ライフサイエンスコーパス: competitive antagonist

1 phobic group (VPC12249) was a dual LPA1/LPA3 competitive antagonist.

2 A) resulting in alpha-hel-CRF being a potent competitive antagonist.

3 sitization, or, alternatively, function as a competitive antagonist.

4 oning is observed with both an agonist and a competitive antagonist.

5 two full agonists and a full agonist plus a competitive antagonist.

6 ceptor at 3.6 A resolution in complex with a competitive antagonist.

7 evelopment of subunit selective agonists and competitive antagonists.

8 activity, inverse agonists behave as simple competitive antagonists.

9 are resistant to Mg2+, MK-801, memantine and competitive antagonists.

10 ns key binding determinants for agonists and competitive antagonists.

11 ut inhibitable by subsequent exposure to non-competitive antagonists.

12 harged ammonium group common to agonists and competitive antagonists.

13 acid residues that determine sensitivity to competitive antagonists.

14 relatively resistant to displacement by non-competitive antagonists.

15 d confers sensitivity to displacement by non-competitive antagonists.

16 5 potentiator binding to displacement by non-competitive antagonists.

17 r JNK1 activation compared with conventional competitive antagonists.

18 sts that two of the five compounds behave as competitive antagonists.

19 Here, we determined inhibition by pairs of competitive antagonists.

20 ntagonists but not by the AMPA-selective non-competitive antagonist 1-(4-aminophenyl)-4-methyl-7,8-me

21 in inhibition and were not observed with the competitive antagonist (1,2,5,6-tetrahydropyridin-4-yl)-

22 Application of the competitive antagonist 2',3'-O-(2,4,6-trinitrophenyl)-AT

23 nition by human P2Y1 receptors of the novel, competitive antagonist 2'-deoxy-N6-methyladenosine 3', 5

24 unbinding rate, which was measured using the competitive antagonist 2-(3-carboxypropyl)-3-amino-6-(4-

25 rth [postnatal day 0 (P0)] by suspending the competitive antagonist 2-amino-5-phosphonopentanoic acid

26 found that occupation of the receptor by the competitive antagonist 2-nonanone protected the receptor

27 ography, using the agonist glutamate and the competitive antagonist [(+/-)-2-carboxypiperazin-4-yl] p

28 Another competitive antagonist, 2-amino-5-phosphonovaleric acid,

29 cognition site of the NMDA receptor with the competitive antagonist 3-(2-carboxypiperazin-4-yl)propyl

30 Although the rho1 competitive antagonist 3-aminopropyl(methyl)-phosphinic

31 The competitive antagonist 3-aminopropyl(methyl)phosphinic a

32 ease in the IC(50) was also observed for the competitive antagonist 3-APMPA, but not for the non-comp

33 We used the NMDA receptor non-competitive antagonist, [3H]MK-801, as a ligand for an a

34 sCD40R, and has been shown to function as a competitive antagonist against CD40 activation.

35 Competitive antagonists against N-methyl-D-aspartate (NM

36 ubunit tetramers soon after the site for the competitive antagonist alpha-bungarotoxin has formed and

37 The competitive antagonist alpha-conotoxin-MII (alpha-CTx-MI

38 23) led to a high-affinity, RXFP3-selective, competitive antagonist (analogue 3).

39 [(3)H]Bz(2)choline acts as an nAChR competitive antagonist and binds at equilibrium with the

40 Derquantel behaved as a competitive antagonist and distinguished M-nAChRs activa

41 ated conformations solved for complexes with competitive antagonists and a lack of understanding of t

42 ation, desensitization and inhibition by non-competitive antagonists and pore blockers.

43 as fully blocked by picrotoxin but not GABAA competitive antagonists, and was strongly correlated wit

44 ich binding sites for nicotinic agonists and competitive antagonists are found at selected subunit in

45 teric pharmacology and those that are simply competitive antagonists are subtle and intriguing.

