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In vivo apparent pA2 analysis for naltrexone antagonism of discriminative stimulus and analgesic effects of opiate agonists in rats.
TLDR
Six opiate agonists were characterized by in vivo apparent pA2 analysis with respect to their discriminative stimulus, rate-decreasing and analgesic effects, by using the antagonist naltrexone, suggesting that the measured behavioral effects of these agonists are mediated by mu opioid receptors.
Opioid thermal antinociception in rhesus monkeys: receptor mechanisms and temperature dependency.
TLDR
These studies suggest agonists may be differentiated based on antinociceptive effectiveness, receptor selectivity and intrinsic efficacy in the rhesus monkey tail-withdrawal procedure, consistent with possible low-efficacy mu agonist effects of these compounds.
Buprenorphine antagonism of mu opioids in the rhesus monkey tail-withdrawal procedure.
TLDR
Buprenorphine produced dose-dependent shifts to the right for the antinociceptive effects ofAlfentanil, etonitazene, morphine and nalbuphine 72 hr after administration and decreased the maximal effects of morphine in 48 degrees C water and those of alfent anil and eton itazene in 55 degrees CWater.
Opioid antagonists differ according to negative intrinsic efficacy in a mouse model of acute dependence
TLDR
Comparing the capacity of opioid antagonists to elicit withdrawal jumping in mice following two acute pretreatment doses of the opioid agonist morphine reveals a rank order of negative intrinsic efficacy for these opioid antagonists as follows: naloxone=naltrexonediprenorphine>nalorphine=naloxonazine.
Cannabidiol inhibits paclitaxel‐induced neuropathic pain through 5‐HT1A receptors without diminishing nervous system function or chemotherapy efficacy
TLDR
This work sought to determine receptor mechanisms by which CBD inhibits CIPN and whether CBD negatively effects nervous system function or chemotherapy efficacy and reported that chronic administration of the non‐psychoactive cannabinoid cannabidiol prevents PAC‐induced mechanical and thermal sensitivity in mice.
Effects of chemotherapeutic agents 5-fluorouracil and methotrexate alone and combined in a mouse model of learning and memory
TLDR
It is demonstrated that 5-fluorouracil causes increased latencies for retrieval of previously learned behavioral responses and that combination of chemotherapeutic agents may produce greater delays than either agent alone, including when neither agent alone does so.
Buprenorphine/naloxone reduces the reinforcing and subjective effects of heroin in heroin-dependent volunteers
TLDR
These data demonstrate that both 8/2 and 32/8 mg buprenorphine/naloxone were well tolerated and effective in reducing the reinforcing and subjective effects of heroin, relative to the 2/0.5-mg dose, and show for the first time in humans that it is possible to quantify the efficacy and affinity of heroin for mu opioid receptors.
Clavulanic acid enhances glutamate transporter subtype I (GLT-1) expression and decreases reinforcing efficacy of cocaine in mice
TLDR
It is suggested that the β-lactamase inhibitor CA can activate the cellular glutamate reuptake system in the brain reward circuit and reduce cocaine’s reinforcing efficacy at 100-fold lower doses than CTX.
Potency Differences ford-Phe-Cys-Tyr-d-Trp-Arg-Thr-Pen-Thr-NH2as an Antagonist of Peptide and Alkaloid μ-Agonists in an Antinociception Assay
d-Phe-Cys-Tyr-d-Trp-Arg-Thr-Pen-Thr-NH2(CTAP) is a peptide antagonist that demonstrates potent and selective affinity for μ-opioid receptors in radioligand binding assays and in vitro bioassays.
Differential tolerance to antinociceptive effects of µ opioids during repeated treatment with etonitazene, morphine, or buprenorphine in rats
TLDR
It is suggested that magnitude of antinociceptive tolerance is inversely related to relative efficacy of µ agonists, with lower efficacy agonists being more susceptible to tolerance than are higher efficacy agonist under these intermittent dosing conditions.
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