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Chemical Compound Review

CHEMBL540612     N-[4-[4-(2- methoxyphenyl)piperazin-1...

Synonyms: LS-183769, AC1MI4Y6, MLS002153873, SMR001233227, 314776-92-6, ...
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Disease relevance of Lopac-B-9308


Psychiatry related information on Lopac-B-9308

  • In contrast to the full antagonists, against scopolamine-induced amnesia, the partial agonist BP-897 (2 mg/kg i.p.) was inactive, even at the two times higher dose level [2].
  • N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]naphthalene-2-carboxamide (BP 897) is a dopamine D3 receptor selective ligand recently described as partial agonist with potential effects on drug-dependence [3].

High impact information on Lopac-B-9308

  • Here we have designed BP 897, the first D3-receptor-selective agonist, as assessed in vitro with recombinant receptors and in vivo with mice bearing disrupted D3-receptor genes [4].
  • In conditioned mice, BP 897 inhibited c-fos expression in VTA and activated it in amygdala [5].
  • Cocaine-conditioned hyperactivity was inhibited by BP 897 or SB-277011-A, D3R-selective partial agonist and antagonist, respectively [5].
  • Cocaine cue-conditioned c-fos expression was found in cortical areas, notably in the somatosensory cortex, where it was inhibited by BP 897, and in several regions belonging or linked to the limbic system [5].
  • This suggested the hypothesis that intra-NAc or intra-basolateral amygdala (BLA) BP 897 would attenuate the expression, but not the acquisition, of amphetamine-conditioned activity [6].

Anatomical context of Lopac-B-9308

  • In vivo, BP 897 up to 8.2 mg/kg, i.v., had no agonistic effects on firing rate of substantia nigra dopaminergic neurons and antagonized the quinpirole-induced inhibition of firing (DID(50)=1.1 mg/kg) [3].

Associations of Lopac-B-9308 with other chemical compounds

  • RESULTS: D3 receptor agonists (7-OH-DPAT, quinelorane, BP 897) did not induce, alone, a significant CPP but, all of them, at the doses tested, and notably BP 897, a highly selective partial agonist, significantly enhanced acquisition of morphine-induced CPP when administered together with morphine at each conditioning session [7].
  • Our data demonstrate that BP 897 acts, in vivo and in vitro, as a dopamine D3 receptor antagonist [3].
  • 7-OH-DPAT (0.05 and 0.1 mg/kg), BP 897 (0.5 mg/kg) and diazepam (5 and 10 mg/kg), tested at the effective doses in an animal model, did not affect motor coordination but produced significant reduction in exploratory activity in the open field test [8].

Analytical, diagnostic and therapeutic context of Lopac-B-9308

  • In contrast, BP 897 did not alter morphine-induced analgesia, an unconditioned effect of this drug [7].
  • The partial agonist BP-897 (1 mg/kg) evoked slight but significant increase in self-administration, while the lower dose (0.5 mg/kg) was ineffective [9].


  1. BP 897, a selective dopamine D3 receptor ligand with therapeutic potential for the treatment of cocaine-addiction. Garcia-Ladona, F.J., Cox, B.F. CNS drug reviews. (2003) [Pubmed]
  2. Dopamine D3 receptor antagonists improve the learning performance in memory-impaired rats. Laszy, J., Laszlovszky, I., Gyertyán, I. Psychopharmacology (Berl.) (2005) [Pubmed]
  3. The dopamine D3 receptor partial agonist, BP 897, is an antagonist at human dopamine D3 receptors and at rat somatodendritic dopamine D3 receptors. Wicke, K., Garcia-Ladona, J. Eur. J. Pharmacol. (2001) [Pubmed]
  4. Selective inhibition of cocaine-seeking behaviour by a partial dopamine D3 receptor agonist. Pilla, M., Perachon, S., Sautel, F., Garrido, F., Mann, A., Wermuth, C.G., Schwartz, J.C., Everitt, B.J., Sokoloff, P. Nature (1999) [Pubmed]
  5. Role of the dopamine D3 receptor in reactivity to cocaine-associated cues in mice. Le Foll, B., Francès, H., Diaz, J., Schwartz, J.C., Sokoloff, P. Eur. J. Neurosci. (2002) [Pubmed]
  6. Intra-BLA or intra-NAc infusions of the dopamine D3 receptor partial agonist, BP 897, block intra-NAc amphetamine conditioned activity. Aujla, H., Beninger, R.J. Behav. Neurosci. (2004) [Pubmed]
  7. Dopamine D3 receptor ligands modulate the acquisition of morphine-conditioned place preference. Francès, H., Smirnova, M., Leriche, L., Sokoloff, P. Psychopharmacology (Berl.) (2004) [Pubmed]
  8. Anxiolytic-like effects of preferential dopamine D3 receptor agonists in an animal model. Rogóz, Z., Skuza, G., Kłodzińska, A. Polish journal of pharmacology. (2003) [Pubmed]
  9. Targeting the dopamine D3 receptor cannot influence continuous reinforcement cocaine self-administration in rats. Gál, K., Gyertyán, I. Brain Res. Bull. (2003) [Pubmed]
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