期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 47, 期 12, 页码 2969-2972出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm0342358
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资金
- NIDA NIH HHS [DA 015091, DA 01533] Funding Source: Medline
In view of recent pharmacological studies suggesting the existence of delta-kappa opioid receptor heterodimers/oligomers in the spinal cord, we have synthesized and evaluated (intrathecally in mice) a series of bivalent ligands (KDN series) containing kappa and delta antagonist pharmacophores. Pharmacological and binding data have provided evidence for the bridging of spinal delta-kappa receptor heterodimers by KDN-21 and for their identification as delta(1) and kappa(2). The selectivity profile of KDN-21 and the apparent absence of coupled delta(1)-kappa(2) phenotypes in the brain suggest a new approach for targeting receptors.
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