ライフサイエンスコーパス: M4 receptor

1 inhibits modulation of Ca(2+) current by the M4 receptor.

2 one of which was identical to the endogenous M4 receptor.

3 rs, but it increases ACh potency 3.5-fold at M4 receptors.

4 cells transfected with the Gi-coupled M2 and M4 receptors.

5 approximately 1.5-fold by brucine-N-oxide at m4 receptors.

6 n the levels of mRNA encoding the M1, M2 and M4 receptors.

7 It had 13-fold lower affinity for M4-receptors, 260-fold lower affinity for M3-receptors,

8 We propose that M4 receptor agonists could represent an innovative strat

9 y": a lack of action at any concentration at M4 receptors and an action at M2 and M3 receptors.

10 acetylcholine dip must interact, via D1 and M4 receptor, and a dopamine dip must interact with adeno

11 ments in rats were related to stimulation of M4 receptors, and that these movements could be suppress

12 Remarkably, pretreatment with muscarinic (m2/m4) receptor antagonists resulted in robust oxotremorine

13 Immunoreactivity in cat to the m1 or m4 receptor antibodies was undetectable.

14 Lower levels (5% to 10%) of the m2 and m4 receptors are present in these tissues.

15 gested that the dopamine release-stimulating M4 receptors are probably located on neuronal cell bodie

16 this TM7 epitope is likewise present in the M4 receptor, as M4(436)serine.

17 were found not to be mediated via M1, M2 or M4 receptors, as they were not blocked by the M1-selecti

18 it inhibits [3H]NMS dissociation from M1 to M4 receptors at submillimolar concentrations and from M5

19 and a full agonist with an IC50 of 11 nM at M4-receptors, based on inhibition of cyclic AMP accumula

20 o increases the direct binding of [3H]ACh to M4 receptors but decreases it slightly at M2 receptors.

21 to 5-fold for inhibiting [3H]NMS binding to M4 receptors but has no effect on ACh affinity at M1 to

22 um, which contain autoinhibitory presynaptic M4 receptors, but not from hippocampal slices, which con

23 blocked cloned M2 receptors had no effect on M4 receptors, but slightly increased [(3)H]NMS binding t

24 , suggesting that preferential expression of m4 receptors by striatonigral neurons may contribute to

25 While a contributory role of the M4 receptor cannot be ruled out, there is no evidence in

26 or histological defects, and the m2, m3, and m4 receptors continue to be expressed in brain with no e

27 cluded that there is a relative abundance of M4 receptors controlling the direct pathway.

28 Muscarinic m2 and m4 receptors couple preferentially to inhibition of aden

29 otally abolished in tissues prepared from M2-M4 receptor double KO mice.

30 ha2-AR analgesia would also destroy nNOS and M4 receptor expression.

31 tivity of N-chloromethyl brucine with ACh on M4 receptor function was also observed, thereby demonstr

32 nd cerebral cortex, but predominantly by the M4 receptor in the striatum.

33 R-neurons by selectively blocking muscarinic M4 receptors in the NAc-S, which tightly regulate the ac

34 half of all projection neurons, and mRNA for M4 receptors is prevalent only in striatonigral neurons.

35 riatal [3H]dopamine release was abolished in M4 receptor KO mice, significantly increased in M3 recep

36 ability, with blockade of presynaptic m2 and m4 receptors, leading to increased out-of-field firing.

37 hese fibers In contrast, changes in nNOS and M4 receptor location on spinal cord neurons are not resp

38 e most specific antagonists known for M1 and M4 receptors (m1-toxin and m4-toxin), it was screened fo

39 xin that binds with very high specificity to M4 receptors (m4-toxin) was biotinylated for use as a se

40 d selectively to one of five mAChR subtypes, M4 receptors (M4Rs), at their C-terminal regions of seco

41 uculline methochloride suggested that M3 and M4 receptors mediate their dopamine release-modulatory e

42 ggest that pharmacological antagonism of the M4 receptor modulates select behavioral responses in the

43 s tested, nearly all expressed M2-class (m2, m4) receptor mRNAs, whereas m1 receptor mRNA was found i

44 more rigorously compare the distribution of M4 receptors on rat neurons in these pathways a toxin th

45 Here, we report that activation of M4 receptors on striatal spiny projection neurons result

46 Labeled neurons were probed for M4 receptor protein using biotinylated m4-toxin and fluo

47 iotinylated for use as a selective probe for M4 receptor protein.

48 ide on acetylcholine (ACh) potency at M1 and M4 receptors respectively have been confirmed in guanosi

49 elease studies with brain slices from M2 and M4 receptor single KO mice indicated that autoinhibition

50 ptor subtypes but not with antibodies to the m4 receptor subtype.

51 In particular, the M1 and M4 receptor subtypes have emerged as attractive drug tar

52 Consistent with action at M2 or M4 receptor subtypes, Oxo-M could be antagonized by 10 m

53 The striatum has many more M4 receptors than other tissues, they are located on app

54 expressed in the same zone as the endogenous M4 receptor, the two expression patterns were, in large

55 ons, suggesting preferential localization of m4 receptors to striatonigral neurons.

56 e muscarinic agonist oxotremorine-M, M2, and M4 receptors underwent significantly reduced internaliza

57 ical targeting to the basolaterally targeted M4 receptor, Val270-Lys280 and Lys280-Ser350.

58 M4 receptors were found on 14% of indirect and 86% of di

59 the cDNAs that encode the established M3 and M4 receptors were identified.

60 Ca(V)1.2c, whereas Galphai/o-coupled M2 and M4 receptors were ineffective.

61 M4 receptors were present on neurons in the dorsal horn,

62 ne (1.0 mM), which blocks presynaptic m2 and m4 receptors, were initially strong but then diminished

63 the orthosteric and allosteric sites of the M4 receptor, which provides new insight into how alloste

64 e M2AChR and a partial agonist at the M1 and M4 receptors, with full antagonist activity at M3- and M