ライフサイエンスコーパス: selective antagonist

1 ogenous agonist, and butoxamine is a beta2AR selective antagonist).

2 were eliminated by treatment with an mGluR1-selective antagonist.

3 ocked by treatment with WAY 100635, a 5-HT1A-selective antagonist.

4 tion were blocked by the appropriate subtype-selective antagonist.

5 attenuated by a previously undescribed TRPA1-selective antagonist.

6 g14,Lys15]N/OFQ(1-13)-NH2), an ORL1 receptor-selective antagonist.

7 that this response can be blocked by a B(2)-selective antagonist.

8 could be inhibited by either a BLT1- or BLT2-selective antagonist.

9 e could be rescued by treatment with an AT1R-selective antagonist.

10 ion could be blocked by JAK3/STAT6 signaling selective antagonist.

11 development of well tolerated GluN2B subunit-selective antagonists.

12 , for example by the development of modality-selective antagonists.

13 ha4* (1 mum dihydro-beta-erythroidine)-nAChR-selective antagonists.

14 isrupted by genetic deletion in mice or with selective antagonists.

15 ignificant advance in the development of KOR-selective antagonists.

16 ill require development of high affinity and selective antagonists.

17 pplied alone or in combination with receptor-selective antagonists.

18 complex with UBP302 and UBP310, novel GluR5-selective antagonists.

19 ersed by treatment with RAR- or RXR receptor-selective antagonists.

20 part due to a lack of research tools such as selective antagonists.

21 2X4 function led us to pursue the search for selective antagonists.

22 novel receptor site in complex with isoform-selective antagonists.

23 ed by their sensitivity to ATP analogues and selective antagonists.

24 case has been lacking in the absence of EP2 -selective antagonists.

25 ification of two bivalent noncompetitive D3R-selective antagonists, 18a and 25a, which further deline

26 Here we report that the OX2R selective antagonist 26 induced sleep in mice primarily

27 not glutamatergic synapses, as the receptor-selective antagonist (2S)-alpha-ethylglutamic acid (EGLU

28 The D2R-selective antagonist 3-[4-(4-chlorophenyl)-4-hydroxypipe

29 The GluN2A-selective antagonist, 3-chloro-4-fluoro-N-[4-[[2-(phenyl

30 sphingosine inhibited the binding of the CB1-selective antagonist [3H]N-(piperidinyl)-5-(4-chlorophen

31 Here, we present the mGlu7-selective antagonist 7-hydroxy-3-(4-iodophenoxy)-4H-chro

32 es were not detectable with the alpha(1D)-AR selective antagonist 8-[2-(4-(2-methoxyphenyl)piperazin-

33 e definition of unspecific binding, the A1AR selective antagonist 8-cyclopentyl-1,3-dipropylxanthine

34 eptor potential vanilloid 1 (TRPV1) with the selective antagonist A-425619 reversed the mechanical se

35 ts or antagonists for hMC1R or hMC5R or have selective antagonist activity for hMC3R.

36 dimensional (3D) structural requirements for selective antagonist activity of arylpyrazole compounds

37 Selective antagonists against mu (CTOP: D-Phe-Cys-Tyr-D-

38 Selective antagonists against mu (D-Phe-Cys-Tyr-D-Trp-Or

39 ffects of bimatoprost and a novel prostamide-selective antagonist AGN 211334 on human conventional dr

40 -2) M, n = 4), but not the PG-EP(2) receptor-selective antagonist AH6809 (EC(50) = 4.10 x 10(-9) M, n

41 , hippocampal binding of the alpha7 receptor-selective antagonist alpha-bungarotoxin as well as hippo

42 ease in cell death, which was blocked by the selective antagonist alpha-bungarotoxin.

43 ession, as measured by binding of the alpha7-selective antagonist alpha-bungarotoxin.

44 lockade of the A2A adenosine receptor with a selective antagonist also augmented the efficacy of adop

45 mouse brain membrane preparations, sigma(1)-selective antagonists also potentiated both opioid recep

46 red alone, SR144528 and another CB2 receptor-selective antagonist AM630 increased mIPSC frequency in

47 s protective effect was blocked by the CXCR4 selective antagonist AMD3100.

48 cell lines which can be blocked by the CXCR4-selective antagonist AMD3100.

