Abstract:
:In saturation binding experiments, (+)pentazocine, (+)3-(3-hydroxyphenyl)-N-propylpiperidine (3-PPP), haloperidol and rimcazole did not inhibit the binding of [3H]DTG in a purely competitive fashion. Although Scatchard analysis indicated that [3H]DTG bound to a single site, the inhibition curves of some, but not all, reference compounds exhibited Hill coefficients of less than 0.8. The Scatchard data were consistent with a model of hyperbolic competitive inhibition of binding to the [3H]DTG-defined sigma site, although other possibilities such as negative cooperativity or binding to two sites cannot be definitively excluded. Compounds from numerous pharmacological and structural classes inhibited the binding of [3H]DTG, suggesting that interactions of [3H]DTG with other receptors may have confounded the Scatchard analysis of the binding of [3H]DTG to sigma recognition sites.
journal_name
Life Scijournal_title
Life sciencesauthors
DeHaven-Hudkins DL,Fleissner LCdoi
10.1016/0024-3205(92)90255-nsubject
Has Abstractpub_date
1992-01-01 00:00:00pages
PL65-70issue
9eissn
0024-3205issn
1879-0631pii
0024-3205(92)90255-Njournal_volume
50pub_type
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