Abstract:
:1,3-di(2-[5-3H]tolyl)Guanidine ([3H]DTG) was found to bind to a single saturable population of binding sites in human cerebral cortex and NCB20 cells, a second low-affinity site was apparent in guinea pig brain. Displacement studies were performed to determine the pharmacology of the [3H]DTG binding site in these 3 membrane preparations. In human cortical tissue and NCB20 cell membranes the (+)-stereoisomers of benzomorphans displaced binding with Hill coefficients close to one, displayed similar affinity and did not give the biphasic displacement curve characteristic of guinea pig membranes. The pIC50 of the low-affinity component of the sigma binding site in guinea pig brain correlates best with the affinity of drugs for the binding site in human cortex.
journal_name
Neurosci Lettjournal_title
Neuroscience lettersauthors
Knight AR,Gillard J,Wong EH,Middlemiss DNdoi
10.1016/0304-3940(91)90621-ysubject
Has Abstractpub_date
1991-10-14 00:00:00pages
233-6issue
2eissn
0304-3940issn
1872-7972pii
0304-3940(91)90621-Yjournal_volume
131pub_type
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