Specific 125I-endothelin-1 (125I-ET-1) binding sites were investigated in the rat eye, using receptor autoradiographic techniques. 125I-ET-1 was specifically bound to the rat eye sections, with a slow association rate, as evidenced by kinetic experiments. The radioligand binding reached a maximum at 48hr of incubation and a plateau was maintained for up to 72hr. No degradation of 125I-ET-1 duri...

Receptor-mediated uptake and degradation of 125I-asialoorosomucoid (ASOR) in human hepatoma HepG2 cells is inhibited by the lysosomotropic amines chloroquine and primaquine. In the absence of added ligand at 37 degrees C, these amines induce a rapid (t1/2 5.5-6 min) and reversible loss of cell surface 125I-ASOR binding sites as well as a rapid decrease in 125I-ASOR uptake and degradation. There...

Benztropine and its analogs are tropane ring-containing dopamine uptake inhibitors that produce behavioral effects markedly different from cocaine and other dopamine transporter blockers. We investigated the benztropine binding site on dopamine transporters by covalently attaching a benztropine-based photoaffinity ligand, [125I]N-[n-butyl-4-(4"'-azido-3"'-iodophenyl)]-4', 4"-difluoro-3alpha-(di...

Poly(ethylene glycol), or PEG, conjugation to proteins and peptides is a growing technology used to enhance efficacy of therapeutics. This investigation assesses pharmacodynamic and pharmacokinetic characteristics of PEG-conjugated [D-Pen2,D-Pen5]-enkephalin (DPDPE), a met-enkephalin analog, in rodent (in vivo, in situ) and bovine (in vitro) systems. PEG-DPDPE showed increased analgesia (i.v.) ...

In the chicken, maternal IgG is deposited in the oocyte yolk and subsequently transported intact by the foetal chick yolk sac into the chick circulation. Such transport appears to require a specific membrane-localized IgG receptor. Using the assay of 125I-yolk IgG binding, we have investigated the existence and properties of such receptors in yolk sac tissue disks. We find that: (1) There are s...

A 40-year-old hypothyroid female who had been treated with synthetic thyroxine was admitted to our hospital in October 1988 due to abnormal liver function tests. She had low serum free triiodothyronine (T3; 2.3 pg/ml) and high serum thyrotropin (TSH; 20.8 microU/ml) concentrations. On the other hand, the serum free thyroxine (FT4) level was inappropriately high, being 2.46 ng/dl. Immune precipi...

BACKGROUND Use a banna mini-pig to set up 125I implantation model, and investigate the consequence of radiation-related impairments. METHODS In present study, 125I seeds were implanted into spinal canal of T13 level of spine in banna mini-pigs. After operation, the pigs were raised up to 8 months, behavior changes were recorded within this period. After 8 months, spinal cords were collected f...

We have been investigating the therapeutic efficacy of the thymidine analog 5-iodo-2'-deoxyuridine (IUdR) when radiolabeled with the Auger electron emitter 125I in rats bearing intrathecal (i.t.) or intracerebral (i.c.) 9L gliosarcoma solid tumors. [125I]IUdR was infused i.t. (via subarachnoid catheters) or intracerebrally over a 5- or 2-day period; equimolar concentrations of [127I]IUdR were i...

Translocation is a necessary and rate-limiting step for diphtheria toxin (DT) cytotoxicity. We have reconstituted DT translocation in a cell-free system using endosomes purified from lymphocytes and have demonstrated this using two different probe/cell systems, which provided identical results: 125I-DT/human CEM cells and 125I-transferrin-DT/mouse BW cells. The cell-free DT translocation proces...