Colestyramine

Names

[ Name ]:
Colestyramine

[Synonym ]:
colestyramin
CHOLESTYRAMINE RESIN
4-[3-(4-Ethylphenyl)butyl]-N,N,N-trimethylanilinium chloride
Benzenaminium, 4-[3-(4-ethylphenyl)butyl]-N,N,N-trimethyl-, chloride (1:1)
cholestyraminechloride
cuemid
polystyrenebenzyltrimethylaminoniumchloride
quantalan
MFCD00130784
CHOLESTYRAMINE
EINECS 234-270-8
DOWEX 1 X 2 CL-FORM
Colestyramine

Biological Activity

[Description]:

Colestyramine (Cholestyramine) is a bile acid binding resin and can inhibit intestinal bile acid absorption which results in the increasing bile acid synthesis from cholesterol.

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Cardiovascular Disease

[In Vivo]

Colestyramine (Cholestyramine) is a bile acid binding resin and can inhibit intestinal bile acid absorption which results in the increasing bile acid synthesis from cholesterol[1]. Results reveal that GSPE treatment alone, and co-administration with Colestyramine (CHY), regulate BA, cholesterol and TG metabolism differently compare to Colestyramine (CHY) administration alone. Notably, GSPE decreases intestinal apical sodium-dependent bile acid transporter (Asbt) gene expression, while Colestyramine (CHY) significantly induces expression. Administration with GSPE or Colestyramine (CHY) robustly induces hepatic BA biosynthetic gene expression, especially cholesterol 7α-hydroxylase (Cyp7a1), compare to control, while co-administration further enhances expression. Treatment with Colestyramine (CHY) induces both intestinal and hepatic cholesterologenic gene expression, while co-administration with GSPE attenuates the Colestyramine (CHY)-inducing increase in the liver but not in the intestine. Colestyramine (CHY) also induces hepatic lipogenic gene expression, which is attenuated by co-administration with GSPE[2].

[Animal admin]

Mice are purchased at 7 weeks of age and allowed to acclimate for one week. At 8-weeks of age the mice are given either a control or a 2% Colestyramine (cholestyramine)-supplementing diet for 4 weeks (n=18 per group). Body weight for each mouse is recorded weekly. After 4 weeks, the mice in each group are randomly assigned to one of two treatment groups and orally gavaged with either vehicle (water) or GSPE (250 mg/kg) and terminated 14 hours later (n=9 per experimental group). The four treatment groups are as follows: 1. CON: Control diet for 4 weeks following by oral gavage with vehicle (water) for 14 hrs; 2. GSPE: Control diet for 4 weeks following by oral gavage with 250 mg/kg GSPE for 14 hrs; 3.CHY Colestyramine (cholestyramine): 2% Colestyramine (cholestyramine)-supplementing diet for 4 weeks following by oral gavage with vehicle for 14 hrs; and 4. CHY Colestyramine (cholestyramine)+GSPE: 2% cholestyramine-supplementing diet for 4 weeks following by oral gavage with 250 mg/kg GSPE for 14 hrs. Blood is collected from the orbital plexus under isoflurane anesthesia, and intestines and livers are snap-frozen in liquid nitrogen and stored at -80°C until use. At the start of the 14 hr experiment mice are placed into clean cages, and feces are manually collected at the end of the study[2].

[References]

[1]. Maugeais C, et al. rHDL administration increases reverse cholesterol transport in mice, but is not additive on top of ezetimibe or cholestyramine treatment. Atherosclerosis. 2013 Jul;229(1):94-101.

[2]. Rebecca M. Heidker, et al. Grape Seed Procyanidins and Cholestyramine Differentially Alter Bile Acid and Cholesterol Homeostatic Gene Expression in Mouse Intestine and Liver. PLoS One. 2016; 11(4): e0154305.

[Related Small Molecules]

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₃₀ClN

[ Molecular Weight ]:
331.923

[ Exact Mass ]:
331.206665

[ Water Solubility ]:
Insoluble in water, in methylene chloride and in ethanol (96 per cent).

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Hazard Codes ]:
Xi

[ Safety Phrases ]:
S22-24/25

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
2

[ RTECS ]:
FZ9310000

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