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 | |
State | Published - Jul 23 1991 |
Externally published | Yes |
Keywords
- Analgesia
- CCK analogues
- CCK-B receptors
- Cholecystokinin (CCK)
- Opioid receptors
- Radioligand binding
ASJC Scopus subject areas
- Pharmacology