46 Bicuculline (100 microM), a competitive antagonist at GABA(A) receptors, reduced NMD

47 c currents in the presence of a low-affinity competitive antagonist at glycine receptors [2-(3-carbox

48 is a structural analogue of strychnine and a competitive antagonist at ionotropic glycine receptors (

49 THRX-198321 was a competitive antagonist at mAChR (M(2) pK(B) = 9.98 +/- 0

50 st at receptors containing NR1(D732G), and a competitive antagonist at receptors containing NR1(D732)

51 ATP], suggesting that adenosine may act as a competitive antagonist at the adenine nucleotide binding

52 Caffeine is a competitive antagonist at the adenosine receptors, but i

53 e rP2Y(4) receptor but is a similarly potent competitive antagonist at the hP2Y(4) receptor.

54 assay showed that (1R,2S)-11 is a potent and competitive antagonist at the human D3 receptor.

55 Ketamine is a non-competitive antagonist at the N-methyl-d-aspartate recep

56 t dihydro-beta-erythroidine (DH beta E) is a competitive antagonist at the nAChR.

57 en cell and whole cell assays to behave as a competitive antagonist at the S1P(1) and S1P(3) receptor

58 though the intrathecal application of an NgR competitive antagonist at the time of spinal cord hemise

59 Decanoic acid acts as a non-competitive antagonist at therapeutically relevant conce

60 y of analogs of D-Ser and GluN1 glycine site competitive antagonists at GluD2 receptors containing th

61 mine, metocurine, and pancuronium) to act as competitive antagonists at mouse adult- and fetal-type m

62 fer the lower binding affinity seen for some competitive antagonists at the alpha-delta agonist site.

63 To understand interactions of competitive antagonists at the atomic structural level,

64 agonists of the human mu-opioid receptor and competitive antagonists at the kappa- and delta-opioid r

65 Newer competitive antagonists at the neuromuscular junction ha

66 hates previously were demonstrated to act as competitive antagonists at the P2Y1 receptor.

67 and tetramethylenedisulfotetramine, and the competitive antagonist bicuculline reduced fluorescence

68 cked by picrotoxin and, surprisingly, by the competitive antagonist bicuculline.

69 Lastly, the lipophilic competitive antagonist (+)bicuculline promoted receptor

70 Competitive antagonists bind directly to the integrin li

71 ucidate why DH, an agonist, and MSVIII-19, a competitive antagonist, bind selectively to glutamate re

72 This hypothesis predicts that competitive antagonist binding should require less activ

73 vanilloid sensitivity, [(3)H]RTX binding and competitive antagonist binding to rabbit TRPV1.

74 Alpha-Conotoxin MI, a 14-amino acid competitive antagonist, binds at both interfaces but has

75 Our results suggest that most competitive antagonists block native AMPA and kainate re

76 GluN1-GluN2B NMDA receptor in an ensemble of competitive antagonist-bound states, an agonist-bound fo

77 inding at the alpha-gamma site acts not as a competitive antagonist but as a coactivator or partial a

78 y of drugs, including nicotinic agonists and competitive antagonists, but previous studies have indic

79 many D5,L6 agonists could be converted into competitive antagonists by applying this motif, the most

80 than MTS alone, suggesting that binding of a competitive antagonist can cause movements in the bindin

81 Likewise, the competitive antagonist capsazepine inhibited RTX-induced

82 However, pretreatment with the competitive antagonist CGP-37849 attenuated acquisition

83 bsence of endogenous biological activity and competitive antagonist characteristics.

84 examine the site selectivity for four other competitive antagonists: cisatracurium, pancuronium, vec

85 owed efficacy similar to a full agonist, and competitive antagonists CNQX and DNQX acted as a partial

86 ChR, photoaffinity-labeling studies with the competitive antagonist d-[(3)H]tubocurarine (dTC) identi

87 The competitive antagonist d-tubocurarine (curare) has great

88 ace, but decreases receptor affinity for the competitive antagonist d-tubocurarine (dTC) 5-35-fold.

89 as no effect on the apparent affinity of the competitive antagonist d-tubocurarine (dTC) for the rece

90 rotected from modification by the reversible competitive antagonist d-tubocurarine (dTC).

