2014
DOI: 10.2147/dddt.s55045
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Abstract: Based on numerous pharmacological studies that have revealed an interaction between cannabinoid and opioid systems at the molecular, neurochemical, and behavioral levels, a new series of hybrid molecules has been prepared by coupling the molecular features of two wellknown drugs, ie, rimonabant and fentanyl. The new compounds have been tested for their affinity and functionality regarding CB1 and CB2 cannabinoid and μ opioid receptors. In [35S]-GTPγS (guanosine 5′-O-[gamma-thio]triphosphate) binding assays fro… Show more

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Cited by 9 publications
(10 citation statements)
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References 36 publications
(43 reference statements)
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“…35 S]GTPgS binding tests, fentanyl activated G-protein stimulation with a maximum efficacy of 159.8% (nearly 60% above basal activity) and with a potency of 110.4 nM (Table S2, Figure S3A and C), which corresponds with previous studies 11 . Interestingly, all fentanyl analogues showed inverse agonist properties, since they reduced G-protein basal activity with very similar parameters: the maximum efficacy was between $80-100%, and their potency was between $3-5 mM ( Figure S3A and C, Table S2).…”
Section: S]gtpgs Binding Experimentssupporting
confidence: 89%
“…35 S]GTPgS binding tests, fentanyl activated G-protein stimulation with a maximum efficacy of 159.8% (nearly 60% above basal activity) and with a potency of 110.4 nM (Table S2, Figure S3A and C), which corresponds with previous studies 11 . Interestingly, all fentanyl analogues showed inverse agonist properties, since they reduced G-protein basal activity with very similar parameters: the maximum efficacy was between $80-100%, and their potency was between $3-5 mM ( Figure S3A and C, Table S2).…”
Section: S]gtpgs Binding Experimentssupporting
confidence: 89%
“…Within this context and in continuation to our previous work on multivalent ligands such as dual cannabinoid/PPARα 9, opioid/I 2 imidazoline 10, and cannabinoid/opioid ligands 11, we report here our attempt to prepare and evaluate a series of homobivalent cannabinoids, which could target CB 1 homodimer receptors simultaneously. They are composed of two functional pharmacophores linked by a spacer 12.…”
Section: Introductionmentioning
confidence: 82%
“…For example bivalent ligands for CB 1 receptor and MOR, that utilize the heterodimerization between these two receptors [125,126] are potential analgesics devoid of tolerance [126]. Additionally, the combination of FAAH inhibitors and dual enkephalinase inhibitors (DENKI) [127] might enhance pharmacological responses at lower doses [128].…”
Section: Interactions Between Cannabinoid and Opioid Receptorsmentioning
confidence: 99%