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Biomedical subjects

J Carlsen

Publications and source records attributed to J Carlsen.

58 records · Page 4Linked to original sources

Structure-function studies on red pigment-concentrating hormone, II. The significance of the C-terminal tryptophan amide.

The significance of the C-terminal tryptophan residue of the red pigment-concentrating hormone (RPCH: Glu-Leu-Asn-Phe-Ser-Pro-Gly-Trp-NH2) regulating the blanching of the crustacean chromatophores has been investigated. RPCH and a number of analogues that differ only in the C-terminal part of the hormone, have been synthesized and assayed for biological activity on the shrimp Leander adspersus. It has been shown that the indole skeleton of tryptophan is an absolute requirement for the biological activity of the hormone. To provide maximum response the tryptophan must be blocked as the amide. The activity of synthetic [Tyr4]RPCH and adipokinetic hormone (AKH) purified from Schistocerca gregaria has been compared with the activity of synthetic RPCH.

Amides↗

Structure-function studies on red pigment-concentrating hormone; the significance of the terminal residues.

The significance of the terminal residues of the red pigment-concentrating hormone (RPCH: Glu-Leu-Asn-Phe-Ser-Pro-Gly-Trp-NH2) for its blanching effect on crustacean chromatophores has been investigated. The chemical synthesis of the following small analogues, starting from the C-terminal amino acid are described: Ac-Trp-NH2, Boc-Gly-Trp-NH2, Ac-Gly-Trp-NH2, Gly-Trp-NH2, Ac-Pro-Gly-Trp-NH2, Glu-Trp-NH2, Glu-Pro-Gly-Trp-NH2, Ac-Pro-Gly and Glu-Pro-Gly-NH2. Assay of the biological activity of the various synthetic compounds in the shrimp Leander adspersus has established that only the C-terminal tryptophan residue is indispensable for the blanching effect of the hormone, although elongation of the chain length improves its potency.

Animals↗

N"-Cyano-N-4-pyridyl-N'-1,2,2-trimethyl-propylguanidine, a new vasodilating agent: acute effect of blood pressure and pharmacokinetics in hypertensive patients.

N"-Cyano-N-4-pyridyl-N'-1,2,2-trimethylpropylguanidine (P 1134) is a new vasodilating antihypertensive compound. In an open study, P 1134 was given in single oral doses of from 10 to 25 mg to 12 previously untreated patients with essential hypertension. All patients responded with decreases in mean arterial pressure (MAP) of at least 10 mm Hg and with almost equal blood pressure decreases in the supine and erect position. The increase of dose was significantly correlated with a progressive reduction of blood pressure. At a dose of 25 mg, the maximal decrease in supine MAP averaged 38 mm Hg, and the maximal increase in heart rate averaged 23 beats/min. Peak effect and serum concentration were seen about 1 h after tablet intake. The serum half-life from the peak concentration averaged 2.5 h. It is concluded that P 1134 is a fast-acting, effective antihypertensive agent.

Adult↗