Abstract
The study of κ-opioid receptor function in vivo has been hampered by the limited choice of selective κ-antagonists. Recently discovered κ-antagonists have not yet been utilised in vivo. We here report the synthesis and in vitro evaluation of a new amidine derivative of naltrindole. It showed substantially greater κ-selectivity in binding assays than known analogues with shorter spacer in the amidine side chain. This indicates that in nor-BNI and related selective κ-antagonists, the second basic centre may not be ideally located. (C) 2000 Elsevier Science Ltd.
| Original language | English |
|---|---|
| Pages (from-to) | 2259-2261 |
| Number of pages | 3 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 10 |
| Issue number | 20 |
| Early online date | 9 Oct 2000 |
| DOIs | |
| Publication status | Published - 16 Oct 2000 |
Funding
This work was supported by NIDA (OTDP, Division of Treatment Research & Development) Grants DA 00254 and DA 07315 and pharmacological evaluation carried out at SRI under NIDA contract NO1DA.
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry
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