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Chemical Compound Review

Lopac-C-1112     2-[(1R,2R,5R)-5-hydroxy-2- (3...

Synonyms: CHEMBL559612, SureCN120410, AG-H-31781, C1112_SIGMA, CCG-204284, ...
 
 
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Disease relevance of Lopac-C-1112

  • Inhibition of the sRBC AFC response by both delta 9-THC (22 microM) and CP-55940 (5.2 microM) was also abrogated by preincubation of splenocytes for 24 hr with pertussis toxin (0.1-100 ng/mL) [1].
  • CP 55940 (2.5 mg kg(-1)) and anandamide (15 mg kg(-1)) significantly antagonized cocaine-induced lethality, and CP 55940 and WIN 55212-2 (2.5 mg kg(-1)) significantly attenuated the severity of cocaine-induced convulsive seizures [2].
 

Psychiatry related information on Lopac-C-1112

 

High impact information on Lopac-C-1112

  • The amount of Krox-24 protein and the level of Krox-24 DNA binding activity, as measured by Western blot and electrophoretic mobility shift assay, respectively, were also increased by the addition of CP-55940 [4].
  • Furthermore, CP 55940 was unable to induce mitogen-activated protein kinase activation in either cortical or striatal neurons [5].
  • In conclusion, our results show nanomolar efficiencies for CP 55940 and WIN 55212-2 on adenylyl cyclase activity and no effect on any other signal transduction pathway investigated in primary neuronal cultures [5].
  • The rank order of potency for the activation of MAP kinases with various cannabinoid agonists is CP-55940 > delta 9-tetrahydrocannabinol > WIN 55212.2, in agreement with the pharmacological profile of CB1 [6].
  • Compound 7 discriminates for delta 1-THC (2) in pigeons (ED50 = 0.002 mg/kg, after 4.5 h), at the potency level of 3, and binds to the cannabinoid receptor with a KD of 45 pM, considerably lower than the Ki of 180 pM measured for compound 3 and the Ki of 2.0 nM measured for CP-55940 (1), a widely employed ligand [7].
 

Anatomical context of Lopac-C-1112

  • 1. The dose-related inhibition of the twitch responses of the myenteric plexus-longitudinal muscle preparation of the guinea-pig small intestine by cannabinoid (CB) agonists, (+)-WIN 55212 and CP 55940 during stimulation at 0.1 Hz with supramaximal voltage was confirmed [8].
  • In the present study, we demonstrate that the cannabinoid agonist CP-55940 induced cytosol alkalinization of CHO-CB1 cells in a dose- and time-dependent manner via activation of the Na+/H+ exchanger NHE-1 isoform [9].
  • In anaesthetized rats, intravenous administrations of WIN 55212-2 (31.3-500 microg/kg) or CP 55940 (31.3-500 microg/kg) increased the firing rate of locus coeruleus neurons in a dose-dependent manner [10].
  • Only 3/18 medial vestibular nucleus neurons tested with 1 microM CP 55940 showed changes in firing rate, however these were decreases with an average magnitude of 72.3%; 3/4 neurons tested with 10 microM CP 55940 showed decreases with an average magnitude of 92.7% (P < 0.05 in both cases) [11].
  • Clozapine decreases [3H] CP 55940 binding to the cannabinoid 1 receptor in the rat nucleus accumbens [12].
 

Associations of Lopac-C-1112 with other chemical compounds

  • We investigated the effects of the selective CB1 receptor agonist, CP 55940 (the levorotatory enantiomer of desacetyllevonantradol), on medial vestibular nucleus neurons in guinea pig brainstem slices in vitro [11].
  • When injected unilaterally into the mouse striatum, cannabinoid agonists such as Win 55212-2 (1-100 ng/mouse), CP 55940 (0.1-50 ng/mouse), and anandamide (0.5-50 ng/mouse), the putative endogenous ligand of CB1 receptor, dose-dependently induced turning behavior [13].
  • Spiroperidol (a D2 receptor blocker), (+)-SCH 23390 (a D1 receptor blocker), or prior 6-OHDA lesions of the striatum blocked Win 55212-2- and CP 55940-induced turning, thus suggesting the involvement of DA transmission in cannabinoid-induced turning [13].
 

Gene context of Lopac-C-1112

  • Competition binding in intact mouse splenocytes demonstrated that nonradiolabeled cannabinoids CP-55940, Win-55212-2, CP-56667, delta 9-THC, and cannabinol all competed for receptor binding with 3H-CP-55940, a high-affinity nondiscriminating CB1 and CB2 receptor ligand [14].
  • Local pressure ejection of the cannabinoid agonists Win 55212-2 (WIN2) and CP 55940 increased SNpr spontaneous firing rate by 13-46%, similar to the effects of systemic injections [15].
  • In addition to AEA, the effects of the AEA analogs arachidonyl-2-chloroethylamide (ACEA), arachidonylcyclopropylamide (ACPA) and R-(+)-methanandamide (METH) were compared to the selective and strong CB1 agonist CP 55940 (CP) [16].
 

