ライフサイエンスコーパス: CGRP receptor

1 are humanised antibodies against CGRP or the CGRP receptor.

2 epant), an orally bioavailable antagonist of CGRP receptor.

3 ein-1 (hRAMP1), an obligatory subunit of the CGRP receptor.

4 cell surface as a mature glycoprotein and a CGRP receptor.

5 fragment 8-37, an antagonist of one class of CGRP receptor.

6 ted peptide (h-alpha-CGRP) in activating the CGRP receptor.

7 in this position is not in contact with the CGRP receptor.

8 7) is preferred for high-affinity binding to CGRP receptors.

9 ubstantially increased binding affinities at CGRP receptors.

10 n of antagonists with increased affinity for CGRP receptors.

11 Phe caused no change in binding affinity at CGRP receptors.

12 of ADM receptors, but also to activation of CGRP receptors.

13 ly potent agonist effects of h-alpha-CGRP at CGRP receptors.

14 cluding the calcitonin gene-related peptide (CGRP) receptor.

15 1 to give a calcitonin gene-related peptide (CGRP) receptor.

16 nist of the calcitonin gene-related peptide (CGRP) receptor.

17 that RAMP1 is functionally rate limiting for CGRP receptor activity in the trigeminal ganglion, which

18 mucosal HIV-1 transmission and suggest that CGRP receptor agonists might be used therapeutically aga

19 nstrated in whole muscle tissue, the type of CGRP receptor and its associated proteins or its cellula

20 n SK-N-MC and L6 cells expressing endogenous CGRP receptors and competed with labeled CGRP for bindin

21 Phe(37) of h-alpha-CGRP(8-37) for binding to CGRP receptors and have identified the N-terminus and Hi

22 e required for signal transduction at ocular CGRP receptors and is localized to sites previously repo

23 that mature and immature DCs express type 1 CGRP receptors and that signaling through these receptor

24 eceptors, a calcitonin gene-related peptide (CGRP) receptor and an adrenomedullin receptor.

25 djacent to the lateral ventricle, is rich in CGRP receptors, and has itself been implicated in anxiet

26 We examined the binding sites of a CGRP receptor antagonist (MK-3207) and related this to t

27 al characterization of a highly potent, oral CGRP receptor antagonist BMS-927711 (8).

28 ns of CGRP were probed and elucidated by the CGRP receptor antagonist CGRP(8-37).

29 nthesis was abrogated in the presence of the CGRP receptor antagonist CGRP8-37.

30 CGRP and blocked by coadministration of the CGRP receptor antagonist olcegepant.

31 iography was performed with [(3)H]MK-3207 (a CGRP receptor antagonist).

32 he CGRP pathway was shown in skin by using a CGRP receptor antagonist.

33 The calcitonin gene-related peptide (CGRP) receptor antagonist, CGRP8-37 (1.3 mg/kg i.v.), ad

34 tide (CGRP), as treatment with the selective CGRP-receptor antagonist CGRP(8-37) prevented this effec

35 The advent of CGRP receptor antagonists as a novel therapy for migrain

36 Herein we describe optimization of CGRP receptor antagonists based on an earlier lead struc

37 The observation that various nonpeptide CGRP receptor antagonists display a higher affinity for

38 ndent manner during CSD, and three different CGRP receptor antagonists had a dose-dependent inhibitor

39 Several non-peptide CGRP receptor antagonists have been shown to exhibit mar

40 The development of CGRP receptor antagonists is discussed in detail, as wel

41 igger migraine in humans and the efficacy of CGRP receptor antagonists that evidently do no penetrate

42 Furthermore, nonpeptide CGRP receptor antagonists, CGRP antibodies and CGRP-bind

43 clinical trials with multiple small molecule CGRP receptor antagonists.

44 e for the affinities of structurally diverse CGRP receptor antagonists.

45 Calcitonin gene-related peptide (CGRP) receptor antagonists have demonstrated anti-migrai

46 Calcitonin gene-related peptide (CGRP) receptor antagonists have demonstrated clinical ef

47 t neurons in the central amygdala expressing CGRP receptors are also critical for establishing a thre

48 the possible use of drugs targeting central CGRP receptors as antimigraine agents.

49 c phenotype was due to overexpression of the CGRP receptor at endogenous or novel expression sites.

