caa a22 4500 469079940 CHVBK 20180323132947.0 cr unu---uuuuu 170328e19920201xx s 000 0 eng 10.1007/BF00165736 doi (NATIONALLICENCE)springer-10.1007/BF00165736 Pharmacological comparison of the sigma recognition site labelled by [3H]haloperidol in human and rat cerebellum [Elektronische Daten] [J. Barnes, N. Barnes, P. Barber, S. Champaneria, B. Costall, C. Hornsby, J. Ironside, R. Naylor] Summary: The radioligand binding characteristics of [3H]haloperidol (in the presence of spiperone, 25 nmolL−1) were investigated in rat and human cerebellar membranes. In both rat and human cerebellar membrane preparations saturation studies with [3H]haloperidol (non-specific binding defined by pentazocine, 10 μmolL−1) demonstrated high affinity saturable specific binding to a homogenous population of binding sites (rat, Bmax 6693 ± 1242 fmol mg−1 protein, pKD 8.33 ± 0.08; human, Bmax 2550 ± 437 fmol mg−1 protein, pKD 8.59 ± 0.11; mean ± SEM, n = 3-6). Competition studies employing a wide range of structurally diverse competing compounds displayed that the [3H]haloperidol binding site was pharmacologically similar in both preparations and comparable to sigma recognition sites previously identified in various tissues originating from different species. In addition, with reference to the potential subtypes of sigma recognition sites, the labelling of these sites by low nanomolar concentrations of [3H]haloperidol provides evidence that they belong to the sigma-1 recognition site subtype. The present findings suggest that the pharmacology of the rat and human cerebellar sigma recognition site are directly comparable and provides further supporting evidence towards the use of [3H]haloperidol radioligand binding studies in the rat to detect sigma receptor ligands with potential therapeutic activity. Springer-Verlag, 1992 Sigma recognition sites nationallicence Human cerebellum nationallicence Rat cerebellum nationallicence [3H]haloperidol nationallicence Barnes J. Department of Pharmacology, The Medical School, University of Birmingham, B15 2TT, Edgbaston, Birmingham, UK aut Barnes N. Department of Pharmacology, The Medical School, University of Birmingham, B15 2TT, Edgbaston, Birmingham, UK aut Barber P. Department of Pathology, The Medical School, University of Birmingham, B15 2TT, Edgbaston, Birmingham, UK aut Champaneria S. Postgraduate Studies in Pharmacology, The School of Pharmacy, University of Bradford, BD7 1DP, Bradford, West Yorkshire, UK aut Costall B. Postgraduate Studies in Pharmacology, The School of Pharmacy, University of Bradford, BD7 1DP, Bradford, West Yorkshire, UK aut Hornsby C. Postgraduate Studies in Pharmacology, The School of Pharmacy, University of Bradford, BD7 1DP, Bradford, West Yorkshire, UK aut Ironside J. The Neuropathology Laboratory, Department of Pathology, Western General Hospital, Crewe Road, EH4 2XU, Edinburgh, UK aut Naylor R. Postgraduate Studies in Pharmacology, The School of Pharmacy, University of Bradford, BD7 1DP, Bradford, West Yorkshire, UK aut Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 345/2(1992-02-01), 197-202 0028-1298 345:2<197 1992 345 210 https://doi.org/10.1007/BF00165736 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF00165736 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Barnes J. Department of Pharmacology, The Medical School, University of Birmingham, B15 2TT, Edgbaston, Birmingham, UK aut NATIONALLICENCE 700 1- Barnes N. Department of Pharmacology, The Medical School, University of Birmingham, B15 2TT, Edgbaston, Birmingham, UK aut NATIONALLICENCE 700 1- Barber P. Department of Pathology, The Medical School, University of Birmingham, B15 2TT, Edgbaston, Birmingham, UK aut NATIONALLICENCE 700 1- Champaneria S. Postgraduate Studies in Pharmacology, The School of Pharmacy, University of Bradford, BD7 1DP, Bradford, West Yorkshire, UK aut NATIONALLICENCE 700 1- Costall B. Postgraduate Studies in Pharmacology, The School of Pharmacy, University of Bradford, BD7 1DP, Bradford, West Yorkshire, UK aut NATIONALLICENCE 700 1- Hornsby C. Postgraduate Studies in Pharmacology, The School of Pharmacy, University of Bradford, BD7 1DP, Bradford, West Yorkshire, UK aut NATIONALLICENCE 700 1- Ironside J. The Neuropathology Laboratory, Department of Pathology, Western General Hospital, Crewe Road, EH4 2XU, Edinburgh, UK aut NATIONALLICENCE 700 1- Naylor R. Postgraduate Studies in Pharmacology, The School of Pharmacy, University of Bradford, BD7 1DP, Bradford, West Yorkshire, UK aut NATIONALLICENCE 773 0- Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 345/2(1992-02-01), 197-202 0028-1298 345:2<197 1992 345 210 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer