Characterisation, CNS distribution and function of NK2 receptors studied using potent NK2 receptor antagonists

Effect of the acute and chronic administration of the selective neurokinin2 receptor antagonist SR 48968 on midbrain dopamine neurons in the rat: An in vivo extracellular single cell study

“…However, a recent report has shown that the radiolabeled peptide Lys 5 , Tyr (I 2 ) 2 , MeLeu 9 , Nle 10 NKA4-10, a selective NK 2 agonist, does not appear to label NK 2 receptors in the rat CNS (Mussap et al, 1993). In addition, using tritiated GR100679, a selective NK 2 peptide antagonist, it has been reported that NK 2 receptors are found only in brains from immature but not adult rats (Hagan et al, 1993). However, in support of the presence of NK 2 receptors in the adult brain, it has been shown that the microinjection of the selective NK 2 agonist GR 51667 into the SNC area produces contralateral turning and this effect can be blocked by the NK 2 antagonist L659877 (Elliott et al, 1991).…”

Endogenous modulation of excitatory amino acid responsiveness by tachykinin NK1 and NK2 receptors in the rat spinal cord

“…The solutions used for the iontophoretic administration of EAA and NK agonists were also given. In the present study the following NK antagonist drugs were also used: the peptide NKI antagonist GR82334 (Hagan et al, 1991); the non-peptide NKI antagonist CP-99,994 (McLean et al, 1993); the peptide NK2 antagonist GR103537 (Hagan et al, 1993); and the non-peptide NK2 antagonist GR159897 (Ball et al, 1994). Details of structures and of the solutions used for microiontophoresis are shown in Table 1 recovery (t1') was 6 min, with a range of 3-22 min.…”

The pharmacology of GR203040, a novel, potent and selective non‐peptide tachykinin NK1 receptor antagonist

“…Human NK2 receptors were stably expressed in CHO cells as previously described (Hagan et al, 1993). U373 MG cells were purchased from the American tissue culture collection.…”

“…NK2 receptor binding assays in CHO cell membranes were carried out essentially as described previously (Hagan et al, 1993;Beresford et al, 1995). The membrane suspension (5 Mg protein) in assay buffer (Tris base (50 mM), MnCl2 (3 mM), bovine serum albumin (0.05%), chymostatin (2 Mg ml-') and leupeptin (4 Mg ml-, pH 7.4)) were incubated for 90 min at room temperature with wash buffer (Tris base (50 mM), MnCl2 (3 mM), lauryl sulphate (0.01%), pH 7.4) or test compound, and [3H]-GR100679 (0.5 nM final concentration).…”