ライフサイエンスコーパス: alpha-2 adrenoceptor

1 tionalized by the binding site models of the alpha 2-adrenoceptor.

2 than the desired decreased, affinity for the alpha 2-adrenoceptor.

3 d and evaluated for activity at alpha 1- and alpha 2-adrenoceptors.

4 potent and selective agonist activity at the alpha 2-adrenoceptors.

5 en prepared and evaluated as ligands for the alpha(2) adrenoceptor.

6 ) results in a reduction in affinity for the alpha(2)-adrenoceptor.

7 elective due to significant affinity for the alpha(2)-adrenoceptor.

8 highly selective due to low affinity for the alpha(2)-adrenoceptor.

9 NMT) inhibitory potency and affinity for the alpha(2)-adrenoceptor.

10 itors of PNMT and for their affinity for the alpha(2)-adrenoceptor.

11 sion via mechanisms that are specific to the alpha(2)-adrenoceptor.

12 nhibitors of the binding of clonidine at the alpha(2)-adrenoceptor.

13 isplay the opposite stereoselectivity at the alpha(2)-adrenoceptor.

14 d and evaluated for affinity at PNMT and the alpha(2)-adrenoceptor.

15 nhibitors of the binding of clonidine at the alpha(2)-adrenoceptor.

16 was mediated by N-methyl-D-aspartate and/or alpha(2)-adrenoceptors.

17 idazoline sites but rather the activation of alpha(2)-adrenoceptors.

18 hanism of action of the drug is to stimulate alpha(2)-adrenoceptors.

19 action which likely involves stimulation of alpha(2)-adrenoceptors.

20 esent study investigated the hypothesis that alpha(2)-adrenoceptor activation inhibits icilin-induced

21 These results suggest that alpha(2)-adrenoceptor activation inhibits shaking induce

22 the innate vascular response to alpha(1)- or alpha(2)-adrenoceptor activation.

23 lethanolamine N-methyltransferase (PNMT) and alpha(2)-adrenoceptor affinities were predicted through

24 c ring, showed poor PNMT affinity and modest alpha 2-adrenoceptor affinity (PNMT Ki = 330 microM, alp

25 reduced selectivity on account of increased alpha 2-adrenoceptor affinity as compared to 1 (PNMT Ki

26 ce as the acidic NH of 1, exhibited the best alpha 2-adrenoceptor affinity of any of the compounds st

27 uent was found to have a major effect on the alpha(2)-adrenoceptor affinity of these compounds with t

28 drenoceptor, while the latter were devoid of alpha(2)-adrenoceptor affinity, but also lost potency at

29 midazoline, 3, a potent, peripherally acting alpha 2 adrenoceptor agonist.

30 ut little heterologous desensitization to an alpha 2-adrenoceptor agonist (UK 14304) or somatostatin.

31 In combination with carbachol, the alpha 2-adrenoceptor agonist brimonidine elicited large

32 Clonidine is a centrally active alpha 2-adrenoceptor agonist that raises concentrations

33 ), an analogue of 2 (Bay a6781), is a potent alpha(2) adrenoceptor agonist.

34 anol abolishes the hypotensive effect of the alpha(2)-adrenoceptor agonist clonidine in this rat mode

35 noamine oxidase (MAO) inhibitor harmane, the alpha(2)-adrenoceptor agonist clonidine, the mu-opioid r

36 tudy, we examined the effect of brimonidine (alpha(2)-adrenoceptor agonist) on RGC survival after inc

37 Brimonidine, a selective alpha(2)-adrenoceptor agonist, has recently been shown t

38 fects of dexmedetomidine, a highly selective alpha(2)-adrenoceptor agonist, on extracellular dopamine

39 Pretreatment with a peripherally restricted alpha(2)-adrenoceptor agonist, ST91 (0.075, 0.15 mg/kg),

40 ization induced by opioid, somatostatin, and alpha 2-adrenoceptor agonists was studied in brain slice

41 e demonstrated that the analgesic actions of alpha(2) adrenoceptor agonists are mediated by the alpha

42 nd -thiazoles were prepared and evaluated as alpha(2) adrenoceptor agonists.

43 the notion that the protective action of the alpha(2)-adrenoceptor agonists does not involve imidazol

44 In addition, the neuroprotective effect of alpha(2)-adrenoceptor agonists in the retina may involve

45 n between the effectiveness of the different alpha(2)-adrenoceptor agonists was not possible.

