aticaprant (JNJ-67953964) / J&J 
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  • ||||||||||  aticaprant (JNJ-67953964) / J&J
    Review, Journal:  Aticaprant: (a ?-opioid receptor antagonist) for major depressive disorder. (Pubmed Central) -  Sep 26, 2024   
    Early evidence indicates Aticaprant may possess desirable pharmacodynamic and pharmacokinetic properties. A lack of convincing efficacy data at the time of writing precludes any definitive statement on its potential as an antidepressant.
  • ||||||||||  aticaprant (JNJ-67953964) / J&J
    Sex dependent regulation of effort and delay-related decision making by mu and kappa opioid receptors (WCC Halls A-C) -  Nov 3, 2023 - Abstract #Neuroscience2023NEUROSCIENCE_9496;    
    Rats were well trained until they displayed stable choice patterns, and then received systemic treatment with the selective mu receptor antagonist Naloxone or the selective kappa receptor antagonist Aticaprant (0, 1, 3, 10mg/kg doses used for both drugs)...Notably, however, these perturbations only appeared in the latter half of the session despite the task contingencies remaining stable over the entire session - suggesting altered satiety processing as a potential mechanism for the change in choice preference. Collectively, these data build a foundation for understanding the contribution of opioid receptor activity to cost/benefit decision making.
  • ||||||||||  aticaprant (JNJ-67953964) / J&J
    Imaging Kappa Opioid Receptor Status in a Titi Monkey Model of Human Pair Bonding; a Positron Emission Tomography (PET) Study (WCC Halls A-C) -  Nov 3, 2023 - Abstract #Neuroscience2023NEUROSCIENCE_2990;    
    Six adult titi monkeys were imaged on a dedicated primate brain PET scanner (PiPET, Brain Biosciences) under baseline conditions and after administration of: 1) a KOR antagonist (LY2456302; 0...This discrepancy may be due to facets of the KOR specific to titi monkeys as variation in binding affinity to these compounds is seen across primates. Nonetheless, these results indicate [11C]GR103545 PET is a powerful tool for monitoring KOR status in titi monkeys and will enable assessment of the KOR system concurrent with pair bonding behavioral assays.
  • ||||||||||  aticaprant (JNJ-67953964) / J&J
    The role of Claustrum Dynorphin/KOR signaling involved in stress-induced binge eating (WCC Halls A-C) -  Nov 3, 2023 - Abstract #Neuroscience2023NEUROSCIENCE_2681;    
    Injection of the KOR selective agonist U50,488H (5 mg/kg) resulted in an increase in HPD consumption while the KOR selective antagonists aticaprant (5 mg/kg) and norBNI (10 mg/kg) blocked forced-swim induced binge-eating behaviors, indicating a prominent role for dynorphin/KOR signaling in this behavior...Furthermore, the dynorphin/KOR system in the CLS appears to be important for this elevation in HPD intake after stress. This assay will allow researchers to begin to study the underlying hormonal and neural determinants behind stress-induced binge-eating behaviors mimicking eating disorders in humans.
  • ||||||||||  ASP8062 / Astellas, aticaprant (JNJ-67953964) / J&J
    Successes in Translation: Rapid Medication Development for PTSD, Alcohol and Opioid Use Disorders (Poinciana 3-4) -  Mar 18, 2023 - Abstract #ASCP2023ASCP_108;    
    P2
    Learning Objectives At the conclusion of the presentation, the learner will know more about promising novel treatments for ASUDs . At the conclusion of the presentation, the learner will have a better understanding of pre-clinical studies critical to establishing potential efficacy prior to assessing these treatments in human clinical trials.
