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KMID : 0378020080510010023
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New Medical Journal
2008 Volume.51 No. 1 p.23 ~ p.29
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Characterization of Opioid Receptor Binding of Butylthevinones
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Jang Yeon
Chung Eun-Yong
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Abstract
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Background: Opioids have been administered for hundreds of years to allay anxiety and to reduce the pain associated with surgery. The development of pharmacologic agents with the analgesic potency of opioids without adverse effect is anticipated. The purpose of the present study is to investigate the novel centrally-acting analgesic drugs from thebaine derivatives.
Methods: Receptor binding affinity/selectivity of two newly synthesized thebaine derivatives was examined by employing type-selective radiolabelled ligand for μ, δ, κ-opioid receptor.
Result: R-butylthevinone, a newly synthesized thebaine derivative, displaced [3H] DAMGO from opioid μ-receptors, but it showed lower affinity than DAMGO or morphine. This compound displaced [3H] NTI and [3H] U69 binding with higher affinity than morphine. The ratio of affinity to μand other two receptors, δand κ, was 3.1 and 3.4, respectively. S-butylthevinone showed similar binding profile for opioid μ, δ, and κreceptors. This compound showed 8-, 7-, and 4-fold higher affinity for μ, δ, and κreceptor types, respectively. Also, the ratio of affinity to μand other two receptors, δand κ, was greater than R-isomer.
Conclusions: These results showed that butylthevinone can be a potential candidate for the development of novel centrally-acting analgesic drugs.
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KEYWORD
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Brain, Guinea pig, Opioid receptor
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