49 inhibitor of ERalpha, which is a potent and selective antagonist and downregulator of ERalpha in vit

50 2 expression, but it was inhibited by a COX2-selective antagonist and imitated by exogenous prostagla

51 ise sensitive to pertussis toxin or a CysLT1-selective antagonist and was attenuated by treatment wit

52 ented by AM630, a CB(2) cannabinoid receptor-selective antagonist and was not observed in skin from C

53 Using adenosine receptor subtype selective antagonists and BMDC derived from A(2A)AR(-/-)

54 Using selective antagonists and dopamine D1 and D2 receptor kn

55 y project with the aim of creating both OX2R selective antagonists and DORAs.

56 Selective antagonists and neurons from knock-out mice de

57 ts fibrinolytic activity, through the use of selective antagonists and new tPA formulations.

58 Future research and development of D3R-selective antagonists and partial agonists for substance

59 as a measure of activation and with isozyme-selective antagonists and siRNA.

60 The inhibitory potency of mAChR subtype-selective antagonists and small interfering RNAs (siRNAs

61 odels, encouraging efforts to develop GluN3A-selective antagonists and/or explore alternative therape

62 674042 (OX1 selective antagonist), EMPA (OX2 selective antagonist), and others.

63 romised by the Cry1Ab toxin, which acts as a selective antagonist, and supports the notion that BT-R(

64 ctive peptide agonists, the inactivity of Y1-selective antagonists, and a change from surmountable to

65 11 mutant D(1) receptors for D(1)- and D(2)-selective antagonists, and rhodopsin-based homology mode

66 F2 antagonist astressin-2B, but not the CRF1-selective antagonist antalarmin, blocked the anxiogenic

67 One might expect highly selective antagonists are available for the human beta-a

68 Several D3R-selective antagonists are effective in animal models of

69 Opioid receptor selective antagonists are important pharmacological prob

70 P2X receptor subtype-selective antagonists are promising candidates for treat

71 ar to psoriasis and AD, clinical trials with selective antagonists are required to dissect key pathog

72 s of the NMDA and AMPA iGlu receptor subtype selective antagonists ArgTX-93 and ArgTX-48.

73 erazine (JNJ7777120) has been described as a selective antagonist at the H(4) receptor and is widely

74 were characterized in vitro as high affinity selective antagonists at cholecystokinin types 1 and 2 (

75 three analogues, compounds, 9, 4, and 7, are selective antagonists at the hMC5 receptor.

76 mer population, but the receptor subtype non-selective antagonists atropine and N-methylscopolamine d

77 itive cells, which were blocked with the DP2-selective antagonist AZD6430.

78 protection is mimicked by a Sigma-1 receptor-selective antagonist (BD1063), but not an agonist (PRE-0

79 ive antagonist ICI-118,551 but not with B1AR-selective antagonist bisoprolol.

80 ced vasodilation in mice, and MK-0524, a DP1-selective antagonist, blocked both PGD2- and NA-induced

81 idine were prevented by the alpha-2A subtype selective antagonist BRL-44408 (1 mg/kg, i.p.).

82 files and selectivity are preserved with the selective antagonists BRL44408 and ARC239.

83 eover, in silico docking unveils that GluN2B-selective antagonists broadly divide into two distinct c

84 inactivator of Gi proteins) and by DPCPX (A1-selective antagonist), but not by SCH58261, MRS1706, and

85 Yet sigma receptor selective antagonists, but not agonists, shifted the EC(

86 Pharmacological blockade of C5aR with a selective antagonist (C5aR-A) during the first 7 d after

87 ber (P<0.01), which was blocked by the A1 AR-selective antagonist C8-(N-methylisopropyl)-amino-N6-(5'

88 transients that were suppressed by the TRPV1-selective antagonists capsazepine and JYL 1421.

89 nhibition of histamine release, whereas EP2 -selective antagonists caused rightward shifts in the PGE

90 rs, as it was prevented by the S1P3 receptor selective antagonist CAY1044 and in neurons in which S1P

91 in luciferase reporter assay, and PPAR-gamma selective antagonist completely inhibited MDSC induction

92 ffect could only be removed using the CRF-R1 selective antagonist CP-154526, suggesting Ucn1 acts thr

93 on, on the basis of inhibition with the site-selective antagonists d-tubocurarine and alpha-conotoxin

94 The use of selective antagonists demonstrated the involvement of do

95 EP4 -selective antagonists did not affect the PGE2 inhibition

96 sitive to the beta2 subunit-containing nAChR-selective antagonist, dihydro-beta-erythroidine (DHbetaE

97 duced neurotoxicity; whereas the alpha4beta2-selective antagonist, dihydro-beta-erythroidine, does no

98 hthylmethyl)thio]-9H-purine) is a potent and selective antagonist displaying IC(50) values of ~1 muM

