The results suggest a relationship between the ligand requirements of CCK-B and δ-opioid receptors which further implies a possible structural relationship between these receptors.",

keywords = "Analgesia, CCK analogues, CCK-B receptors, Cholecystokinin (CCK), Opioid receptors, Radioligand binding",

author = "Jirina Slaninova and Knapp, {Richard J.} and Jinji Wu and Fang Su-Nan and Thomas Kramer and Burks, {Thomas F.} and Hruby, {Victor J.} and Yamamura, {Henry I.}",

year = "1991",

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doi = "10.1016/0014-2999(91)90688-M",

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AU - Slaninova, Jirina

AU - Knapp, Richard J.

AU - Wu, Jinji

AU - Su-Nan, Fang

AU - Kramer, Thomas

AU - Burks, Thomas F.

AU - Hruby, Victor J.

AU - Yamamura, Henry I.

PY - 1991/7/23

Y1 - 1991/7/23

N2 - Four analogues of cholecystokinin (CCK) octapeptide having analgesic activity after i.c.v. administration and high affinity for CCK-B receptors were studied for their ability to displace specific ligands,[3H]D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2. [3H]D-Pen2, 4'-Cl-Phe4,D-Pen5]enkephalin and [3H]U-69,593. for μ-, δ- and κ-opioid receptors, respectively. None of the analogues tested have high affinity for either μ- or κ-receptors (IC50 values > 0.7 μM), but their IC50 values for δ-receptors range from 29 to 1023 nM. The results suggest a relationship between the ligand requirements of CCK-B and δ-opioid receptors which further implies a possible structural relationship between these receptors.

AB - Four analogues of cholecystokinin (CCK) octapeptide having analgesic activity after i.c.v. administration and high affinity for CCK-B receptors were studied for their ability to displace specific ligands,[3H]D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2. [3H]D-Pen2, 4'-Cl-Phe4,D-Pen5]enkephalin and [3H]U-69,593. for μ-, δ- and κ-opioid receptors, respectively. None of the analogues tested have high affinity for either μ- or κ-receptors (IC50 values > 0.7 μM), but their IC50 values for δ-receptors range from 29 to 1023 nM. The results suggest a relationship between the ligand requirements of CCK-B and δ-opioid receptors which further implies a possible structural relationship between these receptors.

KW - Analgesia

KW - CCK analogues

KW - CCK-B receptors

KW - Cholecystokinin (CCK)

KW - Opioid receptors

KW - Radioligand binding

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Opioid receptor binding properties of analgesic analogues of cholecystokinin oceapeptide

Abstract

Keywords

ASJC Scopus subject areas

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