Uses
Tesmilifene fumarate (DPPE fumarate), an H1C receptor antagonist, potentiates a wide range of cytotoxics and even to offer some protection of normal cells[1][2].
Biological Activity
Binds with high affinity to the antiestrogen binding site but not to the estrogen receptor. An inhibitor of histamine binding at the intracellular histamine (H lc ) site.
in vivo
Tesmilifene (DPPE, 20 mg/kg (s.c.) and 20 μg (icv in 5 μL)) potentiated seizures induced by both convulsants[2].
| Animal Model: | Male BKTO mice (25-45 g)[2]. |
| Dosage: | 20 mg/kg (s.c.) and 20 μg (icv in 5 μL). |
| Administration: | S.C. and icv. |
| Result: | Potentiated seizures induced by both convulsants. |
References
[1] Mark Vincent, et al. Tesmilifene may enhance breast cancer chemotherapy by killing a clone of aggressive, multi-drug resistant cells through its action on the p-glycoprotein pump. Med Hypotheses. 2006;66(4):715-31. DOI:
10.1016/j.mehy.2005.11.005[2] G Sturman, et al. Modulation of the intracellular and H3-histamine receptors and chemically-induced seizures in mice Agents Actions. 1994 Jun;41 Spec No:C68-9. DOI:
10.1007/BF02007771