46 Other alpha(2)-adrenoceptor agonists, brimonidine and apraclon

47 dy is that the neuroprotective properties of alpha(2)-adrenoceptor agonists, like clonidine, are very

48 alpha(2)-adrenoceptor agonists, such as clonidine, atten

49 sponses evoked in the finger by alpha(1)- or alpha(2)-adrenoceptor agonists.

50 Alpha-2 adrenoceptor agonists (e.g., clonidine) are effe

51 nt clinical trial study show the efficacy of alpha-2 adrenoceptor agonists in decreasing stress-induc

52 e effects of prolonged stimulation of MOR on alpha(2)-adrenoceptor (alpha(2)-AR) function.

53 affinity for imidazoline receptors (IR) over alpha(2)-adrenoceptors (alpha(2)AR).

54 ral similarity to ligands of imidazoline and alpha-2 adrenoceptors (alpha-2 AR).

55 analog 5a showed significant selectivity for alpha 2-adrenoceptors and behaved as a partial alpha 1-a

56 n this study, the anatomical distribution of alpha 2-adrenoceptors and its relationship to the distri

57 methyl-THIQs are too potent (too hot) at the alpha(2)-adrenoceptor and the 3-trifluoromethyl-THIQs ar

58 1,2,3,4-tetrahydroisoquinoline (THIQ) at the alpha(2)-adrenoceptor and to the decreased pK(a) of the

59 zed Wistar rats, we have studied the role of alpha(2)-adrenoceptors and neuropeptide Y (NPY) Y(1) rec

60 he present study to examine whether specific alpha-2 adrenoceptor antagonism would protect against le

61 gonist atropine, but was not affected by the alpha 2-adrenoceptor antagonist yohimbine, the serotoner

62 by a selective alpha 1- but not a selective alpha 2-adrenoceptor antagonist.

63 The alpha(1) adrenoceptor antagonist WB4101, alpha(2) adrenoceptor antagonist yohimbine and mu-opioid

64 Systemic administration of the alpha(2)-adrenoceptor antagonist yohimbine (YO) activate

65 idence of local noradrenaline release as the alpha(2)-adrenoceptor antagonist yohimbine increased the

66 ly reversed antinociception, but neither the alpha(2)-adrenoceptor antagonist yohimbine nor the alpha

67 ease was stimulated by administration of the alpha(2)-adrenoceptor antagonist yohimbine.

68 a(1)-adrenoceptor antagonist), yohimbine (an alpha(2)-adrenoceptor antagonist) and phentolamine (a no

69 Yohimbine (Yoh, alpha(2)-adrenoceptor antagonist) or BIBP 3226 (Y(1)-rec

70 nt and co-infusion with the highly selective alpha(2)-adrenoceptor antagonist, atipamezole (ATZ).

71 ral noradrenergic tone using atipamezole, an alpha-2 adrenoceptor antagonist, could induce a long-ter

72 by intrathecal administration of yohimbine (alpha-2-adrenoceptor antagonist).

73 lpha 1-adrenoceptor antagonist prazosin, the alpha 2-adrenoceptor antagonists idazoxan and yohimbine,

74 effect of clonidine was attenuated when the alpha(2)-adrenoceptor antagonists yohimbine or rauwolsci

75 Alpha-2 adrenoceptors are widely distributed in vascular

76 alin analogs had a distinct influence on the alpha 2-adrenoceptor binding affinity.

77 ceptor modeling were combined to rationalize alpha 2-adrenoceptor binding data of the imidazole analo

78 4-Methylindan analog 6 was the most potent alpha 2-adrenoceptor binding ligand among these 4-substi

79 In addition, this study suggests that alpha 2-adrenoceptors blocked by yohimbine injected I.C.

80 ese results show that stimulation of central alpha 2-adrenoceptors by clonidine attenuates the cardio

81 In contrast, stimulation of endogenous alpha(2)-adrenoceptors by norepinephrine produced stable

82 dicate that vasoconstricting post-junctional alpha(2)-adrenoceptors contribute more to basal vascular

83 ding of [125I]p-iodoclonidine ([125I]PIC) to alpha 2-adrenoceptors coordinately with counts of neurom

84 fit into the proposed "methyl pocket" of the alpha 2-adrenoceptor defined by the residues Leu110, Leu

85 more potent enantiomer at both PNMT and the alpha(2)-adrenoceptor for these 3-fluoromethyl-, 3-hydro

86 er insight into central neurotransmitter and alpha 2-adrenoceptor-hypothalamic abnormalities in MSA.

