ライフサイエンスコーパス: imidazoline

1 r only part of the secretory response to the imidazoline.

2 ecretion evoked by glucose, tolbutamide, and imidazolines.

3 o nonsymmetric cis-stilbene diamines and cis-imidazolines.

4 ides react with the sulfur ylides to provide imidazolines.

5 We, therefore, assayed a pure imidazoline 1 agonist, LNP599, which generated an effect

6 Moxonidine, has high affinity for imidazoline 1 receptors.

7 that ImP caused atherosclerosis through the imidazoline-1 receptor (I1R, also known as nischarin) in

8 he NO-scavenger 2-phenyl-4,4,5,5-tetramethyl-imidazoline-1-oxyl 3-oxide (PTIO).By blocking the activi

9 ited by carboxy-2-phenyl-4,4,5,5-tetramethyl-imidazoline-1-oxyl-3-oxide (-85.0 +/- 10.0%; p = 0.008)

10 nger 2-(4-carboxyphenyl)-4,4,5,5-tetramethyl-imidazoline-1-oxyl-3-oxide (PTIO) had opposite effects,

11 oxide scavenger 2-phenyl-4,4,5,5-ketramethyl-imidazoline-1-oxyl-3-oxide or by the nitric oxide syntha

12 , or 2-(4-carboxyphenyl)-4,4,5,5-tetramethyl-imidazoline-1-oxyl-3-oxide potassium (cPTIO), a NO scave

13 helator carboxy-2-phenyl-4,4,5,5-tetramethyl-imidazoline-1-oxyl-3-oxide, mitochondrial hyperpolarizat

14 be blocked by 2-phenyl-4,4,5, 5-tetramethyl-imidazoline-1-oxyl-oxide and could not be mimicked by de

15 Imidazoline 14 is a competitive adenosine A1 receptor an

16 atment of cancer cells with the noncytotoxic imidazoline 1d (10 nM) resulted in a significant increas

17 Our results indicate that the imidazoline 1d modulates the pro-survival NF-kappaB path

18 sation chemistry of pyrroline 1 (X = CH(2)), imidazoline 2 (X = NH), and 2-oxazoline 3 (X = O).

19 nglia and brainstem; therefore, by measuring imidazoline 2 binding site levels we can indirectly eval

20 Imidazoline 2 binding sites are expressed on activated a

21 nd with high specificity and selectivity for imidazoline 2 binding sites.

22 008, a novel astrocytic PET ligand targeting imidazoline-2 binding sites (I(2)BS) on astrocytes, migh

23 the first example of an iodonium complex of imidazoline-2-selone derivatives, while [L1(mu-Se)](I)(2

24 ynthesized 2-[(5-methylbenz-1-ox-4-azin-6-yl)imidazoline, 3, a potent, peripherally acting alpha 2 ad

25 7,10-tetraazacyclododecane, 1) utilizing bis-imidazoline, 6 (1,1'-ethylenedi-2-imidazoline), with 1,2

26 is replaced by an appropriately substituted imidazoline, a 1,2,4- or 1,3,4-oxadiazole, or an alkylat

27 ll as for other phenethylamines, but not for imidazolines, a class of structurally distinct alpha ago

28 ,5,6-tetrahydropyrimidine, H(2)bim = 2,2'-bi-imidazoline, acac = 2,4-pentandionato, py-imH = 2-(2'-py

29 is generated in response to the putative I1-imidazoline agonist moxonidine.

30 observed with catecholamines, azepines, and imidazolines albeit to different degrees.

31 pletely blocked by pretreatment with the non-imidazoline alpha(2)AR-antagonist, SKF86466 (0.5 or 1.0

32 evious report that the 2-(substituted-benzyl)imidazoline alpha-adrenergic agonist oxymetazoline (8) b

33 as prevented by idazoxan (5 mg/kg, i.p.), an imidazoline/alpha(2)-adrenoeceptor receptor antagonist.

34 in addition to effects on the KATP channel, imidazolines also interact with a more distal component

35 The dihydrothiazole and imidazoline analogues, 5-7, displayed moderate GAT activ

36 A methyl imidazoline and a dimethylamide are good alternatives fo

37 thus has structural similarity to ligands of imidazoline and alpha-2 adrenoceptors (alpha-2 AR).

