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August 1, 1977Canadian Journal of Physiology and Pharmacology

Receptors for bradykinin in rabbit aortae

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Authors

DRD. RegoliUniversity of SienaJBJ. BarabéUniversité de SherbrookeWPW. K. Park

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Implication

Pharmacological study reveals distinct bradykinin receptor subtypes in rabbit aorta, indicating a unique contractile receptor mechanism.

Key Points

  • To characterize the pharmacological properties and structure–activity relationships of bradykinin receptors mediating contractions in rabbit aorta.
  • Assayed isolated rabbit aorta strips with bradykinin, octapeptide fragment (1-8 BK), and synthetic analogues.
  • Treated tissues with phentolamine, methysergide, mepyramine, 8-Leu-AT II, and indomethacin to confirm response specificity.
  • Calculated dose–response curves, agonist affinities (pD2), and antagonist affinities (pA2).
  • The octapeptide 1-8 BK exhibited higher potency than native bradykinin (pD2 = 7.19 vs. pD2 = 6.40), showing that 8-Phe is critical for receptor activation.
  • Substituting 8-Phe with aliphatic residues generated competitive antagonists, including 8-Leu-Octa (pA2 = 6.75) and 8-Leu-OMe-Octa (pA2 = 6.66), with pA2 – pA10 values near 0.95.
  • The unique pharmacological profile confirmed a novel bradykinin receptor distinct from classical receptors identified in intestinal and uterine tissues.

Cite This Study

Regoli et al. (1977) studied this question.

synapsesocial.com/papers/6a70d827439bab0cabc359c4https://doi.org/10.1139/y77-115
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Also Consider

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  5. 5Angiotensin-converting enzyme, bradykinin, angiotensin, and cerebral vessel reactivity.1983 · 24 citations