LY2828360 News - LARVOL Sigma

|||||||||| Acomplia (rimonabant) / Sanofi, MJN110 / Scripps Research Institute, LY2828360 / Eli Lilly
Journal: Combined Endocannabinoid and Cyclooxygenase Inhibition Additively Attenuates Post-Surgical Pain. (Pubmed Central) - Feb 14, 2025
The dose-dependent anti-allodynic effects of the MAGL inhibitors (irreversible MAGL inhibitor [JZL184] and selective MAGL inhibitor [MJN110]) and the NSAID diclofenac, as well as the additive potential of combined MAGL and cyclooxygenase (COX) inhibition, were assessed...Similarly, the anti-allodynic effects of the CB2-selective agonist (LY2828360) were tested...The anti-allodynic effects of JZL184 (40 mg/kg) were blocked by pre-treatment of the CB2 antagonist SR144528 (3 mg/kg) but not the CB1-selective antagonist rimonabant (SR141716A; 3 mg/kg), suggesting a CB2-mediated mechanism of anti-allodynia via MAGL inhibition...Finally, HPI per se increased pro-inflammatory cytokine levels, which were unaltered by MAGL inhibition despite the anti-allodynia assessed behaviorally. These data support simultaneously targeting endocannabinoids and COX enzymes as a potential post-operative pain management approach.

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Preclinical, Journal: The cannabinoid CB2 agonist LY2828360 suppresses neuropathic pain behavior and attenuates morphine tolerance and conditioned place preference in rats. (Pubmed Central) - Jan 6, 2025
These data support simultaneously targeting endocannabinoids and COX enzymes as a potential post-operative pain management approach. Here we show that LY2828360 (3 and 10

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Cannabinoid receptor 1 and 2 are involved in HIV-related neuropathic pain model (Exhibition Hall/Poster Area) - Jul 18, 2024 - Abstract #IASP2024IASP_1641;
Current preliminary data suggest that both CB1/2 agonists produced analgesia, but chronic ACEA for induced antinociceptive tolerance in HIV-related neuropathic pain model. We will continue to study the molecular mechanisms of HIV-related pain.No Conflict(s) of Interest in the research.

|||||||||| morphine sulphate / Generic mfg., paclitaxel / Generic mfg.
Journal: Cannabinoid CB2 receptors in primary sensory neurons are implicated in CB2 agonist-mediated suppression of paclitaxel-induced neuropathic nociception and sexually-dimorphic sparing of morphine tolerance. (Pubmed Central) - Jun 19, 2024
LY2828360 (3?mg/kg per day i.p. x 8 days) delayed, but did not prevent, the development of paclitaxel-induced mechanical or cold allodynia in either CB2f/f or CX3CR1CRE/+; CB2f/f mice of either sex. Our findings have potential clinical implications.

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Journal: Interacting with luteinizing hormone receptor provides a new elucidation of the mechanism of anti-androgenicity of bisphenol S. (Pubmed Central) - Jan 29, 2024
BPS mainly accumulated on the cell membrane, impermeable BPS-bovine serum albumin exposure still inhibited androgen synthesis, BPS interacted with rat luteinizing hormone receptor (LHR) via formation of hydrogen bonds in the transmembrane region, and the inhibitory effects of BPS on ERK1/2 phosphorylation were blocked by luteinizing hormone (the natural agonist of LHR), indicating that LHR located on the cell membrane is the target of action of BPS. This paper provides a new elucidation of the mechanism of anti-androgenicity of BPS, especially for the non-genomic pathways.

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Tlr4, lcn2, and cb1/2 are involved in HIV-related neuropathic pain model in mice (WCC Halls A-C) - Nov 3, 2023 - Abstract #Neuroscience2023NEUROSCIENCE_8929;
Either CB1 receptor agonist ACEA or CB2 receptor agonist LY2828360 suppressed neuropathic pain in mice. Current preliminary data suggest that TLR4, LCN2, and CB1/2 are involved in HIV-related neuropathic pain model in mice.