91 Modified channels are insensitive to the competitive antagonists D-2-amino-5-phosphonovaleric aci

92 agenesis were used to examine binding of the competitive antagonist, d-tubocurarine (dTC), to the mus

93 An agrin fragment that acts as a competitive antagonist depresses action potential freque

94 agonist alone, but we show that the classic competitive antagonist dihydro-beta-erythroidine inhibit

95 The affinity of the competitive antagonist dihydro-beta-erythroidine is >700

96 cotine, the partial agonist cytisine, or the competitive antagonist dihydro-beta-erythroidine; we als

97 subtype of glutamate receptors using the non-competitive antagonist dizocilpine maleate (MK801) arres

98 oietin 2 (Ang2) was originally shown to be a competitive antagonist for Ang1 of the receptor tyrosine

99 Here we show that acetylcholine is a competitive antagonist for ELIC.

100 ry from blockade of presynaptic NMDAr with a competitive antagonist, frequency-dependent facilitation

101 These compounds are based on the competitive antagonist gabazine and incorporate a variet

102 The agonist-competitive antagonist hybrids can be very useful for th

103 tration-response curves, whereas the agonist-competitive antagonist hybrids produce concentration-res

104 sons between the agonist RTX and the related competitive antagonist I-RTX.

105 P, and adenosine-2',5'-diphosphate also were competitive antagonists in studies with the cloned human

106 to functionally profile receptor kinetics of competitive antagonists in the absence of a labeled trac

107 ation disrupts high-affinity binding of many competitive antagonists in transfected cells.

108 ducible receptor expression system and a non-competitive antagonist, in conjunction with the transloc

109 e tissue-binding function of factor H with a competitive antagonist increased complement activation a

110 We also show that competitive antagonists induced distinct rearrangements

111 supported by the picrotoxin resistance of a competitive antagonist-induced fluorescence change.

112 Competitive antagonists inhibited only PI hydrolysis and

113 Like the competitive antagonists, intrastriatal infusion of the n

114 The major determinant of sensitivity to both competitive antagonists is located between residues 54 a

115 ing in various conditions, including CNQX, a competitive antagonist; kainate, a weak partial agonist;

116 at 180 nM while another (SCaM-1) served as a competitive antagonist (Ki approximately 120 nM) of this

117 pothesis in wild-type receptors, we used the competitive antagonist kynurenate, which has higher affi

118 The rapidly dissociating competitive antagonists kynurenate and L-2-amino-5-phosp

119 However, unlike competitive antagonists, local infusion of 1 mM MK-801 p

120 Eyes pretreated with the melatonin receptor competitive antagonist luzindole before the dark phase p

121 The resting state, stabilized by the competitive antagonist LY466195, closely resembles the c

122 the presence of high agonist concentrations, competitive antagonists may have the effect of shifting

123 micked by the agonist DHPG, abolished by the competitive antagonist MCPG, and partially inhibited by

124 agonists and changes the potency of the non-competitive antagonist mecamylamine.

125 receptor (AChR) was compared to that for the competitive antagonist methyllycaconitine (MLA).

126 deactivation kinetics and the effects of the competitive antagonist NVP-AAM077.

127 tyl]-L-arginine (SB 290157), functioned as a competitive antagonist of (125)I-C3a radioligand binding

128 GYKI 52466, a selective non-competitive antagonist of AMPA receptors, did not affect

129 currents (EPSCs) produced by a low-affinity competitive antagonist of AMPA receptors, gamma-DGG.

130 We appended a competitive antagonist of BET bromodomains to a phthalim

131 opening rate demonstrating that it acts as a competitive antagonist of CCh-mediated activation.

132 type I cGMP-dependent protein kinase, but a competitive antagonist of channel activation, it will be

133 elocytic leukemia (APL) and a small molecule competitive antagonist of CXCR4, AMD3100, to examine the

134 a and found in atherosclerotic lesions, is a competitive antagonist of estrogen receptor action in th

135 ed that the FHR1/FH hybrid protein acts as a competitive antagonist of FH.

