Chlorcyclizine

Research use only, not for human use.

CHLORCYCLIZINE is a histamine H1 antagonist and a potent hepatitis C virus (HCV) entry inhibitor.

CHLORCYCLIZINE is a histamine H1 antagonist and a potent hepatitis C virus (HCV) entry inhibitor.(In Vivo):Pregnant rats were administered 30, 60, or 90 mg/kg CHLORCYCLIZINE on Gestation Days 11 to 14. Fetal palate gene expression was also assessed after 90 mg/kg CHLORCYCLIZINE at 8, 15 and 30 hours post-dose on Gestation Day 14 using microarray and qRT-PCR. Rats in the 60- and 90-mg/kg groups exhibited adverse clinical signs and body weight loss. Rats in the 90-mg/kg group also demonstrated increases in late resorptions and decreases in fetal weight. Effects in the low-dose group were limited to decreases in body weight gain. Fetal assessment on Gestation Day 21 revealed that findings were limited to the 60- and 90-mg/kg groups, and included cleft palate (80% of litters for both groups), high arched palate, small nose, micrognathia, high domed head, digits shortened/absent and small limb. The fetal incidence of cleft palate was higher at 90 mg/kg, thus this dose was selected to assess palate gene expression. The altered genes associated with CHLORCYCLIZINE-induced cleft palate included Wnt5a, Bmp2, Bmp4, Fgf10, Fgfr2, Msx1, and Insig1 but the magnitude of the change was relatively small (1.5- to 2-fold).

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Pregnant rats administered 30, 60, and 90mg/kg Chlorcyclizine during the sensitive period for palate development survived until scheduled sacrifice on Gestation Days (GDs) 17 or 21. The rats administered 60 or 90mg/kg Chlorcyclizine have transient adverse clinical signs (chromorhinorrhea, red peri-oral substance, urogenital staining, and scant stool) and a concomitant body weight loss of 7% and 11%, respectively, over the dosing interval. Rats administered 30mg/kg Chlorcyclizine do not exhibit any adverse clinical signs, but do not gain weight over the dose interval as would be expected during pregnancy. Based on the testing facility’s historical control database (16 studies, n=380). pregnant rats typically gain about 6% body weight from GDs 12 to 15.

1-((4-chlorophenyl)(phenyl)Methyl)-4-Methylpiperazine

Microbiology/Virology

HCV

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82-93-9

300.83

C18H21ClN2

>98% (HPLC)

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CN(CC1)CCN1C(c1ccccc1)c(cc1)ccc1Cl

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(-20℃)

With Ice Pack

≥ 2 years