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盐酸Piperoxan

盐酸Piperoxan用途

Piperoxan hydrochloride 是一种 α₂ 肾上腺素受体拮抗剂。

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盐酸Piperoxan名称

[ CAS 号 ]:
135-87-5

[ 中文名 ]:
盐酸Piperoxan

[ 英文名 ]:
Piperoxan hydrochloride

[英文别名 ]:

Benzodioxane hydrochloride
Benodaine hydrochloride
EINECS 205-222-3
933F Hydrochloride
933F
2-Piperidinomethyl-1,4-benzodioxan hydrochloride
Piperoxan hydrochloride
Piperoxan (hydrochloride)

盐酸Piperoxan生物活性

[ 描述 ]:

Piperoxan hydrochloride 是一种 α2 肾上腺素受体拮抗剂。

[ 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 >> 炎症/免疫

[ 靶点 ]

adrenoceptor[1]

[体外研究]

当髓质用α2肾上腺素能受体拮抗剂Piperoxane(50μM; 5分钟)灌注,而脑桥用人工脑脊液(ACSF)时,三种无活性制剂以低频率(2-4 c/min)显示节律性膈神经爆发,在Piperoxane应用的最后3分钟内,12个活性物质的膈爆发频率显着增加(先前平均频率的163±12％)。在活性髓质制剂中,当ACSF(n = 8)或α2肾上腺素能受体拮抗剂Piperoxane(50μM; PIP-ACSF; n = 5)灌注制剂时,比较NA应用的效果(25μM; 5分钟)。 )。单独的NA应用(NA-ACSF)或与Piperoxane(PIP-ACSF + NA)的NA应用显着增加了膈爆发频率。然而,Piperoxane对延髓α2肾上腺素能受体的阻断增强了膈神经突发频率的增加：在NA应用的第5分钟,当单独应用ACSF时,膈爆发频率达到平均对照值的171±11％,并且234±21％当PIP-ACSF应用于控制条件[1]时的平均控制值。

[激酶实验]

小鼠新生儿（P0-P3）被乙醚麻醉并去除大脑;解剖出脑干和颈髓，并将腹侧朝上放置在2 mL室内，该室用人工脑脊液（ACSF）灌注，温度为27±0.25°C（平均值±SD），以2 mL / min的速率更新。 ACSF [含有（以mM计）129 NaCl，3.35 KCl，1.26 CaCl 2,1.15 MgCl 2,21 NaHCO 3,0.58 NaH 2 PO 4和30葡萄糖]通过鼓泡碳原子（95％O2-）氧化和平衡（pH 7.4在27°C） 5％CO2）。在药理实验中，它被另一种溶解有生物反应物质的ACSF所取代：25μM的去甲肾上腺素（NA-ACSF）或α2肾上腺素能受体拮抗剂，50μM的Piperoxane（PIP-ACSF）或50μM的育亨宾（YO-学联）。在一些实验中，膜片钳微电极（1μm直径尖端）在腹侧脑桥内降低到A5核中，其中ACSF或NA（1mM）的溶液被压力喷射。对于持续2 s的压力脉冲，估计弹出体积为20 nL [1]。

[动物实验]

小鼠[2]使用雄性Balb-C小鼠，体重在20至25g之间。在使用α-肾上腺素能受体拮抗剂Piperoxan或纳洛酮预处理的小鼠中，在乙酸前15分钟给予3×10-5 mol / kg sc的剂量，（ - ） - 异丙肾上腺素的抗伤害作用仅略微拮抗。剂量比为1.45和1.7，由这两种拮抗剂产生。

[参考文献]

[1]. Viemari JC, et al. Nasal trigeminal inputs release the A5 inhibition received by the respiratory rhythm generator of the mouse neonate. J Neurophysiol. 2004 Feb;91(2):746-58.

[2]. Bentley GA, et al. The antinociceptive action of some beta-adrenoceptor agonists in mice. Br J Pharmacol. 1986 Jul;88(3):515-21.

[相关活性小分子]

盐酸Piperoxan物理化学性质

[ 密度 ]:
1.113g/cm3

[ 沸点 ]:
331.5ºC at 760mmHg

[ 分子式 ]:
C₁₄H₂₀ClNO₂

[ 分子量 ]:
269.76700

[ 闪点 ]:
118.1ºC

[ 精确质量 ]:
269.11800

[ PSA ]:
21.70000

[ LogP ]:
3.05220

[ 蒸汽压 ]:
0.000155mmHg at 25°C

[ 储存条件 ]:
通风低温干燥

盐酸Piperoxan毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TM4550000

CHEMICAL NAME :: Piperidine, 1-(1,4-benzodioxan-2-ylmethyl)-, hydrochloride

CAS REGISTRY NUMBER :: 135-87-5

LAST UPDATED :: 199509

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C14-H19-N-O2.Cl-H

MOLECULAR WEIGHT :: 269.80

WISWESSER LINE NOTATION :: T66 BO EOT&J C1- AT6NTJ &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 502 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - excitement

REFERENCE :: JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 48,409,1959

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 175 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - excitement

REFERENCE :: JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 48,409,1959

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 500 mg/kg

TOXIC EFFECTS :: Behavioral - analgesia

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 13,17,1958

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 26 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 105,221,1956 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 735 mg/kg

SEX/DURATION :: female 3-9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 100,555,1959

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 250 mg/kg

SEX/DURATION :: female 5 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 100,555,1959