136 The potency of Zn2+ as a non-competitive antagonist of GABA-activated responses on al

137 GHRH (0.001, 0.01, and 0.1 nmol/kg) or a competitive antagonist of GHRH (0.003, 0.3, and 14 nmol/

138 We used exendin-9,39, a competitive antagonist of GLP-1, to examine glucose meta

139 Exendin-(9,39) is a competitive antagonist of glucagon-like peptide-1 (GLP-1

140 owed synaptic decays, whereas a low-affinity competitive antagonist of glycine receptors (GlyRs) acce

141 eriments reported here show that L-lysine, a competitive antagonist of L-arginine uptake, suppressed

142 Furthermore, a competitive antagonist of L-arginine, N(G)-methyl-L-argi

143 ed proliferation was blocked by VPC-32179, a competitive antagonist of LPA(1) and LPA(3) receptors, a

144 l]-1,8-octane] diamine) is an M(2)-selective competitive antagonist of muscarinic acetylcholine recep

145 n intraperitoneal injection of MK-801, a non-competitive antagonist of N-methyl-d-aspartate (NMDA)-ac

146 gher affinity for ethylisopropylamiloride, a competitive antagonist of Na(+) o transport.

147 demonstrate that Con G is a subunit-specific competitive antagonist of NMDA receptors.

148 lcium ion channel receptor, and CGS 19755, a competitive antagonist of NMDA-type glutamate receptor.

149 Recently, an endogenous competitive antagonist of NO synthase has been character

150 CaM (wild type CaM (wtCaM)) and a selective competitive antagonist of NOS.

151 Groups of mice receiving CV-6209, a competitive antagonist of PAFr, had survival rates simil

152 PD-1 ectodomain as a high-affinity (110 pM) competitive antagonist of PD-L1.

153 as an inhibitor of fatty acid binding and a competitive antagonist of protein-protein interactions m

154 ethylisothiouronium)benzene (Br-TITU(3+)), a competitive antagonist of Rb(+) and Na(+) occlusion, was

155 receptor and is believed to act as a neutral competitive antagonist of receptor activation.

156 siological retinol metabolite that acts as a competitive antagonist of retinol, blocks cell activatio

157 We conclude that JYL1421 is a competitive antagonist of rVR1, blocking response to all

158 by three different nicotinic agonists and a competitive antagonist of several different nAChR subtyp

159 amily, sigma-conotoxin GVIIIA, is a specific competitive antagonist of the 5-HT3 receptor; thus, alph

160 T) is a highly selective, slowly reversible, competitive antagonist of the alpha3beta2 neuronal nicot

161 angiotensin II in this disorder, losartan (a competitive antagonist of the angiotensin II type 1 [AT1

162 heir chaperone activity and functioning as a competitive antagonist of the co-chaperone Hip.

163 e inactive antithrombin variant was a potent competitive antagonist of the heparin-catalyzed reaction

164 We also identified a competitive antagonist of the interaction of anandamide

165 (Wtx-1) is a 22-amino acid peptide that is a competitive antagonist of the muscle nicotinic receptor

166 -2-piperidine carboxylic acid (CGS 19755), a competitive antagonist of the N-methyl-d-aspartate (NMDA

167 The effects of the competitive antagonist of the N-methyl-D-aspartate (NMDA

168 o-7-sulfamoyl-benzo-(F)quinoxaline (NBQX), a competitive antagonist of the neuronal receptor for alph

169 tself distantly class I-like, that acts as a competitive antagonist of the NKG2D activating receptor.