38 Idazoxan, a mixed antagonist of imidazoline and alpha-2 adrenoceptors, partly inhibited

39 ated NO production and could be inhibited by imidazoline and alpha-2 AR antagonists, thus indicating

40 operties of the series of 2,2,5,5-tetraalkyl imidazoline and imidazolidine nitroxides were investigat

41 Adducts of 1-alkyl-2-imidazolines and two molecules of alkyl propiolate, poss

42 Union of Pharmacology), includes imidazole, imidazoline, and related compounds.

43 s, and activated olefins to form oxazolines, imidazolines, and pyrrolines, respectively.

44 Novel tricyclic imidazoline antagonists of the adenosine A1 receptor are

45 Due to the variety of available imidazoline-based precursors to this ligand, its steric

46 hesis and biological activity of a series of imidazoline-based scaffolds as potent inhibitors of NF-k

47 The imidazoline binding domain is encompassed within a regio

48 Identification of an imidazoline binding domain on MAO-B provides a new oppor

49 To localize the imidazoline binding domain on MAO-B, we labeled the doma

50 immunoprecipitation of labeled peptides, the imidazoline binding domain was localized to residues K14

51 entified B-CK to be the approximately 45 kDa imidazoline binding protein and we have demonstrated the

52 port the isolation of a approximately 45 kDa imidazoline binding protein from rabbit and rat brain us

53 uencing of the isolated approximately 45 kDa imidazoline binding protein, we identified it to be brai

54 Drugs that bind to imidazoline binding proteins have major physiological ac

55 ntly identified as a member of the family of imidazoline binding proteins.

56 opment of a PET radioligand selective for I2-imidazoline binding sites (I2BS) would enable, for the f

57 The I1-subtype of imidazoline binding sites has been characterized concern

58 Pheochromocytoma PC12 cells express I1-imidazoline binding sites in plasma membrane and lack al

59 nomolar) affinity for both type 1 and type 2 imidazoline binding sites, and the synthetic standards w

60 he structure of the endogenous ligand(s) for imidazoline binding sites, clonidine-displacing substanc

61 as developed to preferentially interact with imidazoline binding sites, it requires the alpha(2A)-AR

62 tudy based on 2-[3-azaspiro(5,5)undecanol]-2-imidazoline (BL-1743) was initiated.

63 ["Imidazoline," by consensus (International Union of Pharm

64 In particular, for the imidazoline catalyst, the (+)ESI-MS/(MS) detection of th

65 we observed effects that indicated that the imidazoline class of p38 MAPK inhibitors prevented nucle

66 , an alpha1-adrenoceptor (AR) agonist of the imidazoline class.

67 lectron transfer (PCET) reactions in iron bi-imidazoline complexes is presented.

68 Moxonidine is a centrally-active imidazoline compound with preferential affinity for imid

69 ucose, the sulfonylurea tolbutamide, and the imidazoline compounds efaroxan and phentolamine.

70 by scientists at Hoffmann-La Roche that cis-imidazolines could disrupt the protein-protein interacti

71 Initially, potent imidazoline derivatives were studied, but these compound

72 er different conditions to yield aminoether, imidazoline, diamine and amino bromine.

73 te) and FeII(H2bim) (iron(II) tris[2,2'-bi-2-imidazoline]diperchlorate) both transfer H* to TEMPO (2,

74 AA-RP acts at I-Rs, and because few (if any) imidazolines exist in vivo, we have adopted the term "im

75 e with Asp189 in the S1 pocket and the basic imidazoline fits snugly into the S4 site.

76 bond with the formation of acetophenone and imidazoline fragments.

77 Additionally, a base-catalyzed formation of imidazolines from a nitrile and ethylenediamine was also

78 sequences with hydrogen bonds involving one imidazoline group and the carbazole NH.

79 s in a more "classical" model that uses both imidazoline groups for H-bonding while the carbazole NH

80 ither the 3,6 or 2,7 positions with cationic imidazoline groups gave conclusive, but very surprising,

81 the potential pharmacological development of imidazoline/guanidinium compounds and also presents addi

82 Chiral nonracemic cis-4,5-bis(aryl)imidazolines have emerged as a powerful platform for the

83 Imidazolines have wild-type potencies and intrinsic acti

84 ds for the enantioselective synthesis of cis-imidazolines, however, has limited their more general us

85 002 HCl (2-[2-(2-Methoxy-1,4-benzodioxanyl)] imidazoline hydrochloride; 0.25 mg/kg, i.v.).

