Antihyperalgesic activity of a novel nonpeptide bradykinin B1 receptor antagonist in transgenic mice expressing the human B1 receptor

1 We describe the properties of a novel nonpeptide kinin B1 receptor antagonist, NVP‐SAA164, and demonstrate its in vivo activity in models of inflammatory pain in transgenic mice expressing the human B1 receptor. 2 NVP‐SAA164 showed high affinity for the human B1 receptor expressed in HEK293 cells...

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Veröffentlicht in:	British journal of pharmacology 2005-04, Vol.144 (7), p.889-899
Hauptverfasser:	Fox, Alyson, Kaur, Satbir, Li, Bifang, Panesar, Moh, Saha, Uma, Davis, Clare, Dragoni, Ilaria, Colley, Sian, Ritchie, Tim, Bevan, Stuart, Burgess, Gillian, McIntyre, Peter
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Analgesics - chemistry Analgesics - pharmacology Analgesics - therapeutic use Animals Benzamides - chemistry Benzamides - pharmacology Benzamides - therapeutic use Bradykinin B1 Receptor Antagonists Cell Line COS Cells Dose-Response Relationship, Drug Female Gene Expression Regulation - drug effects Gene Expression Regulation - physiology human B1 receptor knockin Humans hyperalgesia Hyperalgesia - drug therapy Hyperalgesia - genetics Hyperalgesia - metabolism inflammation Kinin B1 receptor Macaca mulatta Mice Mice, Inbred C57BL Mice, Knockout Mice, Transgenic Rats Receptor, Bradykinin B1 - genetics Receptor, Bradykinin B1 - metabolism Sulfonamides - chemistry Sulfonamides - pharmacology Sulfonamides - therapeutic use
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