Synthesis, biochemical and pharmacological properties of BUBUC, a highly selective and systemically active agonist for in vivo studies of δ-opioid receptors

Gacel, G.; Fellion, E.; Baamonde, Ana; Dauge, Valérie; Roques, Bernárd P.

doi:10.1016/0196-9781(90)90021-v

Cited by 36 publications

(16 citation statements)

References 29 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Our binding data (Table 1) have confirmed the high ␦-selectivity of the two compounds in the mouse strain under study. In our in vivo experiments, we have verified that deltorphin II analgesia is mediated by ␦-opioid receptors by using the selective ␦-antagonist naltrindole at a dose reported to be selective of ␦-opioid receptors (Gacel et al, 1990;Kalso et al, 1992). Thus, as for -agonists, we have good indications that the ␦-agonists act in a selective manner under our experimental conditions.…”

Section: ␦-Receptor Activity Is Slightly Reduced In Mice Lacking the mentioning

confidence: 57%

“…In the hot-plate test, naltrindole was able to decrease the analgesic effects of deltorphin II in both groups of mice. Although the dose of antagonist was higher than doses required in previous studies to block ␦-mediated responses (from 0.1 to 1 mg/kg) (Gacel et al, 1990;Baamonde et al, 1992;Kalso et al, 1992), one should note that a residual response seems to remain in the case of the hot-plate test ( jumping response). Furthermore, no significant difference between groups treated with deltorphin II alone or associated with naltrindole was observed for the licking response in MOR ϩ/ϩ mice.…”

Section: ␦ and Analgesia In Mor-deficient Micementioning

confidence: 88%

See 1 more Smart Citation

Activity of the δ-Opioid Receptor Is Partially Reduced, Whereas Activity of the κ-Receptor Is Maintained in Mice Lacking the μ-Receptor

et al. 1998

View full text Add to dashboard Cite

Previous pharmacological studies have indicated the possible existence of functional interactions between -, ␦-and -opioid receptors in the CNS. We have investigated this issue using a genetic approach. Here we describe in vitro and in vivo functional activity of ␦-and -opioid receptors in mice lacking the -opioid receptor (MOR). Measurements of agonist-induced [ ] enkephalin exhibited similar potency to inhibit smooth muscle contraction in both wild-type and MOR Ϫ/Ϫ mice. ␦-Analgesia induced by deltorphin II was slightly diminished in mutant mice, when the tail flick test was used. Deltorphin II strongly reduced the respiratory frequency in wild-type mice but not in MOR Ϫ/Ϫ mice. Analgesic and respiratory responses produced by the selective -agonist U-50,488H were unchanged in MOR-deficient mice. In conclusion, the preservation of ␦-and -receptor signaling properties in mice lacking -receptors provides no evidence for opioid receptor cross-talk at the cellular level. Intact antinociceptive and respiratory responses to the -agonist further suggest that the -receptor mainly acts independently from the -receptor in vivo. Reduced ␦-analgesia and the absence of ␦-respiratory depression in MOR-deficient mice together indicate that functional interactions may take place between -receptors and central ␦-receptors in specific neuronal pathways.

show abstract

Section: ␦-Receptor Activity Is Slightly Reduced In Mice Lacking the mentioning

confidence: 57%

Section: ␦ and Analgesia In Mor-deficient Micementioning

confidence: 88%

Activity of the δ-Opioid Receptor Is Partially Reduced, Whereas Activity of the κ-Receptor Is Maintained in Mice Lacking the μ-Receptor

et al. 1998

View full text Add to dashboard Cite

show abstract

“…Also, the activation of 6-opioid receptors either by BUBU, a highly selective 6-agonist (Gacel et al, 1990) Thus, it could be speculated that the antagonism of the hyperalgesia observed after administration of BC264 by the b-opioid agonist BUBU, could be due to an increase in endogenous CCK release which could counterbalance the hyperalgesic effects of BC264 through activation of the different receptor types.…”

Section: Hot-plate Testmentioning

confidence: 99%

Modulation of opioid antinociception by CCK at the supraspinal level: evidence of regulatory mechanisms between CCK and enkephalin systems in the control of pain

Noble

Derrien

Roques

1993

British J Pharmacology

View full text Add to dashboard Cite

1 Much evidence in the literature supports the idea that cholecystokinin (CCK) interacts with opioids in pain mechanisms. In this work, we have investigated the supraspinal interactions between enkephalins and CCK, using the hot plate test in mice. 2 Intracerebroventricular (i.c.v.) administration of BDNL (a mixed CCKA/CCKB agonist) induced dose-dependent antinociceptive responses on both paw lick and jump responses. In contrast, using the same test, the i.c.v. injection of BC 264 (a selective CCKB agonist) induced a hyperalgesic effect, which was restricted to paw licking and occurred only at a high dose of 2.5 nmol. 3 In addition, i.c.v. administration of BDNL potentiated the antinociceptive effects of the mixed inhibitor of enkephalin degrading enzymes, RB 101 and of the ni-agonist, DAMGO, while BC 264 reduced these effects. 4 Furthermore, at a dose where it interacts selectively with b-opioid receptors, the opioid agonist BUBU reversed the hyperalgesic responses of BC 264 (2.5 nmol) but was unable to modify the effects induced by BDNL. 5 Taken together, these results suggest the existence of regulatory mechanisms between CCK and enkephalin systems in the control of pain. These regulatory loops could enhance the antinociceptive effects of morphine allowing the opiate doses used to be reduced and thus, possibly, the side-effects to be minimized.

show abstract

“…Linear enkephalin analogs with enhanced DOPr selectivity include H-Tyr-D-Ala-Gly-Phe-D-Leu-OH (DADLE) (Beddell et al, 1977), H-Tyr-D-Ser-Gly-PheLeu-Thr-OH (DSLET) (Gacel et al, 1980), H-Tyr-D-ThrGly-Phe-Leu-Thr-OH (DTLET) (Zajac et al, 1983), and H-Tyr-D-Cys(tBu)-Gly-Phe-Leu-Thr(tBu)-OH (BUBUC) (Gacel et al, 1990) (Fig. 6).…”

Section: D-opioid Receptor Ligandsmentioning

confidence: 99%

Molecular Pharmacology ofδ-Opioid Receptors

et al. 2016

View full text Add to dashboard Cite

Synthesis, biochemical and pharmacological properties of BUBUC, a highly selective and systemically active agonist for in vivo studies of δ-opioid receptors

Cited by 36 publications

References 29 publications

Activity of the δ-Opioid Receptor Is Partially Reduced, Whereas Activity of the κ-Receptor Is Maintained in Mice Lacking the μ-Receptor

Activity of the δ-Opioid Receptor Is Partially Reduced, Whereas Activity of the κ-Receptor Is Maintained in Mice Lacking the μ-Receptor

Modulation of opioid antinociception by CCK at the supraspinal level: evidence of regulatory mechanisms between CCK and enkephalin systems in the control of pain

Molecular Pharmacology ofδ-Opioid Receptors

Contact Info

Product

Resources

About