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Long-lasting smooth...
Long-lasting smooth-muscle relaxation by a novel PACAP analogue in human bronchi
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Yoshihara, S. (author)
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Yamada, Y. (author)
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Abe, T. (author)
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Kashimoto, K. (author)
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- Lindén, Anders, 1961 (author)
- Gothenburg University,Göteborgs universitet,Institutionen för invärtesmedicin, Avdelningen för lungmedicin och allergologi,Institute of Internal Medicine, Dept of Respiratory Medicine/Allergology
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Arisaka, O. (author)
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(creator_code:org_t)
- 2004
- 2004
- English.
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In: Regul Pept. ; 123:1-3
- Related links:
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https://gup.ub.gu.se...
Abstract
Subject headings
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- We compared the relaxant effect of original pituitary adenylate cyclase-activating peptide (PACAP)1-27 with that of a newly developed, synthetic PACAP1-27 analogue, [Arg(15,20,21) Leu(17)]-PACAP-Gly-Lys-Arg-NH(2), in human bronchi in vitro (n=4-5 in each group). Using precontraction by carbachol (0.1 muM), cumulative administration of PACAP1-27 and salbutamol caused concentration-dependent smooth muscle relaxation with similar potencies and maximum relaxant effects. Non-cumulative administration of the PACAP1-27 analogue and the original PACAP1-27 caused concentration-dependent relaxation with a similar maximum relaxant effect and potency as well. However, the onset and offset of action was markedly slower for the PACAP1-27 analogue than for the original PACAP1-27 (>90% versus <10% of peak relaxation remaining 5 h after administration). Peptidase inhibition by captopril (10 muM) and phosphoramidon (1 muM) significantly increased the maximum relaxant effect and duration of action of PACAP1-27 but not of the PACAP1-27 analogue, during the 3 h of observation in the human bronchi. We conclude that [Arg(15,20,21) Leu(17)]-PACAP-Gly-Lys-Arg-NH(2) produces significant concentration-dependent and sustained bronchial smooth muscle relaxation in vitro. The sustained relaxant effect is due, at least in part, to the synthetic PACAP1-27 analogue being less susceptible to cleavage by peptidases than the original peptide PACAP1-27.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Lungmedicin och allergi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Respiratory Medicine and Allergy (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
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