86 Targeting the imidazoline I(2) receptor emerges as a new mechanism of

87 This study examined whether a novel imidazoline I(2) receptor ligand CR4056 could serve as a

88 ey all share low micromolar affinity for the imidazoline I(2) receptor, while being devoid of any sig

89 Imidazoline I(2) receptors (I(2)-IR), widely distributed

90 Imidazoline I(2) receptors (I(2)-IRs) are altered in Alz

91 al specificity and appears to be mediated by imidazoline I(2) receptors.

92 Imidazoline (I) receptors have been implicated in the re

93 Changes in the density of imidazoline-I(2) binding sites have been observed in a r

94 olefin in MeCN at room temperature produced imidazoline in high yield.

95 der mild conditions and provides Se-arylated imidazolines in moderate to high yields.

96 es, and 2) a further analysis of the role of imidazolines in the control of insulin release.

97 es, and diamines provides access to 2-aryl-2-imidazolines in yields up to 96%.

98 sed to prepare a wide variety of enantiopure imidazolines, in a modular fashion, from readily availab

99 aroxan or phentolamine selectively inhibited imidazoline-induced insulin secretion but not the secret

100 yme-bound structure of ZK-816042, an amidine-imidazoline inhibitor of human factor Xa (FXa).

101 ought to include the formation of a hydrated imidazoline intermediate.

102 equent proton migrations in zwitterionic His imidazoline intermediates that reform the COOH group and

103 The transformation of 2-imidazolines into 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazi

104 egioselective N-arylation of a 4-substituted imidazoline is reported.

105 e one-pot synthesis of tetrafunctionalized 2-imidazolines is described.

106 The first copper-catalyzed N-arylation of 2-imidazolines is described.

107 enry strategy for preparing nonsymmetric cis-imidazolines is illustrated by a comparison of the roles

108 eparation of enantiopure 1,4-disubstituted 2-imidazolines is reported.

109 ed methamphetamine, ketamine, the endogenous imidazoline ligand agmatine, the monoamine oxidase (MAO)

110 and a phenanthroline ligand or a new pyridyl-imidazoline ligand that further increases the regioselec

111 We studied the effect of moxonidine, an imidazoline ligand, on metabolic and hemodynamic paramet

112 d amine derivatives, using a new pyridinebis(imidazoline) ligand, a copper catalyst and base.

113 nd computational studies on bi-oxazoline and imidazoline ligands, we reveal that a square planar geom

114 drenergic receptors, which recognize many I1-imidazoline ligands.

115 axial chirality and central chirality, (ii) imidazoline moiety over oxazoline moiety, and (iii) phos

116 om 1a undergoes spontaneous isomerization by imidazoline N-H migration, re-forming the COOH group and

117 nalyses of bidentate pyridyl, oxazoline, and imidazoline nitrogen ligands, along with their correspon

118 An approach to the synthesis of new imidazoline nitroxides bearing an N',N'-disubstituted am

119 r 4- and 5-azido analogues; imidazolidine, 4-imidazoline or 4-thiazoline; and N-unsubstituted imine,

120 ocked by the NO scavenger phenyl-tetramethyl-imidazoline-oxyl-oxide as well as by the PKC inhibitor s

121 ain on MAO-B, we labeled the domain with the imidazoline photoaffinity adduct [125I]2-(3-azido-4-iodo

122 ions of 3-trichloromethyl and dichloromethyl imidazoline products (16 examples).

123 on of access to cis-stilbene diamine-derived imidazolines provided by this platform should streamline

124 H group onto the His imidazole ring, forming imidazoline radical intermediates.

125 onors wherein the active doping species, the imidazoline radical, is generated in a postdeposition th

126 Efaroxan, like several other imidazoline reagents, elicits a glucose-dependent increa

127 ), the H2 histamine receptor antagonist with imidazoline receptor activating properties, prevented th

128 ipating in the physiological responses to I1-imidazoline receptor activation.

129 ha2-AR) agonist guanabenz, but not by the Ih-imidazoline receptor agonists moxonidine or rilmenidine.

