ライフサイエンスコーパス: competitive antagonist

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

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

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

4 XR) and thereby act as a partial agonist and competitive antagonist.

5 ed when removing the effect of an endogenous competitive antagonist.

6 -thiazole ring, is a specific A(3)R (< 1 uM) competitive antagonist.

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

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

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

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

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

12 evelopment of subunit selective agonists and competitive antagonists.

13 activity, inverse agonists behave as simple competitive antagonists.

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

15 ns key binding determinants for agonists and competitive antagonists.

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

17 harged ammonium group common to agonists and competitive antagonists.

18 acid residues that determine sensitivity to competitive antagonists.

19 ce of nonvariant leptin, the variants act as competitive antagonists.

20 relatively resistant to displacement by non-competitive antagonists.

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

22 5 potentiator binding to displacement by non-competitive antagonists.

23 r JNK1 activation compared with conventional competitive antagonists.

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

25 rted the discovery of a novel triazine GPR84 competitive antagonist 1.

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

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

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

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

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

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

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

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

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

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

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

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

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

39 eurosteroid has potentiating, inhibitory, or competitive antagonist activity on GABA(A)Rs.

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

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

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

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

44 This potentiation was eliminated by the competitive antagonist AMG-21629, the NADPH oxidase asse

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

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

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

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

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

50 e, kainate receptors on which NMDA acts as a competitive antagonist, and high affinity homomeric glyc

51 of the orthosteric binding site by agonists, competitive antagonists, and allosterically acting chann

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

74 Newer competitive antagonists at the neuromuscular junction ha

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

76 and tetramethylenedisulfotetramine, and the competitive antagonist bicuculline reduced fluorescence

77 bound to the channel-blocker picrotoxin, the competitive antagonist bicuculline, the agonist GABA (ga

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

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

80 Competitive antagonists bind directly to the integrin li

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

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

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

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

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

86 ndicate that B12 and FA bind AhR directly as competitive antagonists, blocking AhR nuclear localizati

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

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

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

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

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

92 Likewise, the competitive antagonist capsazepine inhibited RTX-induced

93 Setrons, a class of competitive antagonists, cause functional inhibition of

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

95 bsence of endogenous biological activity and competitive antagonist characteristics.

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

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

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

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

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

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

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

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

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

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

106 ding kinetics displayed by two alkaloids and competitive antagonists, (+)-DHbetaE and (+)-cocculine,

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

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

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

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

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

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

113 describe a cell specific, light-controllable competitive antagonist for the AMPA receptor called MP-G

114 velopment, suggesting enhanced function as a competitive antagonist for Tie2.

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

116 and Fz4 show phenotypes consistent with Wnt competitive-antagonist functions in vein formation (Fz3

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

118 A plethora of agonists and competitive antagonists have been developed to explore t

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

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

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

122 h was optimized to compound 16 as a full and competitive antagonist (IC(50) = 37 muM).

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

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

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

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

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

128 We also show that competitive antagonists induced distinct rearrangements

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

130 Competitive antagonists inhibited only PI hydrolysis and

131 Like the competitive antagonists, intrastriatal infusion of the n

132 developed during the past decades, including competitive antagonists, ion channel blockers, and negat

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

155 om the conotoxin the linear peptide HT1-0, a competitive antagonist of G(s), G(15), and beta-arrestin

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

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

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

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

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

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

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

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

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

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

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

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

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

169 emory deficit caused by phencyclidine (a non-competitive antagonist of NMDAR), and prevented the NMDA

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

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

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

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

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

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

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

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

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

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

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

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

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

183 ictibant is a specific, orally bioavailable, competitive antagonist of the bradykinin B2 receptor cur

184 We aimed to evaluate icatibant, a competitive antagonist of the bradykinin B2 receptors, f

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

186 Broflanilide acts as a non-competitive antagonist of the gamma-aminobutyric acid re

187 On one occasion, exendin 9-39, a competitive antagonist of the GLP-1 Receptor (GLP1R), wa

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

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

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

191 -2-piperidine carboxylic acid (CGS 19755), a competitive antagonist of the N-methyl-d-aspartate (NMDA

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

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

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

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

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

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

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

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

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

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

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

203 Piezo1 agonist Yoda1, a competitive antagonist of Yoda1 (Dooku1) and an inactive

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

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

206 Strategies to generate competitive antagonists of bioactive peptides include se

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

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

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

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

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

212 ey suppress psychotic symptoms by serving as competitive antagonists of dopamine at D2R.

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

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

215 rt behave as inverse agonists of GHSR and as competitive antagonists of ghrelin-induced inositol phos

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

217 The discovery of competitive antagonists of ligand-induced CatSper activa

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

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

220 previously identified alpha-Ctx ligands are competitive antagonists of orthosteric agonist-binding s

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

222 sts with EC(50) values of 0.9 and 7.3 uM and competitive antagonists of rifampin-dependent induction

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

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

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

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

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

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

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

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

231 by preventing ligand binding to NMDARs with competitive antagonists or blocking downstream Src kinas

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

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

234 Production of RANKL and its competitive antagonist osteoprotegerin (OPG) were analyz

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

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

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

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

239 potential therapeutic value for select CD80 competitive antagonist peptides.

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

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

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

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

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

245 Although agonists and competitive antagonists presumably occupy overlapping bi

246 In both sexes, intrathecal MK-801 (an NMDAR competitive antagonist) prevented LY2456302-evoked reins

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

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

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

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

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

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

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

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

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

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

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

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

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

260 The competitive antagonist SR-95531 inverted this pattern of

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

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

263 6- and 3-fold respectively, and that of the competitive antagonist strychnine by 15-fold.

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

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

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

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

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

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

270 oxicity is readily reversed with naloxone, a competitive antagonist that can restore respiration.

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

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

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

274 ation experiments, we studied the effects of competitive antagonists that block glutamate from bindin

275 Although competitive antagonists that prevent pathogen adhesion a

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

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

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

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

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

281 nd CXCR3 but no longer activate it, becoming competitive antagonists to native CXCL9/CXCL10.

282 Competitive antagonists to nicotinic acetylcholine recep

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

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

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

286 target of setrons, a class of high-affinity competitive antagonists, used in the management of nause

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

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

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

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

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

292 It is the target for setrons, a class of competitive antagonists widely used as antiemetics, and

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

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

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

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

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

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

299 Competitive antagonists with the molecular property of n

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