ライフサイエンスコーパス: NK-1 receptor

1 selective cyclic hexapeptide ligand for the NK-1 receptor.

2 different ratios of the two isoforms of the NK-1 receptor.

3 evented with pharmacological blockade of the NK-1 receptor.

4 elationship between Met174 and Met181 on the NK-1 receptor.

5 eir ability to displace substance P from its NK-1 receptor.

6 ess pronounced in neurons that expressed the NK-1 receptor.

7 27 was highly potent (IC50 of 27 nM) at the NK-1 receptor.

8 ed human receptor subtypes (hSSTRs), and the NK-1 receptor.

9 receptors differ markedly from those at the NK-1 receptor.

10 ing that this effect was mediated through an NK-1 receptor.

11 showed high potency and selectivity for the NK(1) receptor.

12 oma cell line UC11 that expresses endogenous NK(1) receptor.

13 tissue specific pharmacological targeting of NK-1 receptors.

14 This effect is mediated by NK-1 receptors.

15 n mouse dura mater through the activation of NK-1 receptors.

16 cient to exert maximal effects on the target NK-1 receptors.

17 esumably through actions on submucosal gland NK-1 receptors.

18 and in vivo with agonists of 5-HT(2A) and/or NK-1 receptors.

19 rom the NA is mediated, at least in part, by NK-1 receptors.

20 he second extracellular loop (E2) of the SP (NK-1) receptor.

21 of substance P (SP) to the rat neurokinin-1 (NK-1) receptor.

22 d previously as Met-181 on the neurokinin-1 (NK-1) receptor.

23 ly active antagonists at rat, but not human, NK(1) receptors.

24 ve antagonists of 5-HT(2A) and neurokinin 1 (NK-1) receptors.

25 induced by a resiniferatoxin challenge (with NK-1 receptor activation mediating the subsequent increa

26 to the respiratory network via 5-HT(2A) and NK-1 receptor activation.

27 Comparisons of the NK(1) receptor affinity for the various conformational f

28 response to stress indicates that some other NK-1 receptor agonist may substitute for SP.

29 Injections of the selective neurokinin-1 (NK-1) receptor agonist drug GR-73632 also caused bradyca

30 Met(O2)11]-substance P) which were selective NK-1 receptor agonists, had no impact on the cardioaccel

31 ive rage neurons are excited in two ways: by NK(1) receptors and by an ascending input from the PAG.

32 sis infusions of substance P desensitize the NK(1) receptors and that substance P-induced vasodilatat

33 Neurokinin (NK) 1 receptors and CaV2.3 calcium channels are both exp

34 ne the functional sites for SP activation of NK-1 receptors and potential interactions with cholinerg

35 ugh two distinct pathways: via activation of NK(1) receptors, and via a novel neurokinin receptor-ind

36 Two asymmetric syntheses of the NK(1) receptor antagonist 1-[2-(R)-{1-(R)-[3,5-bis(trifl

37 ereoselective synthesis of the orally active NK(1) receptor antagonist Aprepitant is described.

38 mpounds, and suggests that the high affinity NK(1) receptor antagonist L-760735 may prove to be usefu

39 oride 3 is a high affinity, orally active, h-NK(1) receptor antagonist with a long central duration o

40 resent study, the high affinity substance P (NK(1)) receptor antagonist L-760735 (3 mg/kg) significan

41 etrant, hydroisoindoline-based neurokinin-1 (NK(1)) receptor antagonist with a long central duration

42 tagonist, dexamethasone, and a neurokinin 1 (NK(1)) receptor antagonist.

43 icient synthesis of the potent and selective NK-1 receptor antagonist 1 is described.

44 F release is inhibited by treatment with the NK-1 receptor antagonist 733,060.

45 plished with surprising ease, leading to the NK-1 receptor antagonist 9 (IC50 2.0 +/- 0.4 nM).

46 The NK-1 receptor antagonist CP-99,994 significantly inhibit

47 by 43%, effects that were attenuated by the NK-1 receptor antagonist in the nucleus tractus solitari

48 we coadministered morphine with a dose of an NK-1 receptor antagonist that by itself was without effe

49 A number of animals received the non-peptide NK-1 receptor antagonist WIN-51,708 (10 mg/kg) 30 min be

50 thyl]-1 -azabicyclo[2.2.2]octan-3-amine]; an NK-1 receptor antagonist) or PD 098059 (MEK1 inhibitor)

51 ts of iontophoretically applied CP-99,994 (a NK-1 receptor antagonist), SP and SP(1-7) (an N-terminal

52 We aimed to assess rolapitant, an NK-1 receptor antagonist, for prevention of chemotherapy

53 At 6 weeks of age, either vehicle or a NK-1 receptor antagonist, SR 140333, was injected into t

54 effects are blocked by pretreatment with an NK-1 receptor antagonist.

55 was abrogated in the presence of a specific NK-1 receptor antagonist.

56 Guidelines recommend use of a neurokinin-1 (NK-1) receptor antagonist in conjunction with a 5-HT3 re

57 se effects were all blocked through specific NK-1 receptor antagonists.

