Peripheral-type benzodiazepine receptors in human cerebral cortex, kidney, and colon
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Cited by (35)
Two populations of TSPO binding sites in oral cancer SCC-15 cells
2017, Experimental Cell ResearchCitation Excerpt :The ligand binds to high affinity sites with a Kd value of 1.40±0.08 nM and a Bmax value of 1586±48 fmoles/mg protein, and to low affinity sites with a Kd value of 61±5 nM and a Bmax value of 26260±1050 fmoles/mg protein. Previous studies reported that the benzodiazepine Ro 5–4864, a ligand specific for TSPO, binds to various mammalian tissues with different affinities: it binds with a high affinity to rat and guinea pig tissues but has very low affinity to TSPO in most calf tissues and in the human cerebral cortex and colon [29,33]. Furthermore, Ro 5–4864 binding characteristics were found to be different in various species; in the cerebral cortex of the dog and cat it bound to a single population of binding sites, however, in rat, guinea pig, rabbit and calf cerebral cortex, it bound to two populations of binding sites, one with high affinity and the other with low affinity [29].
Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO)
2015, European Journal of Medicinal ChemistryCitation Excerpt :One of the earliest and most widely explored TSPO ligands is the quinoline carboxamide PK11195 (1, Fig. 1). The affinity of PK11195 for TSPO is in the nanomolar range in both rat (Ki = 3.0 nM) [16] and human (Ki = 4.5–22.3 nM) [17,18]. Another structural class of high affinity TSPO ligands are the substituted acetanilides typified by DAA1106 (2) [19].
Anti-neuroinflammatory activity of 1,5-benzodiazepine derivatives
2010, Bioorganic and Medicinal Chemistry LettersThe peripheral-type benzodiazepine receptor and the cardiovascular system. Implications for drug development
2006, Pharmacology and TherapeuticsRelation of cell proliferation to expression of peripheral benzodiazepine receptors in human breast cancer cell lines
2000, Biochemical PharmacologyCitation Excerpt :In general, PK 11195, an isoquinoline carboxamide, showed high-affinity binding in tissues from many species [23]. In contrast to rodent PBR (Kd 1–10 nM), binding of Ro5-4864 to PBR of most human tissues occurred only with low affinity (Kd about 1 μM) [23, 24], except for human lymphocytes and platelets [25] and the human breast cancer cell line BT-20 (Kd 8.5 nM) [19]. The present study clearly demonstrates that the ER-positive breast cancer cell lines MCF-7, BT-474, and T47-D possess PBR, but exhibit little specific binding capacity.
Specific binding of benzodiazepines to human breast cancer cell lines
1999, Life Sciences