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药品详细

Rescinnamine(Rescinnamine)

化学结构式图
中文名
Rescinnamine
英文名
Rescinnamine
分子式
C35H42N2O9
化学名
methyl (1R,15S,17R,18R,19S,20S)-6,18-dimethoxy-17-{[3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy}-3,13-diazapentacyclo[11.8.0.0^{2,10}.0^{4,9}.0^{15,20}]henicosa-2(10),4,6,8-tetraene-19-carboxylate
分子量
Average: 634.716
Monoisotopic: 634.289030952
CAS号
24815-24-5
ATC分类
C02A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Rescinnamine is an angiotensin-converting enzyme inhibitor used as an antihypertensive drug. It is an alkaloid obtained from Rauwolfia serpentina and other species of Rauwolfia. [Wikipedia]

生产厂家
  • Panray corp sub ormont drug and chemical co inc
  • Pfizer laboratories div pfizer inc
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Alkaloids and Alkaloid Derivatives
Substructures
  • Carboxylic Acids and Derivatives
  • Alkanes and Alkenes
  • Acetates
  • Indoles and Indole Derivatives
  • Monolignols
  • Phenols and Derivatives
  • Phenylpropenes
  • Pyrroles
  • Alkaloids and Alkaloid Derivatives
  • Ethers
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Catechols
  • Heterocyclic compounds
  • Aromatic compounds
  • Cinnamaldehydes
  • Anisoles
  • Tryptamines and Derivatives
  • Imines
  • (Iso)quinolines and Derivatives
  • Styrene Derivatives
  • Phenyl Esters
  • Piperidines
  • Cinnamates
适应症
药理
Indication For the treatment of hypertension.
Pharmacodynamics Used to treat hypertension. Rescinnamine inhibits angiotensin-converting enzyme. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex and general vasoconstriction, both of which lead to increases vascular resistance. By inhibiting angiotensin II, aldosterone reabsorption is decreased as well as vasoconstriction. This combined effect serves to decrease blood pressure.
Mechanism of action Rescinnamine Binds to and inhibits the angiotensin converting enzyme. Rescinnamine competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. Inhibition of ACE results in decreased plasma angiotensin II. As angiotensin II is a vasoconstrictor and a negative-feedback mediator for renin activity, lower concentrations result in a decrease in blood pressure and stimulation of baroreceptor reflex mechanisms, which leads to decreased vasopressor activity and to decreased aldosterone secretion.
Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Not Available
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00155 Rescinnamine Pathway SMP00155
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 238.5 °C PhysProp
logP 3.5 Not Available
Predicted Properties
Property Value Source
water solubility 3.49e-03 g/l ALOGPS
logP 4.48 ALOGPS
logP 4.07 ChemAxon
logS -5.3 ALOGPS
pKa (strongest acidic) 16.29 ChemAxon
pKa (strongest basic) 7.56 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 8 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 117.78 ChemAxon
rotatable bond count 11 ChemAxon
refractivity 171.16 ChemAxon
polarizability 69.65 ChemAxon
药物相互作用
食物相互作用
Not Available

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