130 Nischarin, or imidazoline receptor antisera-selected protein, is a pro

131 contrast, pretreatment with the specific I1 imidazoline receptor blocker, efaroxan (100-500 microg;

132 ion, i.c.v. or i.v. pretreatment with the I1-imidazoline receptor blocker, efaroxan, failed to inhibi

133 We hypothesized that the I1-imidazoline receptor couples to a phosphatidylcholine-se

134 Desensitization of the imidazoline receptor following exposure to high concentr

135 te signal transduction pathways for the I(1)-imidazoline receptor in PC12 cells and their interaction

136 The I1-imidazoline receptor is expressed in the rostral ventrol

137 In addition, the imidazoline receptor ligands, BU-226 and AGN-192403 did

138 vous system with a polyclonal antibody to an imidazoline receptor protein (IRP) with binding characte

139 Stimulation of the I(1)-imidazoline receptor with moxonidine, a centrally acting

140 line compound with preferential affinity for imidazoline receptors (IR) over alpha(2)-adrenoceptors (

141 e cross-reactivity of alpha2AR agonists with imidazoline receptors has precluded an understanding of

142 Putative imidazoline receptors have a unique distribution pattern

143 rgic receptors, but not via activation of I1-imidazoline receptors in conscious cats.

144 ated through activation of the I1 subtype of imidazoline receptors in conscious cats.

145 Binding of idazoxan (IDA) to imidazoline receptors of the I2 subtype in astrocytes in

146 ity and selectivity of some compounds for I1 imidazoline receptors over alpha2-adreergic receptors.

147 These findings suggest coupling of I1-imidazoline receptors to a phospholipase C to generate D

148 nd tested for their binding properties on I1 imidazoline receptors vs alpha2-adrenergic receptors and

149 ine is known to bind to alpha-adrenergic and imidazoline receptors, it has been suggested that some o

150 receptors and not through H2-histamine or I1-imidazoline receptors.

151 yperthermic effect of morphine by activating imidazoline receptors.

152 by patients treated with clonidine and other imidazoline-related drugs.

153 se to term this common approach the hydrated imidazoline ring expansion (HIRE) reaction.

154 The hydrated imidazoline ring expansion (HIRE-type) reaction was inve

155 tionic charge density into the five-membered imidazoline ring.

156 s with a distribution of orientations of the imidazoline ring.

157 As anticipated, the naphthalene and imidazoline rings of PIN-acac complexes 18a and 18b were

158 sion strategy involving hydrolytically prone imidazoline rings was thought to include the formation o

159 The imidazoline site agonists, agmatine (150mg/kg, i.p.) and

160 ha(2)-adrenoceptor agonists does not involve imidazoline sites but rather the activation of alpha(2)-

161 ion/deprotonation process for a pH-sensitive imidazoline spin label in aqueous solution where the exc

162 gnificantly from planarity and projected the imidazoline substituents R(1) and R(2) on opposite faces

163 ation of P53 in tumor cells by Nutlin, a cis-imidazoline that inhibits the Hdm2-P53 interaction.

164 to prepare highly substituted cis-4,5-diaryl imidazolines that project unique aromatic rings, and the

165 nd, BL-1743 (2-[3-azaspiro (5,5)undecanol]-2-imidazoline), that inhibits influenza virus growth was i

166 CF(3)) in combination with an imidazolidine, imidazoline, thiazolidine, or thiazoline heterocycle.

167 e complexes were photolyzed with N-protected imidazolines to give protected azapenams.

168 residues are involved in the binding of all imidazoline-type agonists such as oxymetazoline, cirazol

169 alkyl group derives from the substrate; this imidazoline undergoes further reaction in situ to afford

170 hloroethylamidines, which are converted into imidazolines upon workup with aqueous hydroxide.

171 The mechanisms of action of imidazolines were examined in more detail.

172 A series of 2'-alkylthio-2-(anilinomethyl)imidazolines were prepared to examine the effect of the

173 A catalytic asymmetric synthesis of imidazolines with a fully substituted beta-carbon atom b

174 N-Arylation of 2-imidazolines with arylboronic acids promoted by copper(I

175 iamagnetic 4-R-amino-1,2,2,5,5-pentamethyl-3-imidazolines with bromoacetic acid ethyl ester; the prod

176 A pseudo-three-component reaction of 2-imidazolines with terminal electron-deficient alkynes (2

177 lizing bis-imidazoline, 6 (1,1'-ethylenedi-2-imidazoline), with 1,2-dibromoethane.