99 Following perfusion with the group II mGluR-selective antagonist EGLU, ME inhibited eIPSC amplitude

100 dual OX1 and OX2 antagonist), SB-674042 (OX1 selective antagonist), EMPA (OX2 selective antagonist),

101 We used the mineralocorticoid receptor-selective antagonist eplerenone (EPL) to test the role o

102 Thus, the NR2B-selective antagonists exhibit a range of therapeutically

103 AZ10606120 is a selective antagonist for P2X7Rs (IC50 of 10 nM) and ine

104 In an attempt to identify a high-affinity, selective antagonist for the A(2B) AdoR, we synthesized

105 This novel peptide is the most selective antagonist for the hMC1R to date.

106 (6) with d-Phe(6) in gamma-MSH-NH(2) forms a selective antagonist for the hMC3R, whereas, substitutio

107 We developed a potent and selective antagonist for the prostaglandin E2 receptor s

108 -366791), at least, represents an apparently selective antagonist for TRPV1 suggests that this goal i

109 The development of selective antagonists for glutamate receptor subtypes is

110 MMP408 and FSLLRY-NH2 were the selective antagonists for MMP-12 and PAR2, respectively,

111 maceutical companies developing NR2B subtype-selective antagonists for several glutamate-mediated dis

112 Intra-accumbens infusions of selective antagonists for the 5-HT (SB 269970), 5-HT (SB

113 GPCRs, making 7 and 34b the most potent and selective antagonists for the GPRC6A receptor reported t

114 the search of chemically simple, potent, and selective antagonists for the hA3AR, and exemplifies the

115 With the aim to gain more potent and selective antagonists for the MC5R ligands, we have desi

116 as leads to further develop more potent and selective antagonists for the MOR.

117 ythrinanes with the aim of obtaining subtype-selective antagonists for the nAChRs and thereby probe t

118 cells dialyzed with no ATP, whereas the PP2A-selective antagonist fostriecin (30 or 150 nM) was ineff

119 more consistently produced than with the non-selective antagonist gabazine, and both were blocked by

120 CB2-selective antagonists, gene silencing and an inhibitor o

121 cells were blocked by the PG-EP(4) receptor-selective antagonist GW627368 (EC(50) = 1.09 x 10(-2) M,

122 nists - TG4-155 and TG6-10-1, but not by EP4 selective antagonist GW627368X.

123 Moreover, pretreatment with the PPARgamma-selective antagonist GW9662 blocked rosiglitazone-induce

124 as unaffected by pretreatment with the AMPAR selective antagonist, GYKI 52466.

125 d reversal, whereas an NR2B-containing NMDAR-selective antagonist had no effect.

126 The blockage of FP with AL8810, a selective antagonist, hampered Leishmania infection, whe

127 Selective antagonists have been used to define the roles

128 (2+) concentration that was inhibited by the selective antagonists HC030031, AP18, and HC067047, resp

129 itions involve NMDAR overactivation, subunit-selective antagonists hold strong therapeutic potential,

130 The resulting stable and potent FPR2-selective antagonists (i.e., RhB-(Lys-betaNphe)n-NH2; n

131 gration; this effect was abrogated with B2AR-selective antagonist ICI-118,551 but not with B1AR-selec

132 ich were specifically blocked by the beta2AR-selective antagonist ICI-118551 and by the beta2AR ECL2

133 Studies using other nAChR subtype-selective antagonists identified gene expression changes

134 When the GluN2B-selective antagonist ifenprodil was applied, the Mg(2+)

135 eveal modulation of triheteromers by subunit-selective antagonists ifenprodil, CP-101,606, TCN-201, a

136 The GluN2B-selective antagonist, ifenprodil, selectively reduced va

137 exhibited increased sensitivity to a GluN2B-selective antagonist in Neto1 knockouts relative to wild

138 A(1-11)NH2) is a kappa opioid receptor (KOR)-selective antagonist in vitro, is active in vivo, and an

139 Members of these series are potent, selective antagonists in in vitro/in vivo efficacy model

140 that HSP90 inhibitors may be as effective as selective antagonists in regulating platelet P2X1 recept

141 receptor (AdoRA2A), and ZM241385, an AdoRA2-selective antagonist, indicate that the inhibitory effec

142 gets for pain management, and development of selective antagonists is currently progressing.