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Preclinical, Journal: Conditional deletion of CB2 cannabinoid receptors from peripheral sensory neurons eliminates CB2-mediated antinociceptive efficacy in a mouse model of carrageenan-induced inflammatory pain. (Pubmed Central) - Jul 14, 2023
and IL-10 mRNA in paw skin. Our results provide evidence that LY2828360 suppresses inflammatory nociception in mice through a neuronal CB-dependent mechanism that requires peripheral sensory neuron CB receptors and suggest that the clinical applications of LY2828360 as an anti-hyperalgesic agent should be re-evaluated.

|||||||||| morphine sulphate / Generic mfg.
Preclinical, Journal: Peripheral sensory neuron CB2 cannabinoid receptors are necessary for both CB2-mediated antinociceptive efficacy and sparing of morphine tolerance in a mouse model of anti-retroviral toxic neuropathy. (Pubmed Central) - Nov 24, 2022
The present studies indicate that CB2 activation may alleviate HIV-associated antiretroviral neuropathy and identify a previously unreported mechanism through which CB2 activation produces antinociceptive efficacy. Our results also provide the first evidence that a CB2 agonist can reverse established morphine tolerance and demonstrate that CB2 localized to peripheral sensory neurons mediates the opioid tolerance sparing efficacy of CB2 agonists.

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Synthetic CB1 agonists induce respiratory depression in awake adult mice - a potential role for beta arrestin (SDCC Halls B-H) - Oct 10, 2022 - Abstract #Neuroscience2022NEUROSCIENCE_10229;
These results suggest that CB1 receptors are expressed in CNS neurons that are responsible for the regulation of respiratory function. The susceptibility of these neurons to exogenous CB1 agonists may explain clinical observations of respiratory depression after the administration of synthetic cannabinoid drugs.

|||||||||| AM1710 - MAKScientific, Tetra Bio / Pharma, LY2828360 / Eli Lilly
Preclinical, Journal: A peripheral CB2 cannabinoid receptor mechanism suppresses chemotherapy-induced peripheral neuropathy: evidence from a CB2 reporter mouse. (Pubmed Central) - Apr 20, 2022
Quantification of the EGFP signal revealed that Langerhans cells were dynamically increased in the epidermis after paclitaxel treatment. Our studies implicate CB2 expressed in previously unrecognized populations of skin cells as a potential target for suppressing chemotherapy-induced neuropathic nociception.

|||||||||| fentanyl citrate / Generic mfg., paclitaxel / Generic mfg.
Journal: Cannabinoid CB Receptor Activation Attenuates Fentanyl-Induced Respiratory Depression. (Pubmed Central) - Jan 4, 2022
Moreover, the CB agonist, administered alone, did not alter respiration. Our findings suggest that the CB cannabinoid agonist LY2828360 may provide CB-mediated protection against fentanyl-induced respiratory depression, a detrimental and unwanted side effect of opioid use and abuse.

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Journal: Tubular human brain organoids to model microglia-mediated neuroinflammation. (Pubmed Central) - Jul 22, 2021
We found isogenic microglia were activated after exposure to an opioid receptor agonist (DAMGO) and transformed back to the homeostatic status with further treatment by a cannabinoid receptor 2 (CB2) agonist (LY2828360)...Our tubular organoid device is simple, versatile, inexpensive, easy-to-use, and compatible with multiwell-plates, so it can be widely used in common research and clinical laboratory settings. This technology can be broadly used for basic and translational applications in inflammatory diseases including substance use disorders, neural diseases, autoimmune disorders, and infectious diseases.

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Journal: The cannabinoid CB receptor agonist LY2828360 synergizes with morphine to suppress neuropathic nociception and attenuates morphine reward and physical dependence. (Pubmed Central) - May 15, 2021
Moreover, LY2828360 did not reliably alter morphine-induced slowing of colonic transit or attenuate tolerance to morphine antinociceptive efficacy in the hot plate test of acute nociception. Our results suggest that cannabinoid CB receptor activation enhances the therapeutic properties of opioids while attenuating unwanted side-effects such as reward and dependence that occur with sustained opioid treatment.

||||||||||  LY2828360 / Eli Lilly
Trial completion:  A Study of LY2828360 in Patients With Osteoarthritic Knee Pain (clinicaltrials.gov) -  Mar 21, 2012
P2, N=39, Completed,  Sponsor: Eli Lilly and Company
Our results suggest that cannabinoid CB receptor activation enhances the therapeutic properties of opioids while attenuating unwanted side-effects such as reward and dependence that occur with sustained opioid treatment. Recruiting --> Completed



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