50 This study demonstrates CGRP receptor binding sites and expression of the CGRP r

51 To define CGRP receptor binding sites, in vitro autoradiography wa

52 Calcitonin gene-related peptide (CGRP) receptor blockade has been shown to be an effectiv

53 icin) and a calcitonin gene-related peptide (CGRP) receptor blocker (CGRP(8-37)) was also used to elu

54 PCR revealed expression of mRNA for a type 1 CGRP receptor by mature and immature blood-derived DCs.

55 ical studies have shown that blockade of the CGRP receptor can produce antimigraine efficacy comparab

56 The results suggest that HCEC possess CGRP receptors capable of initiating a signal transducti

57 nalysis confirmed the identity of the type 1 CGRP receptor (CGRP-R1).

58 n myometrial contractions and the changes in CGRP receptors (CGRP-Rs) in human myometrium have not be

59 e either a CGRP receptor or a component of a CGRP receptor complex.

60 This CGRP receptor component protein confers CGRP-specific ac

61 In situ hybridization demonstrated that the CGRP receptor component protein is expressed in outer ha

62 sensory nerve density was reduced and RAMP1 (CGRP receptor component) associated with nuclear regions

63 ously shown that this accessory protein, the CGRP-receptor component protein (RCP), is expressed in C

64 s, receptor activity modifying protein 1 and CGRP-receptor component protein, required for ligand spe

65 tion, and refolding of a soluble form of the CGRP receptor comprising a heterodimer of the CLR and RA

66 t that mice with normal levels of endogenous CGRP receptors demonstrate light avoidance following CGR

67 f sensory nerves or knockdown in vivo of the CGRP-receptor-encoding genes Calcrl or Ramp1 substantial

68 fully human monoclonal antibody against the CGRP receptor, for migraine prevention.

69 itized mice that have elevated levels of the CGRP receptor hRAMP1 subunit in nervous tissue (nestin/h

70 receptor binding sites and expression of the CGRP receptor in rhesus and rat TG.

71 We show that pharmacologic inactivation of CGRP receptors in old wild-type animals can restore meta

72 fully human monoclonal antibody against the CGRP receptor, in patients with chronic migraine.

73 t and specific nonpeptide antagonists of the CGRP receptor, including olcegepant and telcagepant (K(D

74 ied ECD complex vs 233 pM for membrane-bound CGRP receptor), indicating that other regions of CLR and

75 results indicate that the activation of BNST CGRP receptors is both necessary and sufficient for some

76 evidence that the responsiveness of neuronal CGRP receptors is strongly enhanced in vitro and in vivo

77 we demonstrate that activation of endogenous CGRP receptors is sufficient to elicit light aversion in

78 The calcitonin gene-related peptide (CGRP) receptor is a heterodimer of two membrane proteins

79 If so, inhibition of CGRP receptors may be a clinically useful strategy for a

80 A candidate CGRP receptor named calcitonin receptor-like receptor (C

81 We first demonstrated that activation of CGRP receptors on cultured trigeminal ganglion neurons i

82 ilic protein that is presumed to be either a CGRP receptor or a component of a CGRP receptor complex.

83 ke receptor (CRLR), can function as either a CGRP receptor or an adrenomedullin receptor, depending o

84 functional calcitonin gene-related peptide (CGRP) receptor or an adrenomedullin (AM) receptor.

85 The target CGRP receptor, produced in part from the calcitonin rece

86 Whereas the distribution of CGRP receptor proteins was similar in SMCs, RAMP1 associ

87 The heterodimeric CGRP receptor requires co-expression of calcitonin recep

88 functional calcitonin gene-related peptide (CGRP) receptor requires dimerization of calcitonin recep

89 f small molecule antagonist affinity for the CGRP receptor reside within the extracellular region of

90 through the alpha(2)-adrenergic receptor and CGRP receptor, respectively, because blocking these rece

91 ction, whose cardiac effects are mediated by CGRP-receptor stimulation.

92 th >100-fold higher affinities for the human CGRP receptor than for receptors from other species.

93 expression of RAMP1 and CRLR reconstituted a CGRP receptor that was able to activate the pheromone-si

94 as a chaperone but was instead coupling the CGRP receptor to downstream effectors.

95 In addition, CGRP receptors were not observed in ventricular myocardi

96 e effects are attributable to stimulation of CGRP receptors within the BNST itself.