作者
Gillian M Burgess, Martin N Perkins, Humphrey P Rang, Elizabeth A Campbell, Michael C Brown, Peter McIntyre, Laszlo Urban, Edward K Dziadulewicz, Timothy J Ritchie, Allan Hallett, Christopher R Snell, Roger Wrigglesworth, Wai Lee, Clare Davis, Steve B Phagoo, Andrew J Davis, Elsa Phillips, Gillian S Drake, Glyn A Hughes, Andrew Dunstan, Graham C Bloomfield
发表日期
2000/1
期刊
British journal of pharmacology
卷号
129
期号
1
页码范围
77-86
出版商
Blackwell Publishing Ltd
简介
- Bradyzide is from a novel class of rodent‐selective non‐peptide B2 bradykinin antagonists (1‐(2‐Nitrophenyl)thiosemicarbazides).
- Bradyzide has high affinity for the rodent B2 receptor, displacing [3H]‐bradykinin binding in NG108‐15 cells and in Cos‐7 cells expressing the rat receptor with KI values of 0.51±0.18 nM (n=3) and 0.89±0.27 nM (n=3), respectively.
- Bradyzide is a competitive antagonist, inhibiting B2 receptor‐induced 45Ca efflux from NG108‐15 cells with a pKB of 8.0±0.16 (n=5) and a Schild slope of 1.05.
- In the rat spinal cord and tail preparation, bradyzide inhibits bradykinin‐induced ventral root depolarizations (IC50 value; 1.6±0.05 nM (n=3)).
- Bradyzide is much less potent at the human than at the rodent B2 receptor, displacing [3H]‐bradykinin binding in human fibroblasts and in Cos‐7 cells expressing the human B2 receptor with KI values of 393±90 nM (n=3) and 772±144 nM (n=3 …
引用总数
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GM Burgess, MN Perkins, HP Rang, EA Campbell… - British journal of pharmacology, 2000