ライフサイエンスコーパス: beta2 adrenoceptor

1 f the angiotensin II type 1 receptor and the beta2 adrenoceptor.

2 ting G protein-coupled receptors such as the beta2-adrenoceptor.

3 wn and does not occur in the closely related beta2-adrenoceptor.

4 used beta-blockers are agonists at the human beta2-adrenoceptor.

5 than that in cells expressing the wild-type beta2-adrenoceptor.

6 beta1-adrenoceptors and unlike those seen at beta2-adrenoceptors.

7 heir ability to internalize GFP-tagged human beta2-adrenoceptors.

8 (log KD -8.95) and is very selective for the beta2-adrenoceptor (1000-fold selectivity over the beta1

9 obodies) to directly probe activation of the beta2-adrenoceptor, a prototypical GPCR, and its cognate

10 Instead, beta2 adrenoceptor activation was responsible for mediat

11 n the amygdala is mediated by both beta1 and beta2-adrenoceptor activation.

12 We have further characterized the novel beta2 adrenoceptor agonist C26 (7-[(R)-2-((1R,2R)-2-benz

13 t dissociation rate we have observed for any beta2 adrenoceptor agonist tested to date.

14 who will inevitably be taking a long-acting beta2-adrenoceptor agonist (LABA)/ICS combination therap

15 Bath application of the selective beta2-adrenoceptor agonist salmeterol (15 microM) facili

16 In addition, the beta2-adrenoceptor agonist zinterol significantly increa

17 odimer combinations (with the Y4 receptor or beta2-adrenoceptor), agonist and antagonist pharmacology

18 The beta2 adrenoceptor agonists formoterol and salbutamol me

19 series of novel, potent, and selective human beta2 adrenoceptor agonists incorporating a sulfone moie

20 can be significantly enhanced by long-acting beta2-adrenoceptor agonists (LABAs) and may contribute t

21 opamine were as potent as several well-known beta2-adrenoceptor agonists (salbutamol, procaterol, and

22 ding kinetics of several clinically relevant beta2-adrenoceptor agonists and antagonists and demonstr

23 h drugs that are currently available such as beta2-adrenoceptor agonists and corticosteroids, it take

24 ent COPD therapy involving anticholinergics, beta2-adrenoceptor agonists and/or corticosteroids, do n

25 buterol has been one of the most widely used beta2-adrenoceptor agonists for the relief of the sympto

26 AHR in the neonatal exposure model, whereas beta2-adrenoceptor agonists had no such effect.

27 clic catecholamine surrogates present in the beta2-adrenoceptor agonists procaterol and BI-167107 (4)

28 tivation is attenuated following exposure to beta2-adrenoceptor agonists such as salbutamol, an effec

29 Dobutamine and terbutaline, beta1- and beta2-adrenoceptor agonists, evoked 17- and 5-fold incre

30 Activation of the beta2-adrenoceptor and cannabinoid CB2 receptors can inh

31 r, was discovered much later than beta1- and beta2-adrenoceptors and exhibits unique properties which

32 lbutamol or by the addition of the selective beta2-adrenoceptor antagonist and inverse agonist ICI 11

33 In the presence of the selective beta2-adrenoceptor antagonist ICI 118,551 HCl (30 microM

34 t and that the administration of the beta1-, beta2-adrenoceptor antagonist propranolol decreases card

35 IBa was reversed by ICI-118,551, a specific beta2-adrenoceptor antagonist, but not by CGP 20712A, a

36 dotoxin, nitro-L-arginine, guanethidine, and beta2-adrenoceptor antagonists.

37 n at least two active conformations, whereas beta2-adrenoceptors are able to induce signaling via dif

38 umulation and CRE gene transcription via the beta2-adrenoceptor at concentrations at which protein ki

39 beta2 adrenoceptor (beta2-AR)-agonists are used to relie

40 Anabolic beta2-adrenoceptor (beta2-AR) agonists have been propose

41 In the heart, stimulation of beta2-adrenoceptor (beta2-AR), a prototypical GPCR, acti

42 echolamine synthesis/degradation and express beta2-adrenoceptors (beta2-AR).

43 of receptors and is implicated in switching beta2 adrenoceptor (beta2AR) G protein specificity in ca

44 Here we report a structure of the human beta2 adrenoceptor (beta2AR), which was crystallized in

45 lation sites into the C-terminal tail of the beta2-adrenoceptor (beta2AR) and demonstrate that this m

46 tion of high-affinity agonist binding at the beta2-adrenoceptor (beta2AR) expressed in Sf9 insect cel

47 In most studies, coupling of the beta2-adrenoceptor (beta2AR) to the stimulatory, heterot

48 beta2-Adrenoceptor (beta2AR)(-/-) FVB/NJ and wild-type F

49 that Vps34 is required for recycling of the beta2-adrenoceptor (beta2AR), a prototypical GPCR, and t

50 ists such as adrenaline, which activates the beta2-adrenoceptor (beta2AR), bind with relatively low a

51 ynamics simulations of lipid-embedded active beta2-adrenoceptor (beta2AR*) in complex with C-terminal

52 (-)-CGP 12177, a beta1- and beta2-adrenoceptor blocker that causes agonist effects t

53 Labetalol, a combined alpha1, beta1, and beta2 adrenoceptor-blocking drug, has been shown to have

54 ct by reducing salmeterol's affinity for the beta2-adrenoceptor by 31-fold.

