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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Opioid receptor binding properties of analgesic analogues of cholecystokinin oceapeptide. / Slaninova, Jirina; Knapp, Richard J.; Wu, Jinji; Su-Nan, Fang; Kramer, Thomas; Burks, Thomas F.; Hruby, Victor J.; Yamamura, Henry I.

In: European Journal of Pharmacology, Vol. 200, No. 1, 23.07.1991, p. 195-198.

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

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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.",

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AU - Su-Nan, Fang

AU - Kramer, Thomas

AU - Burks, Thomas F.

AU - Hruby, Victor J.

AU - Yamamura, Henry I.

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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.

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Opioid receptor binding properties of analgesic analogues of cholecystokinin oceapeptide

Abstract

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ASJC Scopus subject areas

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