143 Blockade of TRPV1 activation by selective antagonists is under investigation by several

144 Blockade of TRPV1 activation by selective antagonists is under investigation in an attem

145 re of the human kappa-OR in complex with the selective antagonist JDTic, arranged in parallel dimers,

146 sed to find that preincubation with the H(4)-selective antagonist JNJ7777120 potentiated rather than

147 Inhibition of ATM with the highly selective antagonist KU55933 markedly increased IL-23 se

148 r half were pretreated with the A2A receptor-selective antagonist KW-6002, inducing full blocking.

149 ble after pretreatment with the A2AR subtype-selective antagonist KW6002.

150 were potently blocked by the 5HT2A-receptor-selective antagonist, M-100907 (Ki = 1 +/- 0.3 nM), but

151 Thus, OX2R selective antagonists may also be beneficial for the tre

152 ion kinetics, and were blocked by the alpha7-selective antagonist methyllycaconitine.

153 Thus, alpha1D-selective antagonists might mediate coronary vasodilatio

154 oline receptors (nAChRs), as an alpha7 nAChR-selective antagonist mimicked the nicotine effect.

155 t was effectively inhibited by the cysLT(1)R-selective antagonist MK571 in a dose-dependent manner an

156 50=8.57), and this was antagonized by the A3-selective antagonist MRS1220 (pK(B)=9.32).

157 nonselective P2 antagonist PPADS or the P2Y1-selective antagonist MRS2179 failed to alter ADP- or ADP

158 junction potentials are blocked by the P2Y1-selective antagonist, MRS2179, and the nonselective P2 r

159 Cs, and responses were prevented by the P2Y1-selective antagonist MRS2500.

160 p III mGluR antagonist MSPG or the group III-selective antagonist MSOP abolished the effect of melato

161 of the mouse delta-OR, bound to the subtype-selective antagonist naltrindole.

162 altrexamine, respectively, but not the delta-selective antagonist naltrindole.

163 systemic administration of the CRF1 receptor selective antagonist, NBI 35965.

164 cked urocortin-induced effects, but the CRF1-selective antagonist NBI27914 (0, 500, 1000 ng/0.5 micro

165 Sensitivity to the P2X1 receptor-selective antagonist NF449 was reduced by approximately

166 ess this problem, the potent and D3-receptor-selective antagonist NGB 2904 (1, 9H-fluorene-2-carboxyl

167 potency was less than that of the known BMP2-selective antagonist, Noggin.

168 Similar to Dyn A, the KOR-selective antagonist nor-binaltorphimine (nor-BNI) lacke

169 R5 knockout mice or mice treated with mGluR5-selective antagonists, Norbin knockout mice showed a beh

170 Treatment with the KOR-selective antagonist norbinaltorphimine (10 mg/kg, i.p.)

171 Next, the GluN2A-selective antagonist NVP or GluN2B-selective antagonist

172 s, and this increase was blocked by the NR2A-selective antagonist NVP-AAM077.

173 Treatment with SB224289 (selective antagonist of 5-HT1B), fluoxetine (SERT inhibi

174 that 4-nitro-PFEB is the most effective and selective antagonist of alpha4beta2 versus alpha3beta4 a

175 SC frequency was attenuated by furosemide, a selective antagonist of alpha6 subunits.

176 the GP neuron's AHP is blocked by apamin, a selective antagonist of calcium-activated SK channels.

177 The resulting compound, 32, is a potent and selective antagonist of CCR3.

178 e insensitive to 1-naphthylacetylspermine (a selective antagonist of CP-AMPARs).

179 mEPSCs) and their sensitivity to IEM-1460, a selective antagonist of CP-AMPARs.

180 -LMMPn; this was inhibited or increased by a selective antagonist of CRF(1) (NBI35965) or astressin(2

181 A selective antagonist of CRF(2) (astressin(2)-B) increase

182 AMD3100, a selective antagonist of CXCL12 that binds to its recepto

183 t ane-1,4-diamine (AMD070) 2 as a potent and selective antagonist of CXCR4 with an IC(50) value of 13

184 t results of trials evaluating plerixafor, a selective antagonist of CXCR4, as a mechanism-oriented s

185 In recent experimental studies, a selective antagonist of endothelin ET(A) receptors, SB 2

186 attenuated in the presence of bicuculline, a selective antagonist of GABAA receptors.

187 -d ione (UBP304), a novel, potent and highly selective antagonist of GLU(K5)-containing kainate recep

188 rt the discovery of chroman 28, a potent and selective antagonist of human, nonhuman primate, rat, an

189 Interestingly, a selective antagonist of kappa-opioid receptors enhanced

190 We now report the discovery of a novel selective antagonist of M(1) mAChRs, termed VU0255035 [N

191 blocked by alpha-conotoxin MII[H9A;L15A], a selective antagonist of nAChRs containing the alpha6 sub

192 rs in afferent signalling, we used AF-353, a selective antagonist of P2X3-containing receptors to inh

193 arketed drug targeting a PAR is vorapaxar, a selective antagonist of PAR1 used to prevent thrombosis.

