Disease relevance of Lopac-B-9308

• At high doses BP 897 has been reported to produce catalepsy in rats [1].

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].

References