生物活性 | |||
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描述 | BD-1047 Dihydrobromide is a selective functional antagonist of sigma-1 receptor, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia. BD 1047 did not decrease amphetamine-induced hyperactivity in mice in a statistically significant manner. Likewise, it did not modify the hyperactivity induced by NMDA receptor antagonists, phencyclidine, memantine or dizocilpine. On the other hand, BD 1047 (1-10 mg/kg; i.p.) attenuated apomorphine-induced climbing in mice and phencyclidine-induced head twitches in rats, like rimcazole and panamesine did[3]. BD-1047 Dihydrobromide prevents that Cutamesine reduces the cell death rate induced by light exposure in murine photoreceptor-derived 661w cells. BD-1047 attenuates that Cutamesine reduces the mitochondrial damage and the elevated level of caspase 3/7 activity[4]. Intrathecal (i.t.) pretreatment with the selective sigma-1 receptor antagonist, BD-1047 dihydrobromide (10-100 nmol) dose dependently reduced formalin-induced pain behaviors in second phase, but not first phase, of the formalin test. I.t. injection of BD-1047 also reduced formalin-evoked Fos expression and pNR1 at the protein kinase C-dependent site, serine-896 (Ser896) and the protein kinase A-dependent site, serine-897 (Ser897) in spinal dorsal horn.i.t[5]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.29mL 0.46mL 0.23mL |
11.44mL 2.29mL 1.14mL |
22.88mL 4.58mL 2.29mL |
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