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Träfflista för sökning "WFRF:(Sheykhzade M) "

Search: WFRF:(Sheykhzade M)

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  • Edvinsson, Lars, et al. (author)
  • Differential localization and characterization of functional calcitonin gene-related peptide receptors in human subcutaneous arteries.
  • 2014
  • In: Acta Physiologica. - : Wiley. - 1748-1716 .- 1748-1708. ; 210:4, s. 811-822
  • Journal article (peer-reviewed)abstract
    • Calcitonin gene-related peptide (CGRP) and its receptor are widely distributed within the circulation and the mechanism behind its vasodilation not only differs from one animal species to another but is also dependent on the type and size of vessel. The present study examines the nature of CGRP-induced vasodilation, characteristics of the CGRP receptor antagonist telcagepant and localization of the key components calcitonin receptor-like receptor (CLR) and receptor activity modifying protein 1 (RAMP1) of the CGRP receptor in human subcutaneous arteries.
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3.
  • Sheykhzade, M, et al. (author)
  • Noncompetitive antagonism of BIBN4096BS on CGRP-induced responses in human subcutaneous arteries
  • 2004
  • In: British Journal of Pharmacology. - : Wiley. - 1476-5381 .- 0007-1188. ; 143:8, s. 1066-1073
  • Journal article (peer-reviewed)abstract
    • 1 We investigated the antagonistic effect of 1-piperidinecarboxamide, N-[2-[[5amino-1-[[4-(4-pyridinyl)-1-piperazinyl]carbonyl]pentyl]amino]-1 -[(3,5-dibromo-4-hydroxyphenyl)methyl]-2-oxoethyl]4-(1,4- dihydro-2-oxo-3(2H)-quinazolinyl) (BIBN4096BS) on the calcitonin gene-related peptide (CGRP)-induced responses by using isometric myograph and FURA-2 technique in human subcutaneous arteries removed in association with abdominal surgery. 2 BIBN4096BS, at the concentration of 1 pM, had no significant effect on the CGRP-induced relaxation in these vessels. 3 At the concentration of 10 pM, BIBN4096BS had a competitive antagonistic-like behaviour characterized by parallel rightward shift in the log CGRP concentration-tension curve with no depression of the E-max. 4 At the higher concentrations (0.1 and 1 nM), BIBN4096BS had a concentration-dependent noncompetitive antagonistic effect on the CGRP-induced responses. 5 The efficacy and potency of CGRP was significantly greater in the smaller ( lumen diameter similar to200 mum) human subcutaneous arteries compared to the larger ones. 6 The apparent agonist equilibrium dissociation constant, K-A, for CGRP(1) receptors in the human subcutaneous arteries was approximately 1 nM. Analysis of the relationship between receptor occupancy and response to CGRP indicates that the receptor reserve is relatively small. 7 Using reverse transcriptase-polymerase chain reaction (RT-PCR), the presence of mRNA sequences encoding the calcitonin receptor-like receptor, receptor activity modifying protein (RAMP1, RAMP2, RAMP3) and receptor component protein were demonstrated in human subcutaneous arteries, indicating the presence of CGRP1-like receptor and the necessary component for the receptor activation. 8 In conclusion, the inhibitory action of BIBN4096BS at the low concentration ( 10 pM) on the CGRP-tension curve (but not intracellular calcium concentration ([Ca2+](i)) resembles what is seen with a reversible competitive antagonist. However, at the higher concentrations ( 0.1 and 1 nM), BIBN4096BS acts as a selective noncompetitive inhibitor at CGRP1 receptors in human subcutaneous arteries.
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