Analytical, diagnostic and therapeutic context of Lopac-C-1112

  • Pre-exposure to the cannabinoid receptor agonist CP 55940 enhances morphine behavioral sensitization and alters morphine self-administration in Lewis rats [17].
  • Likewise, in rat brain slice preparations perfusion with WIN 55212-2 (10 microM) or CP 55940 (10-30 microM) did not specifically affect the spontaneous firing rate of locus coeruleus cells [10].

References

  1. Suppression of the humoral immune response by cannabinoids is partially mediated through inhibition of adenylate cyclase by a pertussis toxin-sensitive G-protein coupled mechanism. Kaminski, N.E., Koh, W.S., Yang, K.H., Lee, M., Kessler, F.K. Biochem. Pharmacol. (1994) [Pubmed]
  2. Protective effects of cannabinoid receptor agonists against cocaine and other convulsant-induced toxic behavioural symptoms. Hayase, T., Yamamoto, Y., Yamamoto, K. J. Pharm. Pharmacol. (2001) [Pubmed]
  3. Repeated cannabinoid exposure during perinatal, adolescent or early adult ages produces similar longlasting deficits in object recognition and reduced social interaction in rats. O'shea, M., McGregor, I.S., Mallet, P.E. J. Psychopharmacol. (Oxford) (2006) [Pubmed]
  4. Stimulation of cannabinoid receptor CB1 induces krox-24 expression in human astrocytoma cells. Bouaboula, M., Bourrié, B., Rinaldi-Carmona, M., Shire, D., Le Fur, G., Casellas, P. J. Biol. Chem. (1995) [Pubmed]
  5. Characterization of CB1 receptors on rat neuronal cell cultures: binding and functional studies using the selective receptor antagonist SR 141716A. Jung, M., Calassi, R., Rinaldi-Carmona, M., Chardenot, P., Le Fur, G., Soubrié, P., Oury-Donat, F. J. Neurochem. (1997) [Pubmed]
  6. Activation of mitogen-activated protein kinases by stimulation of the central cannabinoid receptor CB1. Bouaboula, M., Poinot-Chazel, C., Bourrié, B., Canat, X., Calandra, B., Rinaldi-Carmona, M., Le Fur, G., Casellas, P. Biochem. J. (1995) [Pubmed]
  7. A novel probe for the cannabinoid receptor. Devane, W.A., Breuer, A., Sheskin, T., Järbe, T.U., Eisen, M.S., Mechoulam, R. J. Med. Chem. (1992) [Pubmed]
  8. Inhibition by cannabinoid receptor agonists of acetylcholine release from the guinea-pig myenteric plexus. Coutts, A.A., Pertwee, R.G. Br. J. Pharmacol. (1997) [Pubmed]
  9. Cannabinoid receptor CB1 activates the Na+/H+ exchanger NHE-1 isoform via Gi-mediated mitogen activated protein kinase signaling transduction pathways. Bouaboula, M., Bianchini, L., McKenzie, F.R., Pouyssegur, J., Casellas, P. FEBS Lett. (1999) [Pubmed]
  10. Systemic effect of cannabinoids on the spontaneous firing rate of locus coeruleus neurons in rats. Mendiguren, A., Pineda, J. Eur. J. Pharmacol. (2006) [Pubmed]
  11. Potent effects of a selective cannabinoid receptor agonist on some guinea pig medial vestibular nucleus neurons. Newsham-West, D., Darlington, C.L., Smith, P.F. Eur. J. Pharmacol. (1998) [Pubmed]
  12. Clozapine decreases [3H] CP 55940 binding to the cannabinoid 1 receptor in the rat nucleus accumbens. Sundram, S., Copolov, D., Dean, B. Naunyn Schmiedebergs Arch. Pharmacol. (2005) [Pubmed]
  13. Intrastriatal injection of cannabinoid receptor agonists induced turning behavior in mice. Souilhac, J., Poncelet, M., Rinaldi-Carmona, M., Le Fur, G., Soubrié, P. Pharmacol. Biochem. Behav. (1995) [Pubmed]
  14. Cannabinoid receptors CB1 and CB2: a characterization of expression and adenylate cyclase modulation within the immune system. Schatz, A.R., Lee, M., Condie, R.B., Pulaski, J.T., Kaminski, N.E. Toxicol. Appl. Pharmacol. (1997) [Pubmed]
  15. Local pressure application of cannabinoid agonists increases spontaneous activity of rat substantia nigra pars reticulata neurons without affecting response to iontophoretically-applied GABA. Tersigni, T.J., Rosenberg, H.C. Brain Res. (1996) [Pubmed]
  16. Protective effects of cannabinoid receptor ligands analogous to anandamide against cocaine toxicity. Hayase, T., Yamamoto, Y., Yamamoto, K. Nihon Arukōru Yakubutsu Igakkai zasshi = Japanese journal of alcohol studies & drug dependence. (2001) [Pubmed]
  17. Pre-exposure to the cannabinoid receptor agonist CP 55940 enhances morphine behavioral sensitization and alters morphine self-administration in Lewis rats. Norwood, C.S., Cornish, J.L., Mallet, P.E., McGregor, I.S. Eur. J. Pharmacol. (2003) [Pubmed]
 
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