Gardneramine

Names

[ Name ]:
Gardneramine

[Synonym ]:
(12S,13S,16Z,17S)-3,4,6-Trimethoxy-16-(2-methoxyethylidene)-10-oxa-8,14-diazahexacyclo[11.6.1.0.0.0.0]icosa-2,4,6,8-tetraene
8,11,12a-Ethanylylidene-7H-pyrido[2',3':5,6]oxepino[2,3-b]indole, 7a,8,9,10,11a,12-hexahydro-1,2,4-trimethoxy-9-(2-methoxyethylidene)-, (7aS,8S,9Z,11aS)-
(5β,19E)-9,10,12,18-Tetramethoxy-1,2-didehydro-2,17-epoxy-5,16-cyclocorynox-19-en
8,11,12a-Ethanylylidene-7H-pyrido[2',3':5,6]oxepino[2,3-b]indole, 7a,8,9,10,11a,12-hexahydro-1,2,4-trimethoxy-9-(2-methoxyethylidene)-, (8S,9E,11aS,12aS,13S)-

Biological Activity

[Description]:

Gardneramine is an orally active alkaloid that acts like papaverine. Gardneramine has peripheral vascular diastolic effect, direct inhibition on myocardium and central inhibition. Gardneramine showed antihypertensive, vasodilatation and atrial inhibition effects in rabbit, dog and guinea pig models, respectively. Gardneramine also inhibits the movement of smooth muscle organs such as the stomach and intestines[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Others >> Others

[In Vitro]

Gardneramine (80 μg/mL; 0-20 min) 对豚鼠的心房产生抑制作用[1]。

[In Vivo]

Gardneramine (4 mg/kg; 静脉注射; 单剂量) 在兔子中导致血压下降 (36.6%)[1]。 Gardneramine (0.2 mg/kg, 0.4 mg/kg; 动脉注射; 单剂量) 在狗的后肢中增加血液流速，产生血管扩张作用[1]。 Gardneramine (20 mg/kg, 40 mg/kg, and 80 mg/kg; 腹腔注射; 单剂量) 在小鼠中抑制胃和肠等平滑肌器官的运动[1]。 Gardneramine (20 mg/kg; 口服; 单剂量) 处理小鼠后摘除小肠，显示出松弛作用，轻微抑制应激性离子产生[1]。

[References]

[1]. Harada M, et al. [Pharmacological studies on gardneria alkaloids. II. Peripheral effects (effects on circulatory and digestive systems)]. Yakugaku Zasshi. 1972 Dec;92(12):1540-6. Japanese.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
570.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₃H₂₈N₂O₅

[ Molecular Weight ]:
412.479

[ Flash Point ]:
298.7±32.9 °C

[ Exact Mass ]:
412.199829

[ PSA ]:
61.75000

[ LogP ]:
2.72

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.686

Safety Information

[ Hazard Codes ]:
Xi