58 LAD2 cells with two different neurokinin-1 (NK-1) receptor antagonists and siRNA inhibits TNF secret

59 asal ganglia, we tested and characterized an NK-1 receptor-based method for targeted ablation of spec

60 Conversely the NK-1 receptor binds substance P but not the above ligand

61 hesus showed that this compound provides 90% NK(1) receptor blockade in rhesus brain at a plasma leve

62 increases in the level of mRNA encoding the NK-1 receptor by up to 12- and 13-fold, respectively.

63 These data suggest NK(1) receptors contribute to active vasodilatation and

64 e to active vasodilatation and that combined NK(1) receptor desensitization and NO synthase inhibitio

65 vity in the amygdaloid complex, induction of NK(1) receptor endocytosis in the amygdala following imm

66 the number of dendritic processes undergoing NK(1) receptor endocytosis in the basolateral amygdala t

67 ntify the effect of immobilisation stress on NK(1) receptor endocytosis morphology, a marker of local

68 The NK-1 receptor expressed in Chinese hamster ovary cells w

69 laboratory have suggested that substance P (NK-1) receptor expression by macrophages contributes to

70 This supports the hypothesis that increased NK-1 receptor gene expression contributes to the develop

71 Nociception-evoked alterations in NK-1 receptor gene expression have been studied in rat m

72 ts after formalin or adjuvant injection when NK-1 receptor gene expression is elevated in the dorsal

73 (2))(11)]SP(7-11), to the partially purified NK-1 receptor has been analyzed by this method.

74 press authentic substance P receptors (i.e., NK-1 receptors) has been inferred from radioreceptor bin

75 The distribution of NK(1) receptor immunoreactivity in the amygdaloid comple

76 t mice, indicating an essential role for the NK(1) receptor in mediating NKB-induced skin oedema.

77 Overall, the findings indicate that NK(1) receptors in the medial hypothalamus facilitate de

78 The results indicate that NK(1) receptors in the PAG potentiate defensive rage and

79 xious stimulus-evoked internalization of the NK-1 receptor in lamina I neurons.

80 sents the first evidence of participation of NK-1 receptors in cystitis and a mandatory participation

81 We conclude that stimulation of NK-1 receptors in the superficial laminae of the dorsal

82 C-fiber input, indicating the involvement of NK-1 receptors in wind-up.

83 ntral role for substance P and neurokinin-1 (NK-1) receptors in cystitis.

84 nociception, and SP activates neurokinin-1 (NK-1) receptors in the spinal cord and periphery.

85 correlated with the magnitude of SP-induced NK-1 receptor internalization in dorsal horn neurons.

86 than noxious thermal stimulation in inducing NK-1 receptor internalization, and this was increased in

87 SP release, Fos expression and neurokinin-1 (NK-1) receptor internalization, in the rat.

88 regions of the SP receptor, also termed the NK-1 receptor, involved in peptide recognition, we are u

89 site of Bpa(4)-SP covalent attachment to the NK-1 receptor is Met-174.

90 definitive evidence of the existence of such NK-1 receptor isoforms in tissue has been presented.

91 xtravasation produced by NKB in the lungs of NK(1) receptor knockout mice was unaffected by treatment

92 d (125)I-albumin in wild-type and tachykinin NK(1) receptor knockout mice.

93 bsent in W/W(v) mast cell-deficient mice and NK-1 receptor knockout mice (NK-1R-/-), but was unaltere

94 cough and bronchoconstriction in part by an NK-1 receptor mechanism in the nucleus tractus solitariu

95 ion in young guinea pigs via a neurokinin-1 (NK-1) receptor mechanism at the first central synapse of

96 ays and, most recently, by identification of NK-1 receptor mRNA expression, we know little about NK-1

97 This study assessed behavioral responses and NK-1 receptor mRNA gene expression in mice receiving for

98 ease protection assays were used to quantify NK-1 receptor mRNA levels.

99 NK-1 receptor mRNA was localized to submucosal glands.

100 tion of substance-P-preferring neurokinin-1 (NK-1) receptor mRNA was assessed by in situ reverse tran

101 and IFN-gamma can increase the expression of NK-1 receptors on murine peritoneal macrophages.

102 essed the role of the striatal neurokinin-1 (NK-1) receptor on pre- and post-synaptic METH-induced da

103 igh affinity receptors for SP (Neurokinin-1 (NK-1) receptors) on microglia and shown that this tachyk

104 amined in gerbils, a species with human-like NK(1) receptor pharmacology.

105 icrom dose of substance P to desensitize the NK(1) receptors prior to whole-body heating.

106 significantly increase the expression of the NK-1 receptor protein as measured by Western blot and FA

107 The synthesis of a spirobicyclic NK-1 receptor (Substance-P) antagonist 1 antipode is des

108 lts suggest that human corneal cells express NK-1 receptors that specifically bind SP and induce IL-8

109 e the potential involvement of neurokinin-1 (NK(1)) receptors to active vasodilatation.

110 er, these results demonstrate the ability of NK-1 receptors to signal IL-12 production by macrophages

111 Immunostaining for the NK-1 receptor was mainly absent from the SCN of hamster

112 Mutant NK-1 receptors were constructed by substituting Ala for

113 thod labels both long and short forms of the NK-1 receptor, while the latter labels only the long for

114 and for in vivo quantification of tachykinin NK(1) receptors with PET.

115 sites have been previously reported for the NK-1 receptor, with the use of classical methods (radiol