Investigation into species variants in tachykinin NK1 receptors by use of the non-peptide antagonist, CP-96,345.
The affinity of the non-peptide antagonist CP-96,345 for tachykinin NK1 receptors has been estimated in a range of species by use of both radioligand binding and functional assays. CP-96,345 was 30-120 fold less active at NK1 receptors in rat and mouse than in the other species examined, including man. These results demonstrate the existence of species variations in NK1 receptors.
Beresford
I J
IJ
Department of Neuropharmacology, Glaxo Group Research Ltd., Ware, Hertfordshire.
Birch
P J
PJ
Hagan
R M
RM
Ireland
S J
SJ
D000818:Animals; D001713:Biphenyl Compounds / Q000494:pharmacology*; D002417:Cattle; D006224:Cricetinae; D005849:Gerbillinae; D006168:Guinea Pigs; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009130:Muscle, Smooth / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D011817:Rabbits; D011869:Radioligand Assay; D051381:Rats; D017981:Receptors, Neurotransmitter / Q000037:antagonists & inhibitors*; D018039:Receptors, Tachykinin; D013045:Species Specificity; D013116:Spinal Cord / Q000187:drug effects; D015320:Tachykinins / Q000037:antagonists & inhibitors*
D001713:Biphenyl Compounds; D017981:Receptors, Neurotransmitter; D018039:Receptors, Tachykinin; D015320:Tachykinins; C066892:CP 96345