McN 5691
- Product Name
- McN 5691
- CAS No.
- 99254-95-2
- Chemical Name
- McN 5691
- Synonyms
- 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)-
- CBNumber
- CB91321785
- Molecular Formula
- C30H35NO3
- Formula Weight
- 457.61
- MOL File
- 99254-95-2.mol
McN 5691 Property
- Boiling point:
- 595.6±50.0 °C(Predicted)
- Density
- 1.11±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 9.22±0.50(Predicted)
McN 5691 Chemical Properties,Usage,Production
Uses
McN5691 is a voltage-sensitive calcium channel blocker.
in vivo
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 14C-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 14C-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[2]. 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[3].
References
[1] Flaim SF, et al. Structurally novel antihypertensive compound, McN-5691, is a calcium channel blocker in vascular smooth muscle. J Pharmacol Exp Ther. 1991 Jan;256(1):279-88. PMID:1846419
[2] Wu WN, et al. Excretion and metabolism of the antihypertensive agent, RWJ-26240 (McN-5691) in dogs. Drug Metab Dispos. 1998 Feb;26(2):115-25. PMID:9456297
[3] Flaim SF, et al. Effects of the novel calcium channel blocker, McN-5691, on cardiocirculatory dynamics and cardiac output distribution in conscious spontaneously hypertensive rat. J Cardiovasc Pharmacol. 1988 Apr;11(4):489-500. DOI:10.1097/00005344-198804000-00017
McN 5691 Preparation Products And Raw materials
Raw materials
Preparation Products
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