MCN5691
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- CAS号:
- 99254-95-2
- 英文名:
- McN 5691
- 英文别名:
- McN 5691;RWJ-26240;RWJ-262240;McN-5691,McN5691;N-(3,4-Dimethoxyphenethyl)-5-methoxy-N,α-dimethyl-2-(phenylethynyl)benzenepropan-1-amine;N-[2-(3,4-dimethoxyphenyl)ethyl]-4-[5-methoxy-2-(2-phenylethynyl)phenyl]-N-methylbutan-2-amine;N-[2-(3,4-Dimethoxyphenyl)ethyl]-5-methoxy-N,α-dimethyl-2-(phenylethynyl)benzenepropane-1-amine;Benzenepropanamine, N-[2-(3,4-dimethoxyphenyl)ethyl]-5-methoxy-N,α-dimethyl-2-(2-phenylethynyl)-
- 中文名:
- MCN5691
- 中文别名:
- 化合物 T11979
- CBNumber:
- CB91321785
- 分子式:
- C30H35NO3
- 分子量:
- 457.61
- MOL File:
- 99254-95-2.mol
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MCN5691化学性质
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沸点:
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595.6±50.0 °C(Predicted)
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密度:
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1.11±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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9.22±0.50(Predicted)
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MCN5691性质、用途与生产工艺
McN5691 是一种电压依赖性钙通道 (calcium channel) 阻滞剂。
McN5691 (1 and 10 μM) prevents 60 mM KCl-induced contraction and calcium uptake and causes concentration-dependent relaxation (EC
50
=190 μM) of 30 mM KCl-contracted aortic rings. At or below 10 μM, McN5691 (McN-5691) has no effects on basal tone or calcium uptake (45Ca) in isolated rings of rabbit thoracic aorta. McN5691 causes complete high affinity inhibition (K
d
=39.5 nM) of specific diltiazem binding to the benzothiazepine receptor on the voltage-sensitive calcium channel in skeletal muscle microsomal membranes. In contrast to diltiazem, McN5691 inhibits specific dihydropyridine receptor binding, but the effect is biphasic with high (K
d
=4.7 nM) and low (K
d
=919.8 nM) affinity components. McN5691 inhibits norepinephrine (NE)-induced contraction (10 μM) and calcium uptake (1 and 10 μM) and causes concentration-dependent relaxation (EC
50
=159 μM) of 1 μM NE-contracted rings of rabbit thoracic aorta.
The excretion and metabolism of a 2-ethynylbenzenealkanamine analog, antihypertensive McN5691 (RWJ-26240), in beagle dogs is investigated. A total of 96.8% and 2.8% of the radioactive dose are excreted in feces and urine, respectively, during the 7 days after oral administration of
14
C-McN5691. Of the radioactive dose, 96.8% and 2.8% is recovered in feces and urine, respectively, in the 7 days after oral administration of
14
C-McN5691. More than 87% of the dose is excreted in feces during the 48 hours. McN5691 is extensively metabolized in dogs. Unchanged McN5691 is found in less than 0.1% and 19% of the dose in the 0-24 hour urine and 0-48 hour fecal extract, respectively, and 36% of the sample in the 4 hour plasma. In the McN5691 (McN-5691) study, vascular resistances tend to be higher in spontaneously hypertensive rat (SHR) than in Wistar-Kyoto (WKY) but the differences are statistically significant only in the cerebellum and the midbrain.
MCN5691
上下游产品信息
上游原料
下游产品
99254-95-2, MCN5691 相关搜索:
- 化合物 T11979
- 99254-95-2
- McN-5691,McN5691
- Benzenepropanamine, N-[2-(3,4-dimethoxyphenyl)ethyl]-5-methoxy-N,α-dimethyl-2-(2-phenylethynyl)-
- N-[2-(3,4-dimethoxyphenyl)ethyl]-4-[5-methoxy-2-(2-phenylethynyl)phenyl]-N-methylbutan-2-amine
- RWJ-26240
- RWJ-262240
- N-[2-(3,4-Dimethoxyphenyl)ethyl]-5-methoxy-N,α-dimethyl-2-(phenylethynyl)benzenepropane-1-amine
- N-(3,4-Dimethoxyphenethyl)-5-methoxy-N,α-dimethyl-2-(phenylethynyl)benzenepropan-1-amine
- McN 5691