ライフサイエンスコーパス: mGluR4

1 submicromolar potency at both human and rat mGluR4.

2 amides as positive allosteric modulators of mGluR4.

3 g, we discovered more than 400 novel PAMs of mGluR4.

4 ompound is a mixed allosteric agonist/PAM of mGluR4.

5 logical profile consistent with mediation by mGluR4.

6 CC) is a selective allosteric potentiator of mGluR4.

7 sent in brains of knockout mice deficient in mGluR4.

8 rongly activates group III mGluR, especially mGluR4,-6,-8 but not group I or II mGluR.

9 ound selectively potentiated agonist-induced mGluR4 activity in cultured cells expressing this recept

10 ) transient amplitude were more sensitive to mGluR4 agonist.

11 ein-coupled metabotropic glutamate receptor, mGluR4, also is expressed in lingual tissues and is limi

12 naptic mGluR2/3 and mGluR8 receptors but not mGluR4, although this receptor is present.

13 4 confirmed the interaction observed between mGluR4 and a selection of exocytosis proteins, including

14 d that residue 74 corresponding to lysine in mGluR4 and asparagine in mGluR7 might play a key role, a

15 amate-selective G protein-coupled receptors, mGluR4 and mGluR1, and the taste bud-expressed heterodim

16 luR3 mRNAs were low or undetectable, whereas mGluR4 and mGluR5 mRNA signals were high in most neurons

17 he metabotropic glutamate receptors (mGluRs) mGluR4 and mGluR7 have been postulated to serve as presy

18 Instead, we found that mGluR4 and mGluR7 were located close to bipolar cell rib

19 ceptor, mGluR1, and the group III receptors, mGluR4 and mGluR7.

20 mice lacking either mGluR4, mGluR8, or both mGluR4 and mGluR8.

21 mGluR7 differs from mGluR4 and other group III mGluR in that L-glutamate and

22 including the presynaptic glutamate receptor mGlur4 and the Wnt receptor Fzd3.

23 metabotropic glutamate receptor 1 (mGluR1), mGluR4, and mGluR5 by human brain and dermal microvascul

24 artners that co-immunoprecipitated with anti-mGluR4 antibodies were identified and classified accordi

25 Immunoprecipitations using anti-mGluR4 antibodies were performed with cerebellar extract

26 ytics, and positive allosteric modulators of mGluR4 appear to be an exciting new target for the treat

27 citing results provide continued support for mGluR4 as a therapeutic target in PD.

28 ified the metabotropic glutamate receptor 4 (mGluR4) as a potential drug target and predicted that se

29 ype 4 metabotropic glutamate receptor (taste-mGluR4),as umami-responsive receptors.

30 d also exhibited partial agonist activity at mGluR4 at a site that was distinct from the glutamate bi

31 n, a process that is exclusively provided by mGluR4 at parallel fiber-Purkinje cell synapse in rodent

32 mGluR4 belongs to group III and is mainly localized pres

33 PHCCC, enhanced the potency of glutamate at mGluR4 by 8-fold, and did not show any significant poten

34 esults could give indications to explain how mGluR4 can modulate glutamate release at parallel fiber-

35 emistry experiments showed that Munc18-1 and mGluR4 colocalized at plasma membrane in HEK293 cells, o

36 corresponding to the cytoplasmic domains of mGluR4 confirmed the interaction observed between mGluR4

37 e interesting possibility that activation of mGluR4 could decrease the excessive inhibition of the GP

38 t and predicted that selective activation of mGluR4 could provide palliative benefit in PD.

39 understanding of molecular mechanisms of the mGluR4 depressant effect, we decided to identify the pro

40 no-4-phosphonobutyrate (L-AP4), a ligand for mGluR4, elicit similar tastes in rats.

41 g nontoxic vehicles, a major advance for the mGluR4 field.

42 nd human mGluR4 using two distinct assays of mGluR4 function.

43 amide ethyl ester, which does not potentiate mGluR4, had no effect in this model.

44 In contrast, mGluR4 has in common with other group III mGluR that it

45 vation of metabotropic glutamate receptor 4 (mGluR4) has been shown to modulate neurotransmission in

46 mGluR4 immunostaining was most abundant in IPL sublamina

47 as been used to further validate the role of mGluR4 in PD, but the compound suffers from a lack of se

48 Upregulation of presynaptic mGluR4 in pup CA3 neurons could lead to reduced transmit

49 Expression of mGluR4 in taste buds is higher in preweaning rats compar

50 esidues that when swapped between mGluR1 and mGluR4 increased the potency of L-SOP inhibition relativ

51 It appears that native mGluR4 interacts with several exocytosis proteins such a

52 In situ hybridization demonstrated that mGluR4 is detectable in 40-70% of vallate and foliate ta

53 The metabotropic glutamate receptor 4 (mGluR4) is an emerging target for the treatment of Parki

54 n striatopallidal transmission was absent in mGluR4 knock-out mice, providing convincing evidence tha

55 We conclude that mGluR4 may be a chemosensory receptor responsible, in pa

56 r of mGluRs and suggest that potentiation of mGluR4 may be a useful therapeutic approach to the treat

57 est that the metabotropic glutamate receptor mGluR4 may function in glutamate taste transduction.

58 f mGluR7 in the hippocampus and suggest that mGluR4 may have both presynaptic and postsynaptic functi

59 The finding that mGluR4 may selectively modulate striatopallidal transmis

60 out mice, providing convincing evidence that mGluR4 mediates this effect.

61 glutamate receptor subunits mGluR1, mGluR3, mGluR4, mGluR5, and mGluR7.

62 n genetically engineered mice lacking either mGluR4, mGluR8, or both mGluR4 and mGluR8.

63 In pup but not adult rats, mGluR4 mRNA expression was enhanced in CA3 pyramidal neu

64 diminished the potency/efficacy of L-SOP for mGluR4 mutants.

65 d (VU0155041), contained the majority of the mGluR4 PAM activity and also exhibited partial agonist a

66 boxamide (PHCCC) and combined application of mGluR4 PAMs with the mGluR2 selective PAM biphenyl indan

67 ation of compound 40, a potent and selective mGluR4 positive allosteric modulator (PAM) with good wat

68 boxycyclopropyl)glycine (DCG-IV) or with the mGluR4 selective agonist L-(+)-2-amino-4-phosphonobutyri

69 Furthermore, application of the mGluR4 selective PAMs N-(4-chloro-3-methoxyphenyl)-2-pyr

70 is a positive allosteric modulator (PAM) of mGluR4 that has been used to further validate the role o

71 characterized in vitro at both rat and human mGluR4 using two distinct assays of mGluR4 function.

72 In addition, native mGluR4 was retained on a Sepharose column covalently gra

73 addition, combining ET identified swaps from mGluR4 with one identified by computational docking prod