盐酸吡美诺
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- CAS号:
- 61477-94-9
- 英文名:
- Pirmenol hydrochloride
- 英文别名:
- Cl 845;CI 845;Pimavar;Pirmavar;Ccris 5234;Pirmenol HCl;pirmenol hydrochloride;(à)-Pirmenol hydrochlorid;Pirmenol hydrochloride(cis);Pirmenol hydrochloride, >97%
- 中文名:
- 盐酸吡美诺
- 中文别名:
- 盐酸吡美诺;盐酸吡美诺?, >97%;化合物 PIRMENOL HYDROCHLORIDE
- CBNumber:
- CB31261216
- 分子式:
- C22H31ClN2O
- 分子量:
- 0
- MOL File:
- 61477-94-9.mol
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盐酸吡美诺化学性质
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熔点:
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171-172 °C
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储存条件:
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Sealed in dry,Room Temperature
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溶解度:
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DMSO : ≥ 28 mg/mL (74.68 mM)
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形态:
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Solid
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颜色:
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White to yellow
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盐酸吡美诺性质、用途与生产工艺
Pirmenol hydrochloride 通过阻断毒蕈碱性受体来抑制 IK.ACh。Pirmenol 抑制 Carbachol 诱导的 IK.ACh，IC50 值为 0.1 μM。
Pirmenol inhibits the carbachol-induced I
K.ACh
in a concentration-dependent manner. Pirmenol also inhibits the GTPγS-induced current although the concentrations of Pirmenol needed to inhibit the GTPγS-induced current are much higher than those to inhibit the carbachol-induced I
K.ACh
. The IC
50
of Pirmenol for inhibition of the GTPγS-induced currents is 30 μM. The inhibitory effect of Pirmenol on these I
K.ACh
is almost completely reversible and the outward current reappeared upon washout of Pirmenol. Pirmenol on the muscarinic acetylcholine receptor-operated K
+
current (I
K.ACh
) in atrial cells and on experimental atrial fibrillation in isolated guinea-pig hearts. In isolated atrial myocytes, Pirmenol concentration dependently inhibits the I
K.ACh
induced by carbachol or intracellular loading of GTPγS. In Langendorff-perfused hearts Pirmenol reverses the carbachol-induced decreases in effective refractory periods and atrial fibrillation threshold.
The pyridine-methanol derivative Pirmenol hydrochloride is a new antiarrhythmic agent. Single-dose studies in rodents demonstrate a 10- to 15-fold difference between the po and iv LD
50
values. In rats, the po LD
50
is 359.9 mg/kg and the iv LD
50
is 23.6 mg/kg. Mice LD
50
values are 215.5 and 20.8 mg/kg for po and iv routes, respectively. Short-term subacute iv toxicity studies in rats (2.5, 5.0, and 7.5 mg/kg) and dogs (2.5, 5, and 10 mg/kg) for 4 weeks elicite minimal reactions. Cardiac effects in dogs include drug related increases in heart rate, increases QRS duration, shortening of ST interval without evidence of cardiac tissue damage and mild local reaction at the injection site. Orally, Pirmenol is well tolerated for 13 weeks in rats receiving 25, 50, and 100 mg/kg/day while dogs given 5, 10, and 15 mg/kg/day shows anticholinergic effects at high levels (dryness of mucosae, body tremors). Heart rates are significantly accelerated only at the beginning of the study and QRS changes are seen with wide individual variations. No drug-related tissue changes are elicited in these species. Teratology studies in rats (50, 100, and 150 mg/kg) and in rabbits (10, 25, and 50 mg/kg) show no overt effect on organogenesis but embryotoxicity is seen at 150 mg/kg in rats.
盐酸吡美诺
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-100795A | 盐酸吡美诺
Pirmenol hydrochloride | 61477-94-9 | 5mg | 550元 |
| 2024/04/30 | HY-100795A | 盐酸吡美诺
Pirmenol hydrochloride | 61477-94-9 | 10mg | 900元 |
61477-94-9, 盐酸吡美诺 相关搜索:
- C22H31ClN2O
- 化合物 PIRMENOL HYDROCHLORIDE
- 盐酸吡美诺?, >97%
- 盐酸吡美诺
- 61477-94-9
- (à)-Pirmenol hydrochlorid
- Pirmenol hydrochloride(cis)
- Pirmenol hydrochloride, >97%
- PIRMENOL HYDROCHLORIDE; CI-845; PIMENOL; PIMAVAR
- Pimavar
- 4-((2R,6S)-2,6-Dimethylpiperidin-1-yl)-1-phenyl-1-(pyridin-2-yl)butan-1-ol hydrochloride
- Pirmenol HCl
- Ccris 5234
- 2-Pyridinemethanol, alpha-(3-(2,6-dimethyl-1-piperidinyl)propyl)-alpha-phenyl-, monohydrochloride, Z-(+-)-
- 2-Pyridinemethanol, alpha-(3-(2,6-dimethyl-1-piperidinyl)propyl)-alpha-phenyl-, monohydrochloride, cis-, (+-)-
- 1-Piperidinebutanol, 2,6-dimethyl-alpha-phenyl-alpha-(2-pyridyl)-, hydrochloride, Z-(+-)-
- (+-)-cis-2,6-Dimethyl-alpha-phenyl-alpha-2-pyridyl-1-piperidinebutanol monohydrochloride
- pirmenol hydrochloride
- Pirmavar
- Cl 845
- CI 845
- 2-Pyridinemethanol, a-[3-[(2R,6S)-2,6-dimethyl-1-piperidinyl]propyl]-a-phenyl-, monohydrochloride, rel- (9CI)
- 2-Pyridinemethanol, a-[3-(2,6-dimethyl-1-piperidinyl)propyl]-a-phenyl-, monohydrochloride, cis-(+-)-
- 2-Pyridinemethanol, a-[3-(2,6-dimethyl-1-piperidinyl)propyl]-a-phenyl-, monohydrochloride, cis-
- 4-[(2R,6S)-2,6-dimethyl-1-piperidyl]-1-phenyl-1-pyridin-2-yl-butan-1-o l hydrochloride