87 e levodopa studies they indicated a specific alpha 2-adrenoceptor-hypothalamic deficit in MSA.

88 agent has demonstrated good selectivity for alpha 2 adrenoceptors in binding and functional studies.

89 The uneven distribution of alpha 2-adrenoceptors in the LC demonstrates the importa

90 epinephrine mediates the analgesic action at alpha(2) adrenoceptors in the spinal cord, we now invest

91 e findings do not favor a role for brainstem alpha(2)-adrenoceptors in ethanol-induced attenuation of

92 the density (B(max)) and affinity (K(D)) of alpha(2)-adrenoceptors in the middle (mNTS) and rostral

93 r inhibits nociception through the action of alpha(2)-adrenoceptors in the spinal cord dorsal horn.

94 mers of these compounds at both PNMT and the alpha(2)-adrenoceptor indicates that both sites display

95 mode for phenethylamines and imidazoles with alpha 2-adrenoceptors is proposed.

96 greater than 0.57 and display selectivities (alpha(2)-adrenoceptor K(i)/PNMT K(i)) greater than 200 a

97 ors in this study and display selectivities (alpha(2)-adrenoceptor K(i)/PNMT K(i)) greater than 200.

98 most selective inhibitors of PNMT versus the alpha(2)-adrenoceptor known.

99 ata we propose that exogenous and endogenous alpha(2) adrenoceptor ligands activate different alpha(2

100 Both alpha(1)- and alpha(2)-adrenoceptors mediate these vascular responses

101 onstrated that post-junctional alpha(1)- and alpha(2)-adrenoceptors mediate vasoconstriction in the h

102 he mu-opioid response, with no change in the alpha 2 adrenoceptor-mediated response.

103 These data provide the first evidence for alpha(2)-adrenoceptor-mediated constriction in slow-twit

104 In rat locus coeruleus (LC) neurons, alpha 2 adrenoceptors, mu-opioid and somatostatin recept

105 These results indicate that neither alpha(2)-adrenoceptors nor Y(1) receptors contribute to

106 zoxan, a mixed antagonist of imidazoline and alpha-2 adrenoceptors, partly inhibited L-arginine-initi

107 acids found in the homologous domain of the alpha 2 adrenoceptor (Phe, Phe, Phe).

108 T in comparison with its affinity toward the alpha 2-adrenoceptor (PNMT Ki = 0.55 microM, alpha 2 Ki

109 P accumulation by modifying alpha(1)- and/or alpha(2)-adrenoceptor rather than beta-adrenoceptor sign

110 activation did not alter desensitization of alpha 2-adrenoceptor responses.

111 14,304 to selectively activate alpha(1)- or alpha(2)-adrenoceptors resulted in concentration-depende

112 mong these 4-substituted imidazoles, and its alpha 2-adrenoceptor selectivity was greater than the 5-

113 genistein appears to involve modification of alpha(2)-adrenoceptor signaling mechanisms.

114 increases in peripheral, as well as central, alpha(2)-adrenoceptor signaling oppose the behavioral st

115 By contrast, alpha(2)-adrenoceptor stimulation evokes finger vasocons

116 ponsible for this analgesic action and which alpha(2) adrenoceptor subtype mediates this property.

117 Null mice for each of the three alpha(2) adrenoceptor subtypes (alpha(2A), alpha(2B), an

118 a(2) adrenoceptor ligands activate different alpha(2) adrenoceptor subtypes to produce their analgesi

119 In addition to excellent binding at the alpha(2D) adrenoceptor, the 4-bromo analogues 20e and 21

120 rain to quantify the density and affinity of alpha 2 adrenoceptors under condition of changing radiol

121 reochemical preferences of both PNMT and the alpha(2)-adrenoceptor, which should assist in the develo

122 PNMT due to their decreased affinity for the alpha(2)-adrenoceptor, which was attributed to steric bu

123 Analogous to the effects of alpha(2)-adrenoceptors, which also act prejunctionally t

124 n Ca(V)2.2 inhibition by norepinephrine (via alpha(2)-adrenoceptors, which do not bind NHERF2), nor o

125 elective due to significant affinity for the alpha(2)-adrenoceptor, while the latter were devoid of a