Detail of "70904-56-2"

Reference

Carrier-mediated transport of enkephalins and N-Tyr-MIF-1 across blood-brain barrier

Carrier-mediated transport of enkephalins and N-Tyr-MIF-1 across blood-brain barrier. Banks, William A.; Kastin, Abba J.; Fischman, Alan J.; Coy, David H.; Strauss, Seth L. (Sch. Med., Tulane Univ., New Orleans, LA 70146, USA). Am. J. 99874-39-2 is the cas registry number. This chemical is also mentioned in this article. Physiol., 251(4, Pt. 1), E477-E482 (English) 1986. CODEN: AJPHAP. ISSN: 0002-9513. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) The saturable, carrier-mediated system capable of the brain-to-blood transport of small peptides with an N-terminal tyrosine [60-18-4] was characterized. The rate of disappearance of intraventricularly injected iodinated peptide in the presence or absence of the inhibitor being tested was detd. from formulas based on the residual radioactivity in the brains of mice after decapitation. The injection of 100 nmol/mouse of unlabeled N-Tyr-MIF-1 (TMIF) [77133-61-0] increased the half-time disappearance of 125I-labeled TMIF (ITMIF) in the central nervous system (CNS) from 14.1 to 88.7 min. Tc, a substance transported out of the brain by the same system that transports I, was used as a control; the half-time disappearance of technetium pertechnetate was unaffected by unlabeled TMIF. With 2 related but distinct techniques, the max. transport rate (Vmax) out of the central nervous system (CNS) for TMIF was 0.266 nmol/g of brain/min (method 1) and 0.297 nmol/g/min (method 2), whereas the amt. of unlabeled material needed to achieve 50% of Vmax (Km) was 15.2 nomol/g (method 1) and 15.1 nmol/g (method 2). The lack of effect of the tyrosinated fragments of TMIF as inhibitors indicates that TMIF is being transported in intact form. The Vmax for methionine-enkephalin [58569-55-4] detd. with labeled and unlabeled methionine enkephalin was 0.630 nmol/g/min and the Km was 24.95 nmol/g. Studies with the metabolic modulators furosemide, acetozolamide, reserpine, ouabain, and theophylline suggest that the system is Na dependent and probably independent of ATPase. Of the naturally occurring peptides with an N-terminal tyrosine residue, TMIF, the enkephalins, and b-casomorphin [79805-24-6], but not kyotorphin [70904-56-2], porcine dynorphin A [80448-90-4], b-endorphin [60617-12-1], or dermorphin [77614-16-5] could inhibit the transport of ITMIF out of the CNS. Leucine [61-90-5] caused uncompetitive inhibition of transport, but the amino acid tyrosine was ineffective as an inhibitor. Studies with analogs to these substances confirmed the necessity of an N-terminal L-tyrosine for transport and suggested an ideal size range of 4-8 amino acids. .

Synthesis and activity of kyotorphin and its analogs

Synthesis and activity of kyotorphin and its analogs. Balaspiri, Lajos; Kovacs, Kalman; Gecse, Arpad; Telegdy, Gyula; Neubert, Klaus (Inst. Med. Chem., Med. Sch., Szeged, Hung. 88263-56-3 and 88263-64-3 are cas registry numbers. These chemicals are also mentioned in this article.). Pept., Proc. Eur. Pept. Symp., 17th, Meeting Date 1982, 487-93. Edited by: Blaha, Karel; Malon, Petr. de Gruyter: Berlin, Fed. Rep. Ger. (English) 1983. CODEN: 50GFAA. DOCUMENT TYPE: Conference CA Section: 1 (Pharmacology) The analgesic effect of kyotorphin (I) [70904-56-2] and its analogs [synthesis described in detail, Balaspiri (1982)] was examd. in mice. Fifteen analogs had similar and(or) greater activity than I, some with a long-lasting action. Analgesia induced by some of the compds. was antagonized by naloxone. The analgesic activity of radiolabeled I was also studied. .