Autoradiographic localization of [125I-Tyr0]bradykinin binding sites in brains of Wistar-Kyoto and spontaneously hypertensive rats.

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Privitera PJ, Beckstead RM, Yates P, Walgren R

Autoradiographic localization of [125I-Tyr0]bradykinin binding sites in brains of Wistar-Kyoto and spontaneously hypertensive rats.

Cell Mol Neurobiol. 2003 Oct;23(4-5):805-15.

PubMed ID

14514033 [ View in PubMed

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Abstract

1. The present study was undertaken to localize and characterize bradykinin (BK) binding sites in brains from Wistar-Kyoto (WKY) and spontaneously hypertensive rats (SHR). 2. Serial sections of brains were cut from adult WKY and SHR and specific [125I-Tyr0]bradykinin ([125I-Tyr0]BK) binding was determined using in vitro quantitative receptor autoradiographic techniques. 3. Specific binding of [125I Tyr0]BK was localized in the medulla oblongata to the regions of the nucleus of the solitary tract (NTS), area postrema (AP), dorsal motor nucleus of the vagus (X), and caudal subnucleus of the spinal trigeminal nucleus in both strains of rat. The specific binding (85-90% of total binding) was of high affinity and saturable with KD values in the range of 100 pM and a B(max) of 0.75 fmol per mg tissue equivalent in the NTS-X-AP complex of both the WKY and SHR. In competition studies, the rank order of potencies was similar in both strains with BK = Lys-BK > icatibant >>> DesArg9-BK. The B2 receptor antagonist icatibant inhibited [125I-Tyr0]BK binding with a Ki value of 0.63 +/ 0.19 nM in WKY and 0.91 +/- 0.73 nM in SHR, while Ki values for the B1 receptor agonist DesArg9-BK were 1475 +/- 1055 and 806 +/-362 nM in WKY and SHR, respectively. 4. Our finding of specific high-affinity [125I-Tyr0]BK B2 binding sites in the NTS, AP, and the X of WKY and SHR is important because these brain areas are associated with central cardiovascular regulation. However, alterations in BK B2 receptors in the medulla that could contribute to the hypertensive state in the SHR were not detected.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Icatibant	B2 bradykinin receptor	Protein	Humans	Yes	Antagonist	Details