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EnglishThe synthesis of cis-(+)- and cis-(-)-N-ethyleneamino-N-nordeoxymetazocine and cis-(-)-N-normetazocine analogues is described and their affinities to sigma (1), sigma (2), and kappa opioid receptors are evaluated. The cis-(+)-deoxy compounds displayed high sigma/kappa selectivity with nanomolar K-i values for sigma (1) receptors, whereas in the cis-(-)-N-normetazocine series the compound (-)-7b was found to bind with nanomolar affinity to the kappa opioid receptor (K-i = 21.5 nM). Compound (-)-7b showed good selectivity for the kappa opioid receptor in comparison to the sigma (1), and sigma (2), sites and to the mu and delta opioid receptors. A correlation of the binding affinities between cis-(-)- and cis-(+)-N-deoxynormetazocine derivatives show that both isomers of the deoxy analogs have similar sigma (1) and sigma (2) binding profiles as the cis-(+)-N-normetazocine derivatives.
| Titolo: | SYNTHESIS AND BINDING AFFINITY OF CIS-(-)- AND CIS-(+)-N-ETHYLENEAMINO-N-NORDEOXYMETAZOCINE AND CIS(-)-N-NORMETAZOCINE ANALOGUES AT SIGMA-1, SIGMA-2 AND KAPPA OPIOID RECEPTORS | |
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| Data di pubblicazione: | 2001 | |
| Rivista: | ||
| Handle: | http://hdl.handle.net/20.500.11769/21278 | |
| Appare nelle tipologie: | 1.1 Articolo in rivista |
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