  • ||||||||||  aticaprant (JNJ-67953964) / J&J
    Journal:  Multicatalysis protocol enables direct and versatile enantioselective reductive transformations of secondary amides. (Pubmed Central) -  Nov 24, 2022   
    The protocol also features excellent enantioselectivity, chemoselectivity, and functional group tolerance to be compatible with more reactive functional groups such as ketone and aldehyde. The synthetic utility of the method was further demonstrated by the late-stage functionalization of two drug derivatives and the concise, first catalytic asymmetric approach to the κ-opioid antagonist aticaprant.
  • ||||||||||  aticaprant (JNJ-67953964) / J&J
    Enrollment open:  VENTURA-LT: A Study of Aticaprant in Adult and Elderly Participants With Major Depressive Disorder (MDD) (clinicaltrials.gov) -  Nov 16, 2022   
    P3,  N=840, Recruiting, 
    The synthetic utility of the method was further demonstrated by the late-stage functionalization of two drug derivatives and the concise, first catalytic asymmetric approach to the κ-opioid antagonist aticaprant. Not yet recruiting --> Recruiting
  • ||||||||||  aticaprant (JNJ-67953964) / J&J
    Reversal of Stress Induced Behavioral Deficits by Aticaprant and a Role for Kors in Ketamine’s Antidepressant Action (Grand Sonoran H-J) -  Oct 31, 2022 - Abstract #ACNP2022ACNP_817;    
    Conclusions The ability of aticaprant to reverse stress induced deficits are consistent with clinically used antidepressants and support development of aticaprant as a therapeutic for psychiatric disorders. These studies provide new evidence that initial KOR activation by ketamine, possibly through acute dynorphin release, evokes a persistent downregulation of KOR signaling.
  • ||||||||||  aticaprant (JNJ-67953964) / J&J
    Enrollment open:  A Thorough QT Study of Aticaprant (JNJ-67953964) in Healthy Adult Participants (clinicaltrials.gov) -  May 26, 2022   
    P1,  N=60, Recruiting, 
    Our present study suggests that a combination of clinically developed, short-acting KOR antagonist aticaprant with low-dose naltrexone has therapeutic potential in alcohol "relapse" treatment. Not yet recruiting --> Recruiting
  • ||||||||||  aticaprant (CERC-501) / J&J
    Comparing of the Effects of Two Kappa Opioid Receptor Antagonists in male and female Fragile X transgenic mice (Virtual Only) -  Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_513;    
    To test our hypothesis, we examined the effects of two kappa opioid receptor antagonists, norbinaltorphimine (NorBNI) and aticaprant (LY245630) on nest building behavior in Fmr1 KO male and female mice...We are examining the potential cellular and molecular mechanisms underlying the sex differences. Collectively, our data suggest that the KOR plays a role in nest building behavior in the Fmr1 KO mouse and that FXS drug development efforts could target the KOR.; Grant Support: Jim and Betty Ann Rodgers Chair Fund; Council on Creative Research FSU
  • ||||||||||  aticaprant (CERC-501) / J&J
    Journal:  Kappa Opioid Receptor Antagonists as Potential Therapeutics for Mood and Substance Use Disorders. (Pubmed Central) -  Nov 29, 2021   
    One of these, JNJ-67953964 (also referred to as CERC-501, LY2456302, OpraKappa or Aticaprant) has been studied in humans, and shown to be safe, relatively KOR selective, and able to substantially attenuate binding of a KOR PET tracer to CNS localized KOR for greater than 24 h. While animal studies have indicated that compounds of this structural class are capable of normalizing withdrawal signs in animal models of cocaine and alcohol dependence and reducing cocaine and alcohol intake/seeking, additional studies are needed to determine the value of these second generation KOR antagonists in treating mood disorders and substance use disorders in humans.
  • ||||||||||  fentanyl citrate / Generic mfg.
    Role of dynorphin/κ-Opioid Receptor on Fentanyl Vapor Self-Administration in Mice ([VIRTUAL]) -  Nov 28, 2021 - Abstract #ACNP2021ACNP_1017;    
    The effect of chronic treatment with short-acting -opioid receptor antagonists on opioid self-administration remains to be tested. Deletion of the pro-dynorphin gene may have sex-dependent effects that merit further study.
