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C Lin

Publications and source records attributed to C Lin.

70 records · Page 4Linked to original sources
PubMedDate not supplied

Cysteinyl methyl ester of AVP(4-8), a potent agonist on the maintenance of passive avoidance in rats.

A series of short AVP analogs with D- or L-arginine forming the C-terminal was synthesized, and their peripheral effects, i.e., vasoconstrictor and antidiuretic activities, and behavioral effects in enhancing retention in passive avoidance in rats were evaluated. We found that: 1) AVP(4-8) and its cysteinyl methyl ester were more potent in the behavioral response than its D-Arg homologs; 2) the methyl ester derivative was the most effective analog in this behavioral test among the peptides we synthesized, with a potency 40 times as high as AVP; 3) neither the D- nor the L-Arg short derivatives of AVP showed any peripheral effects up to a dose thousands of times greater than AVP. The results support the contention that arginine in the short analogs plays an important role in their behavioral response associated with a relatively steady peptide conformation.

Amino Acid Sequence↗
PubMedDate not supplied

Pit-1-dependent expression of the receptor for growth hormone releasing factor mediates pituitary cell growth.

In Snell (dw) and Jackson (dwJ) dwarf mice, mutations in the gene encoding Pit-1, a tissue-specific POU-domain transcription factor, lead to the absence of somatotroph, lactotroph and thyrotroph cells. Pre-somatotroph proliferation is stimulated by increased intracellular levels of cyclic AMP, normally induced by growth hormone releasing factor (GRF; refs 7-17). Here we report the cloning of mouse and rat complementary DNAs encoding a new member of the seven-transmembrane-helix, G-protein-coupled receptor family restricted to the pituitary gland, which mediates increases in intracellular cAMP and cAMP-dependent gene transcription in response to GRF. The receptor is expressed in a spatial and temporal pattern corresponding precisely to growth hormone gene expression, and neither is expressed in dw/dw mice. The pituitary hypoplasia in these mice thus appears to be due, at least in part, to the absence of GRF receptor, which is in turn due to the absence of functional Pit-1.

Amino Acid Sequence↗
PubMedDate not supplied

Correlation of 14C-griseofulvin metabolism in rat liver microsomes, isolated perfused rat livers, and in rats with bile duct cannulas.

The metabolism of 14C-griseofulvin has been compared in rat liver microsomes, isolated perfused rat livers, and rats with bile duct cannulas. In all three preparations, 4-desmethylgriseofulvin and 6-desmethylgriseofulvin were the major metabolites. The ratio of total 4-desmethylgriseofulvin to 6-desmethylgriseofulvin formed was 1.20, 0.89, and 1.01 in liver microsomes, isolated perfused livers, and rats with bile duct cannulas, respectively. After a 7-min incubation with liver microsomes, most (96%) of the griseofulvin remained unchanged. Only small amounts of 4-desmethylgriseofulvin (1.26%) of dose) and 6-desmethylgriseofulvin (1.05% of dose) were formed. In isolated perfused liver, most of the drug (59% of dose) was excreted into bile within 4 hr, primarily as 4-desmethylgriseofulvin (24% of dose) and 6-methylgriseofulvin (24% of dose). In animals with bile duct cannulas, 65% of the dose was excreted into bile and 18% of the dose into urine within 4 hours. In bile, 32% of the dose was excreted as 4-desmethylgriseofulvin and 20% of the dose as 6-desmethylgriseofulvin, whereas in urine the drug was excreated predominantly as 6-desmethylgriseofulvin (13% of dose) with only a small amount of 4-desmethylgriseofulvin (1% of dose), during the first 4 hr. These results show that there is good correlation in the metabolic fate of 14C-griseofulvin in the liver microsomes, isolated perfused liver, and rats with bile duct cannulas. In addition to the similar ratio of 4-desmethylgriseofulvin to 6-desmethylgriseofulvin, there is also an agreement in the extent of metabolism and biliary excretion in isolated perfused liver and in rats with bile duct cannulas, which suggests that the isolated perfused liver is an important technique for studying drug metabolism in animals.

Animals↗
PubMedDate not supplied

Isolation and identification of the major metabolite of albuterol in human urine.

The major urinary metabolite of albuterol in man was isolated and purified by ion-exchange chromatography and countercurrent distribution. On the basis of proton magnetic resonance, infrared, and mass-spectral analysis, enzymic hydrolysis, and assay of inorganic sulfate after acid hydrolysis, the metabolite has been identified as the 4'-O-sulfate ester of albuterol.

Albuterol↗
PubMedDate not supplied

Absorption, metabolism, and excretion of 14C-tosifen in the dog and rat.

14C-tosifen [N-2-(1-phenylpropyl)-N'-p-tolyl sulfonylurea] was readily absorbed in both rats and dogs. The rates of absorption, metabolism, and urinary excretion were higher in the rat than in the dog. More of the drug was excreted via the feces than in the urine of the rat, whereas in the dog, the drug was primarily excreted into the urine. The parent drug was the major radioactive component in the plasma of both species. In the urine, however, only a negligible amount of tosifen was found. The major urinary metabolite was a hydroxymethyl derivative which accounted for about 60% and 40% of the total radioactivity in the urine of the dog and rat, respectively.

Absorption↗