+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

Characterization of peripheral type benzodiazepine binding sites in human and rat platelets by using [3H]PK 11195. Studies in hypertensive patients

, : Characterization of peripheral type benzodiazepine binding sites in human and rat platelets by using [3H]PK 11195. Studies in hypertensive patients. Biochemical Pharmacology 33(15): 2467-2472

Peripheral type benzodiazepine binding sites have been studied in human and rat platelets and platelet membranes by using PK 11195 (1-(2-chlorophenyl)-N-methyl-N-(1-methyl propyl)-3-isoquinolinecarboxamide) as a ligand. [3H]PK 11195 binding to the intact cells and membranes is saturable, with a high affinity and presents the pharmacological specificity corresponding to the peripheral binding sites (PK 11195 greater than RO5-4864 greater than diazepam greater than clonazepam). [3H]PK 11195 affinity is not affected by cell lysis, but there is a loss of binding capacity, contrarily to RO5-4864 whose affinity is greatly diminished. For this reason [3H]RO5-4864 binding can only be demonstrated in intact cells. Furthermore opposite to RO5-4864, PK 11195 affinity is not decreased by increasing temperatures. No difference was found between binding parameters (KD and Bmax) for [3H]PK 11195 between normotensive and hypertensive subjects. The very high binding capacity of human and rat platelets (Bmax greater than pmole/10(8) cells) makes them a good biological model for studying the physiological significance of "peripheral type" benzodiazepine binding sites.


PMID: 6087829

Other references

Kaneko, M., 1976: Computer tomography and its future role in nuclear medicine. Rinsho Hoshasen. Clinical Radiography 21(12): 1029-1035

Lyubimov, V.; Atakhanov, B.; Bil'-, K., 1987: Adaptation of the photosynthetic apparatus to extreme conditions in plants of the Karakum Desert. Soviet plant physiology (pub 1987) 33(1): 680-686

Mouaz, M.A.; Rashwan, S.M.T.; Hussein, A.M.; Samia, A.A.; Seham, A.S.; Khodeir, M.H., 1995: Rinderpest virus inhibition in vitro by Ribavirin. The effect of the broad spectrum antiviral agent, Ribavirin, was tested against the replication of rinderpest virus (RPV) in bovine kidney cells (BK) as a primary culture and vero cell line culture. Ribavirin showed no effect on growth and viabili...

Hurley, L.; Kelly, L.; Garrow, A.P.; Glynn, L.G.; McIntosh, C.; Alvarez-Iglesias, A.; Avalos, G.; Dinneen, S.F., 2014: A prospective study of risk factors for foot ulceration: the West of Ireland Diabetes Foot Study. This is the first study to examine risk factors for diabetic foot ulceration in Irish general practice. To determine the prevalence of established risk factors for foot ulceration in a community-based cohort, and to explore the potential for estim...

Naja, G.; Fayad, G.; Modine, T.; Decoene, C.; Azzaoui, R.; Larrue, Bît.; Warembourg, H., 2006: Massive pulmonary valve insufficiency associated with double pulmonary artery and ascending aorta aneurysm. A case is reported of aneurysm of both the ascending aorta and pulmonary artery, associated with massive pulmonary valve insufficiency. Pulmonary artery aneurysm is a rare condition of unknown natural history; therapeutic management has not yet be...

Birkhead, G.S.; Riser, M.H.; Mesler, K.; Tallon, T.C.; Klein, S.J., 2006: Youth development is a public health approach. Introduction. Journal of Public Health Management and Practice 1-S3

Anonymous, 2001: Mental health services guide. Who provides what, where: mental health. Health Service Journal 111(5774): Suppl 10-1

Ando K., 1983: Crohns disease affecting the soft palate stomach duodenum and liver in addition to the colon a case. A 16-yr-old boy who had been treated for colonic Crohn's disease was seen with the complaint of a sore throat. Examination showed many vesiculations with surrounding redness on the soft palate and an ulceration at the base of the uvula. These...

Usui, Y.; Kanke, Y.; Mori, Y., 1977: Effects of gonadal hormones on hyaluronic acid content in male mouse skin. Male mice were injected s.c. with several gonadal hormones daily for 5 days to study their effects on hyaluronic acid (HA) content in the skin. Increases in both total hexosamine and HA contents were in the following order: 17.beta.-estradiol (10...

Kelley, J.L.; Suenram, C.A.; Valente, A.J.; Sprague, E.A.; Rozek, M.M.; Schwartz, C.J., 1985: Evolution of foam cells in subcutaneous rabbit carrageenan granulomas. II. Tissue and macrophage lipid composition. This study describes the lipid composition of differentiating macrophage-derived foam cells in the inflammatory carrageenan granuloma. In this model, macrophages exposed in vivo to diet-induced hypercholesterolemia progressively accumulate electro...