  • ||||||||||  fentanyl citrate / Generic mfg.
    Role of dynorphin/κ-Opioid Receptor on Fentanyl Vapor Self-Administration in Mice (Exhibit Hall C) -  Nov 28, 2021 - Abstract #ACNP2021ACNP_717;    
    The effect of chronic treatment with short-acting -opioid receptor antagonists on opioid self-administration remains to be tested. Deletion of the pro-dynorphin gene may have sex-dependent effects that merit further study.
  • ||||||||||  tamoxifen / Generic mfg.
    Preclinical, Journal:  Sex differences in the modulation of mouse nest building behavior by kappa opioid receptor signaling. (Pubmed Central) -  Aug 14, 2021   
    The effects of the KOR agonist U50,488 and the KOR antagonist aticaprant were assessed on nest building behavior, an ethologically relevant indicator of overall well-being and affect, in adult male and female C57BL/6J mice...Pretreatment with the estrogen receptor modulator tamoxifen, at a dose which blocked estrogen receptors, augmented the effect of U50,488 on nesting in female mice, suggesting that estrogen receptors play a key role in attenuating the effects of KOR ligands in female mice...This behavioral sensitivity, as measured by nesting, may be mediated by estrogen receptors. Together these studies highlight the importance of comparing sex differences in response to KOR regulation on behaviors related to affective states.
  • ||||||||||  aticaprant (JNJ-67953964) / J&J
    Trial completion:  A Study of JNJ-67953964 in Healthy Japanese Adult Male Participants (clinicaltrials.gov) -  Aug 11, 2021   
    P1,  N=30, Completed, 
    Together these studies highlight the importance of comparing sex differences in response to KOR regulation on behaviors related to affective states. Recruiting --> Completed
  • ||||||||||  aticaprant (CERC-501) / J&J
    Preclinical, Journal:  Nicotine increases alcohol self-administration in male rats via a mu-opioid mechanism within the mesolimbic pathway. (Pubmed Central) -  Jun 22, 2021   
    Collectively, these results suggest that nicotine contributes to escalate alcohol self-administration through a dysregulation of MOR activity in the VTA. These data imply that targeting MORs, rather than KORs, may be the preferred pharmacotherapeutic approach for the treatment of alcohol use disorder when nicotine use contributes to alcohol consumption.
  • ||||||||||  naltrexone / Generic mfg.
    Journal:  Pre-training naltrexone increases conditioned fear learning independent of adolescent alcohol consumption history. (Pubmed Central) -  Jun 22, 2021   
    Our experiment replicates and extends previous demonstrations that a preferential MOR antagonist can increase fear learning using conditioned suppression of lever-pressing as a fear measure. However, additional research is needed to determine the cause of the differences in conditioned fear that we previously observed (as they were not observed in the current experiments).
  • ||||||||||  aticaprant (JNJ-67953964) / J&J
    Enrollment open:  A Study of JNJ-67953964 in Healthy Japanese Adult Male Participants (clinicaltrials.gov) -  May 11, 2021   
    P1,  N=30, Recruiting, 
    Moreover, the selectivity of KOR over MOR and DOR increased nearly 2-fold and 7-fold, respectively, compared with (±)LY2456302. Not yet recruiting --> Recruiting
  • ||||||||||  aticaprant (CERC-501) / J&J
    Journal:  Sex differences in kappa opioid receptor inhibition of latent postoperative pain sensitization in dorsal horn. (Pubmed Central) -  Jan 6, 2021   
    Sex studies revealed that LY2456302 (0.3 μg) reinstated hyperalgesia and pERK expression to a greater degree in female as compared to male mice. Our results suggest that spinal MOR and KOR, but not DOR, maintain LS within a state of remission to reduce the intensity and duration of postoperative pain, and that endogenous KOR but not MOR analgesia is greater in female mice.