rat nk1 receptor

Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).

Vofopitant dihydrochloride (GR 205171A) is an orally available, selective tachykinin NK1 receptor antagonist that inhibits [3H]SP binding to NK1 with pKi values of 9.5 and 10.6, respectively. It is a potential compound for the treatment of pathological vomiting.

GR203040 inhibits cyclophosphamide-induced damage in the rat and ferret bladder. GR-203040 is a selective NK1 receptor antagonist.

Nolpitantium Free Base is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no effect in bioassays for NK2 and NK3 receptors. The antagonism exerted by Nolpitantium toward NK1 receptors was apparently non-competitive, with pD2' values between 9.65 and 10.16 in the different assays. Nolpitantium also blocked in vitro [Sar9, Met(O2)11]substance P-induced release of acetylcholine from rat striatum. In vivo, Nolpitantium exerted highly potent antagonism toward [Sar9, Met(O2)11]substance P-induced hypotension in dogs, bronchoconstriction in guinea-pig) and plasma extrava......

GR 64349 is a potent and highly selective NK2 receptor peptide antagonist with an EC50 of 3.7 nM in rat colon, exhibiting over 1000-fold selectivity against NK1 receptors and over 300-fold selectivity against NK3 receptors, ensuring targeted action [1] [2].

[Sar9,Met(O2)11]-Substance P TFA is a selective tachykinin NK1 receptor agonist.[Sar9,Met(O2)11]-Substance P and septide (10-100 pmol per rat, i.c.v.) are equipotent in increasing mean arterial blood pressure (MAP) and heart rate (HR), yet they have dissi

[Sar9,Met(O2)11]-Substance P acetate is a tachykinin NK1 receptor selective agonist. [Sar9,Met(O2)11]-Substance P acetate is a selective tachykinin NK1 receptor agonist.[Sar9,Met(O2)11]-Substance P acetate and septide (10-100 pmol per rat, i.c.v.) are equipotent in increasing mean arterial blood pressure (MAP) and heart rate (HR), yet they have dissimilar time-course. Both agonists increase dose-dependently face washing and sniffing while [Sar9,Met(O2)11]-Substance P acetate is the sole to produce grooming.

Potent and selective tachykinin NK2 receptor agonist (EC50 = 3.7 nM in rat colon). Displays > 1000- and > 300-fold selectivity over NK1 and NK3 receptors respectively. Active in vivo.