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(S)-(-)-哌多洛尔

(S)-(-)-哌多洛尔用途

l-Pindolol((-)-Pindolol)是一种可逆、竞争性和口服活性的5-HT1A/1B拮抗剂。l-Pindolol是一种部分β-肾上腺素受体激动剂。l-Pindolol可用于神经疾病的研究[1][2][3]。

(S)-(-)-哌多洛尔名称

[ CAS 号 ]:
26328-11-0

[ 中文名 ]:
(S)-(-)-哌多洛尔

[ 英文名 ]:
AGI-001

[英文别名 ]:

Tocris-1060
DL-AP4 Sodium salt

(S)-(-)-哌多洛尔生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[体外研究]

l-Pindolol(500 nM和 1微米)拮抗 5-羧胺色胺 (5-CT；10nM)和 5-羟色胺 (5英尺；15μM)通过检测 5克拉和 5吨对第1章锥体细胞的膜超极化[1]。 l-平多洛(1 nM-100μM)抑制 100 nM 5-CT诱导的第1章锥体细胞超极化,国际50值为 92nM[1]l-平多洛(1 nM-100μM)抑制 300 nM 5-CT引起的第三章神经元超极化,国际50值为 522nM[1]

[体内研究]

l-平多洛(15 mg/kg腹腔注射,[3H]-路100635注射前预处理) 减少了 [3H]-路100635在含有 5-羟色胺1a受体的脑区的积累。动物模型：雄性Sprague-Dawley大鼠[1]剂量：15 mg/kg给药：腹膜内注射；注射[3H]-WAY 100635前15 mg/kg、20分钟急性治疗或24小时、16小时和20分钟短期治疗结果：减少了含5-HT1A受体的脑区[3H]-WAY 10065的积聚,但对中缝背核(DRN)以及CA1和CA3海马区无影响。

(S)-(-)-哌多洛尔物理化学性质

[ 密度 ]:
1.152g/cm3

[ 沸点 ]:
457.1ºC at 760mmHg

[ 分子式 ]:
C₁₄H₂₀N₂O₂

[ 分子量 ]:
248.32100

[ 精确质量 ]:
248.15200

[ PSA ]:
57.28000

[ LogP ]:
2.29650

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
3.77E-09mmHg at 25°C

[ 折射率 ]:
1.596

(S)-(-)-哌多洛尔安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2933990090

(S)-(-)-哌多洛尔海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

(S)-(-)-哌多洛尔文献

Chemical genetics reveals a complex functional ground state of neural stem cells.

Nat. Chem. Biol. 3(5) , 268-273, (2007)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain canc...

Loss of [125I]-pindolol binding to beta-adrenoceptors on rat nodose ganglion after chronic isoprenaline treatment.

J. Auton. Nerv. Syst. 60 , 12-16, (1996)

The nodose ganglion contains the cell bodies of afferent nerves which convey predominantly sensory information from the viscera to the central nervous system (CNS). Autoradiographic studies show bindi...

Pindolol suppresses serotonergic neuronal activity and does not block the inhibition of serotonergic neurons produced by 8-hydroxy-2-(di-n-propylamino)tetralin in awake cats.

J. Pharmacol. Exp. Ther. 291 , 229, (1999)

Clinical studies have shown that pindolol can enhance the effects of antidepressant drugs, presumably by acting as an antagonist at somatodendritic 5-hydroxytryptamine (5-HT)(1A) autoreceptors, which ...

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