-
Benzodiazepines that bind at peripheral sites inhibit cell proliferation.
[3H]Ro5-4864 binds to mouse thymoma cells in a specific, saturable, and reversible manner. Scatchard analysis shows a single class of binding sites with a Kd of 4.4 nM and a Bmax of 477 fmol per 10(6) cells. This benzodiazepine binding site is of the peripheral type, based on the relative potencies of Ro5-4864 and clonazepam in competing for [3H]diazepam binding. Fifteen benzodiazepines that bind to this site with affinities ranging from 6 nM to 1 microM also reversibly inhibit the proliferation of thymoma cells in culture at the micromolar dose range. There is a strong positive correlation (r = 0.85) between the binding constants of these compounds for the peripheral-type sites and their ED50 in inhibiting the uptake of [3H]thymidine into the cells. These sites may be involved in the regulation of thymoma cell proliferation.
PMID: 6322168 [PubMed - indexed for MEDLINE]
PMCID: PMC344914
-
Cited by 11 PubMed Central articles
-
ReviewTranslocator protein 18 kDa (TSPO): molecular sensor of brain injury and repair.
Chen MK, Guilarte TR.
Pharmacol Ther. 2008 Apr; 118(1):1-17. Epub 2008 Feb 9.
[Pharmacol Ther. 2008]
-
Immunomodulating effects of tofizopam (Grandaxin) and diazepam in vitro.
Kalashnikov SV, Kalashnikova EA, Kokarovtseva SN.
Mediators Inflamm. 2002 Feb; 11(1):53-9.
[Mediators Inflamm. 2002]
-
Tumor selective G2/M cell cycle arrest and apoptosis of epithelial and hematological malignancies by BBL22, a benzazepine.
Xia W, Spector S, Hardy L, Zhao S, Saluk A, Alemane L, Spector NL.
Proc Natl Acad Sci U S A. 2000 Jun 20; 97(13):7494-9.
[Proc Natl Acad Sci U S A. 2000]
- » See all...
Patient Drug Information
-
Diazepam (Diazepam Intensol® , Valium® )
Diazepam is used to relieve anxiety, muscle spasms, and seizures and to control agitation caused by alcohol withdrawal.
-
Clonazepam (Klonopin® )
Clonazepam is used alone or in combination with other medications to control certain types of seizures. It is also used to relieve panic attacks (sudden, unexpected attacks of extreme fear and worry about these attacks)....