The metabolism of the tumor promoters 120-O-[3H]tetradecanoylphorbol-13-acetate ([3H]TPA) and [3H]phorbol-12,13-didecanoate ([3H]PDD) was analyzed in several cell types in culture. In contrast to the rapid metabolism of [3H]TPA, [3H]PDD was degraded much more slowly in hamster, rat, chick, and mouse fibroblasts. Human fibroblasts did not significantly metabolize either phorbol diester over a th...

The formation and metabolism of inositol pentakis-and hexakisphosphates (InsP5 and InsP6) were investigated in Xenopus laevis oocytes. After [3H]inositol injection, [3H]InsP5 and subsequently [3H]Insp6 increased progressively over 72 h. In intact oocytes, [3H]InsP5 was progressively converted to [3H]InsP6 from 6 to 72 h of incubation and was not metabolized to lower inositol phosphates. In cont...

Previous EM autoradiographic studies have shown that injection of [3H]proline ([3H]Pro) into the cat dorsal column nuclei (DCN) results in heavy labeling of macroglia but negligible labeling of DCN neurons. [3H]Leucine ([3H]Leu), in contrast, was extensively incorporated into both neurons and glia. We now report preliminary assessment of differences in molecular labeling patterns produced by th...

[3H]Squalene 2,3(S);22(S),23-dioxide was prepared by incubation of [3H]mevalonate with S10 rat liver homogenate in the presence of 4,4,10 beta-trimethyl-trans-decal-3 beta-ol, a specific inhibitor of oxidosqualene cyclase (EC 5.4.99.7). Aerobic incubation of [3H]squalene 2,3(S);22(S),23-dioxide with S10 rat liver homogenate affords 24(S),25-epoxycholesterol with an efficiency comparable to that...

To obtain drugs which are more selective at benzodiazepine (BZD) receptors, design and synthesis of functionally selective ligands for BZD receptors is the current strategy of our pharmaceutical chemistry department. The affinity of newly synthesized ligands is assessed by radioligand receptor binding assays. Based on our previous studies, 2-phenyl-5-oxo-7-methyl-1,3,4-oxadiazolo[a,2,3]-pyrimid...

The biosynthesis of tRNA was investigated in cultured astroglial cells and the 3-day-old rat brain in vivo. In the culture system astrocytes were grown for 19 days and were then exposed to [3H]guanosine for 1.5-7.5 h; 3-day-old rats were injected with [3H]guanosine and were killed 5-45 min later. [3H]tRNA was extracted, partially purified, and hydrolyzed to yield [3H]guanine and [3H]methyl guan...

In the presence of a 30 nM prazosin mask, [3H]-2-(2,6-dimethoxyphenoxyethyl) aminomethyl-1,4-benzodioxane ([3H]WB4101) can selectively label 5-HT1 serotonin receptors. Serotonin exhibits high affinity (Ki = 2.5 nM) and monophasic competition for [3H] WB4101 binding in cerebral cortex. Furthermore, we have found a significant correlation (r = 0.96) between the affinities of a number of serotoner...

[20-3H]Phorbol 12,13-dibutyrate ([3H]PDBU) and [20-3H]phorbol 12-myristate 13-acetate ([3H]PMA) bound specifically and with high affinity to one class of saturable binding sites in particulate preparations from mouse brain. The dissociation constants for binding of [3H]PDBU and [3H]PMA were 7 nw and 66 PM, respectively. At half-maximal specific binding, binding of [3H]PDBU was 96% specific and ...

To understand the signaling and growth-inhibitory effects of retinoids, we have examined the metabolism of [3H]retinol in a number of estrogen receptor-positive (ER+) and estrogen receptor-negative (ER-) human breast cancer cell lines. We have also assayed the metabolism of [3H]retinol in normal human mammary epithelial cells. The ER+ breast cancer cell lines MCF-7 and T47D produce [3H]4-oxoret...

Occurrence of emerging organic micropollutants in water bodies and their effects are a concern related to quality reused water. Advanced oxidation processes have demonstrated promising results address this challenge. Nonetheless, these may lead the generation more toxic by-products. The aim study was investigate coupling ozonation nanofiltration (NF) applied carbamazepine (CBZ). It consisted mo...