BD 1063 Dihydrochloride | 150208-28-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: BD 1063 Dihydrochloride
• 英文别名: 1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine;dihydrochloride
• CAS: 150208-28-9；206996-13-6
• 化学式: C13H20Cl4N2
• 分子量: 346.1
• InChiKey: NXFDBTLQOARIMH-UHFFFAOYSA-N

物化性质

• 溶解度：
  H2O：>15mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  3.63
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  6.5
• 氢给体数：
  2
• 氢受体数：
  2

制备方法与用途

生物活性

BD1063 2HCL (BD1063 氢氯化物) 是一种有效的选择性 sigma-1 受体（σ1R）拮抗剂，对应的 Ki 值为 4.43 nM。

靶点

Target	Value
σ1R (Cell-free assay)	4.43 nM(Ki)

体内研究

BD1063 在剂量依赖性地减少大鼠在戒断和依赖状态下对酒精的自我管理行为（sP 大鼠：3.3-11 mg/kg；撤药依赖 Wistar 大鼠：4-11 mg/kg），且不会改变非依赖 Wistar 大鼠的平均酒精自我管理行为。BD1063 还减少了 sP 大鼠在梯度增强强化条件下为获得酒精而工作的断点，并剂量依赖性地减少暴饮暴食以及规律性进食，同时阻止了可口大鼠的进食速率增加。在明暗冲突测试中，BD1063 抗阻了避开区域的停留时间增加和可口饮食摄入量增加，但不影响运动活动。在 WT 小鼠给药 30 分钟前给予 BD1063 可预防 paclitaxel 引起的寒冷和机械性痛觉过敏现象。此外，急性给药的 BD1063 剂量依赖性地逆转了两种类型的 paclitaxel 引发的痛觉过敏。

用途

BD1063 是一种新颖的 σ-受体配体，具有拮抗作用。

文献信息

• COMPOSITIONS AND METHODS FOR TREATING HIV-ASSOCIATED NEUROCOGNITIVE DISORDERS
  申请人：NAIR MADHAVAN

  公开号：US20180256720A1

  公开（公告）日：2018-09-13

  The invention pertains to a formulation comprising magnetic nanoparticles (MENPs) conjugated to or mixed with a therapeutic cargo, the therapeutic cargo comprising an HIV inhibitor, an inhibitor of BACE-1 activity or expression, and a cocaine antagonist. In one embodiment, the formulation comprises WA, miR-107, and BD1063. The MENPs conjugated or mixed with the therapeutic cargo can be encapsulated within liposomes. The liposomes can be surface modified with an affinity ligand that targets the liposomes to the brain. The invention also pertains to a method of treating an HIV infection in a subject having cocaine addiction, by administering to the subject the formulation of the invention and applying to the subject magnetic forces to guide the MENPs across the blood brain barrier and into brain parenchyma and releasing the therapeutic cargo into the brain parenchyma by applying to the subject an alternating current.
• [EN] MEANS FOR MODULATION OF THE EFFECTS OF OPIOID-LIKE SUBSTANCES<br/>[FR] MOYEN DE MODULATION DES EFFETS DE SUBSTANCES DE TYPE OPIOIDE
  申请人：UNIVERSITAETSKLINIKUM MUENSTER

  公开号：WO2005079767A2

  公开（公告）日：2005-09-01

  The present invention relates to the use of an opiate-receptor antagonist for the preparation of a pharmaceutical composition for treating or preventing heart failure in a human subject or multi-organ dysfunction syndrome in a subject. The invention also relates to a method for treating a human subject suffering from heart failure or multi-organ dysfunction syndrome comprising the step of administering to said subject an opiate-receptor antagonist in a thera­peutically effective dosage.
• [EN] COMPOUND INDUCING LBPA ACCUMULATION FOR INHIBITING CELL-TO-CELL TRANSMISSION OF HIV<br/>[FR] COMPOSÉ INDUISANT UNE ACCUMULATION DE LBPA POUR INHIBER LA TRANSMISSION INTERCELLULAIRE DU VIH
  申请人：INST NAT SANTE RECH MED

  公开号：WO2012055814A1

  公开（公告）日：2012-05-03

  The present invention concerns a compound inducing Lyso-Bis Phosphatidic Acid (LPBA) accumulation in multi-vesicular bodies (MVB) of a cell for use for inhibiting i) cell-to-cell transmission of a Human Immunodeficiency Virus (HIV), and/or ii) entry of HIV into a cell, in an individual in need thereof. The invention further relates to products comprising a compound inducing LPBA accumulation in multi-vesicular bodies of a cell and an anti-HIV agent as combination products for simultaneous, sequential or separated use for the treatment and/or prevention of an infection with a HIV virus.