170 The main action of phencyclidine is as a non-competitive antagonist of the NMDA class of glutamate re

171 In contrast, focal pretreatment of MD with a competitive antagonist of the NMDA receptor 2-amino-7-ph

172 ist of the NMDA receptor and of LY 235959, a competitive antagonist of the NMDA receptor on L-arginin

173 spartate (NMDA) receptor and of LY 235959, a competitive antagonist of the NMDA receptor on the analg

174 Phencyclidine (PCP), a non-competitive antagonist of the NMDA subtype of glutamate

175 The effect of MK-801, a non-competitive antagonist of the NMDA subtype of glutamate

176 d-Tubocurarine (dTC) is a potent competitive antagonist of the Torpedo nicotinic acetylch

177 blocked by pretreatment with capsazepine, a competitive antagonist of the vanilloid type 1 receptor.

178 Both forms act as competitive antagonists of alpha-melanocyte stimulating

179 Functionally, selective competitive antagonists of apelin receptor were shown to

180 Strategies to generate competitive antagonists of bioactive peptides include se

181 nstrate that these CFHR proteins function as competitive antagonists of CFH to modulate complement ac

182 binding from gating, we identified the first competitive antagonists of CNG channels: specific phosph

183 Anti-leukotrienes, which are competitive antagonists of cysteinyl-leukotriene-1 recep

184 ing system and with two different classes of competitive antagonists of DAA.

185 Both compounds were characterized as competitive antagonists of dexamethasone without intrins

186 mple approach to determining the kinetics of competitive antagonists of G protein-coupled receptors b

187 Bicuculline or gabazine (two competitive antagonists of GABA binding) reduced the cur

188 Here we demonstrate that TXA and EACA are competitive antagonists of glycine receptors in mice.

189 Here, we identify competitive antagonists of NgR derived from amino-termin

190 otoxins are disulfide-rich peptides that are competitive antagonists of nicotinic acetylcholine recep

191 ts that beta5-containing dimers could act as competitive antagonists of other Gbetagamma dimers on GI

192 resistant to proBDNF-induced apoptosis, and competitive antagonists of sortilin block sympathetic ne

193 xifen and ICI 182,780 have been portrayed as competitive antagonists of the estrogen binding site of

194 in the striatum, and 2) competitive and non-competitive antagonists of the NMDA receptor differently

195 Another current animal model utilizes non-competitive antagonists of the NMDA/glutamate receptor,

196 F165 transformed each into potent, selective competitive antagonists of their respective normal and o

197 alpha-Conotoxins GI and MI are competitive antagonists of this receptor and, like d-tub

198 ligand (GV150013X) acted as a high affinity competitive antagonist on CCK2R(G) but was nearly ineffi

199 om that for GABA, and that CTZ acts as a non-competitive antagonist on the GABA(C) receptor.

200 the subunit level was unaffected by agonist, competitive antagonist, or isoflurane, state-dependent p

201 lassified as agonists (or partial agonists), competitive antagonists, or noncompetitive antagonists.

202 A competitive antagonist (P22) for heparin binding EGF-lik

203 ne-2'- phosphate-5'-phosphate also exhibited competitive antagonist/partial agonist activities.

204 efficacy of a novel CD80-blocking agent CD80-competitive antagonist peptide (CD80-CAP) in suppressing

205 he CD80 blocking agents, called CD80-binding competitive antagonist peptides (CD80-CAPs), at the time

206 potential therapeutic value for select CD80 competitive antagonist peptides.

207 of novel peptide agents referred to as CD80 competitive antagonist peptides.

208 The non-competitive antagonist picrotoxin blocked nearly 50% of

209 tive antagonist 3-APMPA, but not for the non-competitive antagonist picrotoxin.

210 Schild plot analysis using the competitive antagonists pirenzepine and himbacine indica

211 inhibited in a dose-dependent manner by the competitive antagonists prazosin, WB4101, and 5-methylur

212 Although agonists and competitive antagonists presumably occupy overlapping bi

213 els that are distinguished by their distinct competitive antagonist properties.

