Constantine J W, Lebel W S, Woody H A
Exploratory Medicinal Chemistry, Pfizer Central Research, Pfizer Inc., Groton, CT 06340.
Naunyn Schmiedebergs Arch Pharmacol. 1990 Dec;342(6):722-4. doi: 10.1007/BF00175719.
Neurokinin A, neurokinin B and substance P caused concentration-related contractions of rabbit isolated aorta with pD2 values of 8.1, 6.9, and 6.0, respectively. [D-Pro2, D-Trp7, 9]-substance P, a competitive tachykinin antagonist, had pA2 values of 5.3 against neurokinin A, 5.1 against neurokinin B and 5.2 against substance P indicating that tachykinin receptors mediated responses to the agonists. [pGlu5,MePhe8,-MeGly9]-substance P 5 - 11 (DiMe-C7), senktide and septide did not contract the aorta. It is concluded that of the known tachykinin receptors smooth muscle of the rabbit isolated aorta contains only the NK-2 type.