Characteristics of endothelin binding sites in the spinal cord of spontaneously hypertensive rats

The binding of [125I]sarafotoxin 6b (SRT 6b) and [125I]endothelin-1 (ET-1) to endothelin (ET) receptors of neuronal membranes prepared from cerebral cortex and spinal cord of 8-week-old spontaneously hypertensive rats (SHR) and normotensive Wistar-Kyoto rats (WKY) was determined. SHR had significantly higher blood pressure as compared to WKY. Heart rate was similar in SHR and WKY. [125I]SRT 6b and [125I] ET-1 bound to the membranes of cerebral cortex and spinal cord at a single, high affinity site. The binding of [125I]SRT 6b and [125I]ET-1 in the cerebral cortex and spinal cord membranes was found to be similar in SHR and WKY. Concentration-dependent inhibition of [125I]ET-1 binding in spinal cord membranes by unlabeled ET-1, ET-2 and ET-3 was performed. The Ki values were found to be 2.35 +/- 0.68, 0.29 +/- 0.08 and 24.10 +/- 5.90 nM for ET-1, ET-2 and ET-3, respectively in WKY. The Ki values of ET-1 and ET-2 were found to be similar in WKY and SHR. However, the Ki value of ET-3 were found to be significantly lower (P less than 0.004) in SHR as compared to WKY. Concentration-dependent inhibition of [125I]SRT 6b binding in spinal cord membranes by unlabeled ET-1, ET-2 and ET-3 were also performed. The Ki values were found to be 9.50 +/- 2.10 pM, 0.17 +/- 0.04 nM and 31.20 +/- 6.00 nM for ET-1, ET-2 and ET-3, respectively in WKY. The Ki values of ET-1 and ET-2 were found to be similar in WKY and SHR.(ABSTRACT TRUNCATED AT 250 WORDS)