214 We used a peptide-based 14-3-3 competitive antagonist, R18, to disrupt 14-3-3-ligand as

215 Amiloride acted primarily as a competitive antagonist, reducing the sensitivity of the

216 AMPA receptor potentiators and non-competitive antagonists represent potential targets for

217 Furthermore, the concentration of competitive antagonist required to inhibit alpha-factor-

218 one-inactivated astrocyte r5-HT receptors to competitive antagonists resulted in the reactivation of

219 antaneous competition between agonists and a competitive antagonist revealed that binding rates were

220 n with high concentrations of NMDA or of the competitive antagonist (RS)-3-(2-carboxypiperazine-4-yl)

221 -electron resonance experiments, we show how competitive antagonists rupture the ligand binding domai

222 nine 59 as a residue critical in determining competitive antagonist sensitivity.

223 de, the most widely used AR antagonist, is a competitive antagonist shown previously to stabilize AR

224 During pregnancy, the density of the NMDA competitive antagonist site measured by [3H]-CGP 39653 w

225 y decreases GABA activation and converts the competitive antagonist SR-95531 into a partial agonist,

226 The competitive antagonist SR-95531 inverted this pattern of

227 Coapplication of either GABA or the competitive antagonist SR-95531 significantly slows MTSE

228 gnificant changes in the K(I) values for the competitive antagonist, SR-95531.

229 6- and 3-fold respectively, and that of the competitive antagonist strychnine by 15-fold.

230 suggested that CRF, its family members, and competitive antagonists such as astressin [cyclo(30-33)[

231 onic acid (AA) release but behaved as simple competitive antagonists, suggesting that these receptors

232 aried in their sensitivity to a low-affinity competitive antagonist, suggestive of a synaptic heterog

233 n the absence and presence of bicuculline, a competitive antagonist that also allosterically inhibits

234 TDBzcholine acts as a nAChR competitive antagonist that binds at equilibrium with eq

235 ics of opioid signaling we developed a caged competitive antagonist that can be quickly photoreleased

236 nding pocket, thus acting predominantly as a competitive antagonist that inhibits the cyclic-nucleoti

237 hylbenzeneacetic acid (LY367385) is a potent competitive antagonist that is selective for mGluR1, whe

238 A(A) receptor causes channel gating, whereas competitive antagonists that bind at the same site do no

239 The competitive antagonists TNP-ATP and A-317491 stabilize t

240 n intracisterna magna (ICM) injection of the competitive antagonist to HMGB1, Box-A, downregulates ba

241 hedding of soluble NgR(ECD), which acts as a competitive antagonist to NgR for binding of inhibitory

242 SMZ is a structural analog and competitive antagonist to p-aminobenzoic acid (PABA), wh

243 on-competitive mechanism and synergizes with competitive antagonists to disrupt AR activity.

244 Competitive antagonists to nicotinic acetylcholine recep

245 The selectivity of acetylcholine and the competitive antagonists (+)-tubocurarine and metocurine

246 mutations decreased the affinities of three competitive antagonists, (+)-tubocurarine, hexamethonium

247 rtial agonist, to adenosine, which acts as a competitive antagonist under these conditions.

248 Compounds in this series were shown to be competitive antagonists using an in vitro NK-1 smooth mu

249 Strategies based on the use of competitive antagonist vectors offer particular scope, a

250 was abolished by vanadate and P-glycoprotein competitive antagonists, verapamil and GF120918, in a do

251 d blocking endogenous S1P receptors with the competitive antagonist VPC23019 all significantly inhibi

252 exhibited by the alpha 1A subtype selective competitive antagonists WB 4101 and 5-methylurapidil com

253 hese receptors, combining a selective mGluR1 competitive antagonist with either an mGluR1- or mGluR5-

254 Gipg013 is a specific competitive antagonist with equally high potencies to mo

255 Compound 9m is a reversible and competitive antagonist with high binding affinity (IC(50

256 how by Schild analysis that TK40 is a potent competitive antagonist with Kb values of 21-63 nM at the

257 Thus, gabazine is a competitive antagonist with negligible negative efficacy

258 Schild analysis revealed that TNP-ATP was a competitive antagonist with pA(2) values of -8.7 and -8.

259 Competitive antagonists with the molecular property of n

260 h the closed-state structure in complex with competitive antagonist ZK 200775 suggests conformational