Abstract
1 In this study, [(3)H]GR205171 (3(S)-(2-methoxy-5-(5-trifluoromethyltetrazol-1-yl)-phenylmethylamino)-2(S)-phenylpiperidine), a potent and selective NK1 receptor antagonist, was characterised in autoradiographic studies in gerbil brain and in binding experiments on homogenates from gerbil and human brain cortex and striatum. 2 In autoradiographic studies in gerbil brain, highest levels of [(3)H]GR205171 binding sites were observed in caudate putamen, nucleus accumbens, medial and cortical nuclei of the amygdala and intermediate levels were detected in the hypothalamus, basolateral amygdala, septum, and cortex. 3 Saturation experiments in homogenates of brain striatum from gerbil showed that [(3)H]GR205171 binds to a single receptor population with a pK(d) value of 10.8+/-0.2 and a B(max) value of 607+/-40 fmol mg(-1). A lower number of NK1 receptor sites was found in cortex, where a B(max) of 94+/-6 fmol mg(-1) protein was obtained. Saturation experiments performed on homogenates from brain striatum of two human subjects and brain cortex of three human subjects showed that [(3)H]GR205171 binds with pK(d) values not different from gerbil and B(max) values ranging from 318+/-51 to 432+/-27 fmol mg(-1) protein in striatum and fro...Continue Reading
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