Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027960 (mole)
 21,279 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Substance P (6.25-25 p-mole) produced dose-dependent flare and wheal responses when injected intradermally into the volar surface of the human forearm. The maximum flare response was obtained within the first 3 min of injection and declined thereafter. The wheal response reached a maximum after 12 min following the injection. Only those peptides having one or more basic residues in the N-terminal region were effective in producing a flare reaction. Eledoisin-related peptide and SP1-9 were 17 and 7 times less active than substance P respectively, whilst [D-pro2, D-phe7, D-trp9]SP1-11 was twice as active. The N-terminal tetrapeptide, SP1-4 and eledoisin were inactive in the dose range tested. Wheal-producing activity was not dependent on the presence of basic residues and the rank order of relative potencies was: physalaemin (2.0): [D-pro2, D-phe7, D-trp9]SP1-11 (1.1): SP1-11 (1.0): SP4-11 (0.4): SP1-9 (0.15): eledoisin-related peptide (0.08): eledoisin (0.06). The N-terminal tetrapeptide failed to produce a wheal response in the dose range tested. Substance P was approximately equi-active with poly-L-arginine in the production of wheal and flare and both of these agents were about 10 times more potent than histamine. Adenosine triphosphate (25-400 n-mole) produced dose-dependent wheal and flare responses and was 10,000 times less potent than substance P. Pre-treatment of the subjects with the H1 histamine antagonist, chlorpheniramine, (20 mg I.V.) reduced the wheal and flare responses to substance P. Local anaesthetic injection into the skin reduced the spread of the flare response but did not affect the development of the wheal response. Pre-treatment of the skin with capsaicin reduced the flare but not the wheal response to intradermal injection of histamine. The results are discussed in relation to the mechanism of the 'axon reflex' vasodilatation in skin. This is thought to involve mast cells in addition to substance P-containing primary afferent neurones.
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PMID:Structure-activity relationships for some substance P-related peptides that cause wheal and flare reactions in human skin. 619 37

Direct capillary zone electrophoretic methods were developed for the separation of the enantiomers of unnatural beta-methyl-amino acids such as erythro- and threo-beta-methylphenylalanine, beta-methyltyrosine, beta-methyltryptophan and beta-methyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid. Capillary zone electrophoresis was carried out using sulfopropylated-alpha-CD (SP2-alpha-CD), sulfopropylated-beta-CD (SP2-beta-CD) both with a degree of substitution of 2 moles/mole cyclodextrin, and sulfopropylated-beta-CD (SP4-beta-CD) with a degree of substitution of 4moles/mole beta-cyclodextrin. The effects of selector and buffer concentrations, electrolyte pH and applied voltage were studied on the separation efficiency. Varying the electrophoretic conditions with application of 20 kV, hydrodynamic injection, unmodified silica capillary, three different buffers (borate, phosphate and acetate) and modified cyclodextrins as chiral selectors all compounds investigated are nearly baseline resolved. The elution sequence was determined in most cases.
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PMID:Enantioseparation of beta-methyl-substituted amino acids with cyclodextrins by capillary zone electrophoresis. 1851 44

Direct capillary zone electrophoretic methods were developed for the separation of the enantiomers of unnatural beta-substituted tryptophan analogues such as erythro- and threo-beta-methyl-, beta-2-propyl-, beta-3-pentyl-, beta-phenyl- and beta-2,5-dimethoxyphenyltryptophan. Cyclodextrins (CDs) were chosen as chiral selectors because of their favorable properties (stability, commercial availability, low cost, UV transparency, inertness, etc.). Capillary zone electrophoresis was carried out using sulfopropylated-alpha-CD (SP2-alpha-CD), sulfopropylated-beta-CD (SP2-beta-CD) both with a degree of substitution of 2moles/mole cyclodextrin, and sulfopropylated-beta-CD (SP4-beta-CD) with a degree of substitution of 4moles/mole beta-cyclodextrin. With this technique all compounds investigated are baseline resolved using different background electrolytes and chiral additives. The elution sequence was determined in all cases.
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PMID:Enantioseparation of beta-substituted tryptophan analogues with modified cyclodextrins by capillary zone electrophoresis. 1921 27