55 l signaling and highlight the ability of the beta2-adrenoceptor/cAMP/PKA axis to rewire EphA2 signali

56 Prejunctional beta2-adrenoceptors can enhance neuronal acetylcholine r

57 Some blockers of beta1- and beta2-adrenoceptors cause cardiostimulant effects throug

58 is currently thought that activation of the beta2-adrenoceptor causes c-AMP dependent activation of

59 cyclase activity in cells expressing the CAM beta2-adrenoceptor correlated well with the level of exp

60 The CAM beta2-adrenoceptor displayed higher affinity for the ago

61 s was not observed after exposure of the CAM beta2-adrenoceptor-expressing cells to alprenolol, and a

62 embrane (TM) regions of the human beta1- and beta2-adrenoceptors, followed by single point mutations,

63 In contrast, arrestin-3 interaction with a beta2-adrenoceptor fused to the carboxyl-terminal tail o

64 Functionally relevant polymorphisms of the beta2-adrenoceptor gene (ADRB2) are common in white popu

65 tution at the 16 position (rs1042713) in the beta2-adrenoceptor gene (ADRB2) is associated with enhan

66 Beta2-adrenoceptors, however, are proportionally higher

67 f C57BL/6J mice, pharmacologic activation of beta2 adrenoceptors improved the severity of shock, incl

68 These results indicate that beta2-adrenoceptors in regulatory lymphocytes are critic

69 sponses to sustained stress are dependent on beta2-adrenoceptors in the CNS.

70 e potent compounds able to increase cAMP via beta2-adrenoceptors in U937 cells, and may have potentia

71 eoyldopamine were found to increase cAMP via beta2-adrenoceptors in U937 cells.

72 report evidence that agonist binding to the beta2 adrenoceptor induces a conformational change aroun

73 n of these amino acids to those found in the beta2-adrenoceptor (L195Q and W199Y), or mutation of a s

74 Despite the large up-regulation of CAM beta2-adrenoceptor levels, treatment with betaxolol did

75 ionship between structural properties of the beta2-adrenoceptor ligands and their interactions with m

76 orepinephrine, which then act on presynaptic beta2-adrenoceptors located on the neighboring nitrergic

77 Here, measurements of beta2-adrenoceptor-mediated cAMP accumulation and cAMP r

78 1-adrenoceptor-mediated vasoconstriction and beta2-adrenoceptor-mediated vasodilation.

79 evealed an intense distribution of beta1-and beta2-adrenoceptor mRNA in the BLA.

80 t both systems converge in the activation of beta2-adrenoceptors of splenic regulatory lymphocytes to

81 ects via their binding to the active site of beta2-adrenoceptors on ASM, which triggers a signaling c

82 to express stably either the wild-type human beta2-adrenoceptor or a constitutively active mutant (CA

83 not demonstrate up-regulation of either CAM beta2-adrenoceptor or G(Salpha) mRNA, and up-regulation

84 O had no effect on signaling and function of beta2-adrenoceptor or numerous procontractile GPCRs, but

85 ptors, reduced homologous desensitization of beta2-adrenoceptors) or AMP-independent mechanisms (e.g.

86 sion levels of both beta-adrenoceptors, with beta2-adrenoceptors outnumbering beta1-adrenoceptors in

87 Here we show that activation of beta2-adrenoceptors promoted STD long-term synaptic pote

88 AMP-dependent (e.g., increased expression of beta2-adrenoceptors, reduced homologous desensitization

89 Half-maximal up-regulation of the CAM beta2-adrenoceptor required concentrations of betaxolol

90 determine the exact amino acids in the human beta2-adrenoceptor responsible for this very high select

91 e protein LMBRD2 as a potential regulator of beta2 adrenoceptor signaling, underscoring the value of

92 ild-type mice selectively increased (40-60%) beta2-adrenoceptor signaling and function.

93 timulation mediated via canonical beta1- and beta2-adrenoceptor signaling pathways; and (5) evidence

94 ity to enforce the specificity of beta1- and beta2-adrenoceptor signaling.

95 ransregulation of M2 muscarinic receptors by beta2-adrenoceptor stimulation can be demonstrated at th

96 The pathway involves activation of beta2-adrenoceptors that increase cAMP levels and activa

97 Desensitization of beta2-adrenoceptors that occurs during the first few day

98 y engineering phosphorylation sites into the beta2-adrenoceptor the receptor showed prolonged interac

99 y agonists induce a chemical modification in beta2-adrenoceptors (via phosphorylation) that reduces a

100 Betaxolol-mediated up-regulation of the CAM beta2-adrenoceptor was both time and concentration depen

101 en a phosphorylation-deficient mutant of the beta2-adrenoceptor was used.

102 A series of mutant beta2 adrenoceptors with a limited number of cysteines a

103 Pretreatment of cells harboring the CAM beta2-adrenoceptor with betaxolol resulted in a large (4

104 growth factor receptor (EGFR) with EGF, the beta2-adrenoceptor with dopamine, or the hepatocyte grow

105 Stimulation of beta2-adrenoceptors with the selective beta2 agonist pro