Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0406810 (NAME)
 13,345 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Prospidin--N,N3-di(beta-chloroethyl)-N1,N2-dispirotripiperazinium - is a broad-spectrum antineoplastic drug with low toxicity. Experiments on albino rats with transplanted sarcoma M-1 were made to study the distribution and kinetics of 14C-prospidin labeled in the dispirotripiperazinium part of the molecule. On being given intravenously the drug accumulated for 15 minutes. The maximum value of the differential accumulation ratio (CAR) amounted to 3.34 (kidneys) and 0.16 (thymus). The content of the label in organs and tissues was related both to its presence in the blood and to the penetration into the cell structures. The magnitude of the integral indicator in the kidneys, liver, small intestine, bone marrow, lungs and tumor was considerably higher than in other organs. The accumulation of 14C-prospidin mainly by the lung tissue, bronchi, throat and bone marrow enables a correlation to be elucidated between the accumulation and antineoplastic action in the organs under consideration. The presence of the label in different fragments of the 14C-prospidin molecule (14C-dispirotripiperazinium and 14C-hydroxypropyl grouping) made it possible to establish that the DAR for the former label in organs and tissues 3--6 hours after the drug administration was 2--6 times greater than for the latter. As judged from the integral content of the label, prospidin had begun metabolizing and its biological activity decreased by the time indicated.
 ...
PMID:[Pharmacokinetics of the antineoplastic agent 14C-prospidin in rats according to distribution data of the radioactive label]. 730 54

Arhodamine-derived, membrane-permeable fluorophore (DAR-4M AM) sensitive to nitric oxide production has been developed recently. The authors evaluated this reagent in both 96 and 384-well formats using heterologously expressed neuronal nitric oxide synthase (nNOS). nNOS transfected into HEK-293T cells was stimulated by the addition of ionomycin. The calcium mobilization resulting from ionomycin treatment of nNOS-expressing 293T cells induced a robust increase in emission intensity, as measured using a standard rhodamine filter set. The effect was time dependent, and a 3 to 4-fold stimulation could be achieved in a 2-h time period. Ionomycin-dependent nitric oxide (NO) production was completely inhibited by several arginine analogs at micromolar concentrations (e.g., L-NAME IC 50=3.0 micro M). Several arginine analog inhibitors of nNOS were revealed to be differentially reversible over increasing substrate concentrations. The assay is a facile method for characterizing inhibitors of nNOS in a relatively unperturbed cell environment.
 ...
PMID:A homogeneous fluorescent cell-based assay for detection of heterologously expressed nitric oxide synthase activity. 1623 40