194 Administration of a potent and selective antagonist of T-type calcium channels, TTA-A2,

195 S44819 is a novel competitive selective antagonist of the alpha5-GABAAR at the GABA-bi

196 CCL2 transcription inhibitor (bindarit) or a selective antagonist of the CCR2 receptor (RS102895).

197 indole-2-carboxylic acid, 1, is a potent and selective antagonist of the glycine site of the N-methyl

198 A potent and selective antagonist of the melanocortin-4 receptor, 1-[

199 reatment with indomethacin or capsazepine, a selective antagonist of the transient receptor potential

200 identification of compound 31, a potent and selective antagonist of TRPA1 in vitro (IC50 = 0.015 muM

201 of purinone 27 (AM-0902), which is a potent, selective antagonist of TRPA1 with pharmacokinetic prope

202 preparations from neonatal rats treated with selective antagonists of 5-HT(2A) and neurokinin 1 (NK-1

203 Infusion of selective antagonists of alpha(1)- (terazosin) or alpha(

204 Selective antagonists of alpha-amino-3-hydroxy-5-methyl-

205 These effects were blocked by selective antagonists of alpha6-containing (alpha6*) nAC

206 Both tPyQB and tkP3BzPB were selective antagonists of alpha7.

207 ng with BAPTA abolished the potentiation and selective antagonists of Ca(2+)-permeable AMPA receptors

208 However, there are no known selective antagonists of Ca(V)1.3 L-type calcium channel

209 Past efforts to develop peripherally selective antagonists of CB1 have largely targeted rimon

210 , and arylsulfonamides) as highly potent and selective antagonists of EPAC2.

211 ly potent inhibitor, which is among the most selective antagonists of GSK-3 to date.

212 on, which results in neuronal death; and (3) selective antagonists of homomeric NR2B/NR2B- and hetero

213 Taken together, these data suggest that selective antagonists of M(1) mAChRs do not induce the s

214 We describe a new class of subunit-selective antagonists of N-methyl D-aspartate (NMDA)-sel

215 Surprisingly, many potent selective antagonists of Nav1.7 are weak analgesics.

216 alpha-Conotoxins are selective antagonists of neuromuscular or neuronal nicot

217 racellular ATP, a process that is blocked by selective antagonists of P2X7R.

218 Previous studies suggest that selective antagonists of specific subtypes of muscarinic

219 Selective antagonists of the BMP type I receptors repres

220 nes, which can be effectively inhibited with selective antagonists of the BMP type I receptors.

221 namide compounds were shown to be potent and selective antagonists of the H(3) receptor.

222 Isoform-selective antagonists of the lysophosphatidic acid (LPA)

223 synthesized and characterized as potent and selective antagonists of the melanocortin-4 receptor (MC

224 Selective antagonists of the metabotropic receptors 1 (m

225 substituted-phenyl) benzamides as potent and selective antagonists of this protein-protein interactio

226 As there are no available selective antagonists of TrkB, we used a lentivirus enco

227 ich could be blocked by treatment with a CB2-selective antagonist or ROS scavenger.

228 Their inactivation with selective antagonists or small interfering RNAs inhibite

229 e PKC delta isoform with either rottlerin, a selective antagonist, or small interference RNA blocks t

230 atically increased affinity for several D(2)-selective antagonists, particularly spiperone (225-fold)

231 (11)C-LY2795050 is a novel kappa-selective antagonist PET tracer.

232 one were similar to those of the D3 receptor-selective antagonist PG01037 and qualitatively different

233 0.1, 0.3 or 1 nmol/side), OXO plus the M(1) selective antagonist pirenzepine (PIRENZ; 0.3 nmol/side)

234 acological blockade of M1R using specific or selective antagonists, pirenzepine, VU0255035, or muscar

235 largely blocked by the alpha(1)-adrenoceptor-selective antagonist prazosin, and are mimicked by the a

236 In particular, the most potent and selective antagonist presents an (S) alpha-phenylethylam

237 d ventral tegmental area (VTA) with receptor-selective antagonist pretreatment capable of blocking th

238 -piperidine propranol] (0.5 microM), an NR2B selective antagonist, prevents the estradiol-induced inc

239 These results indicate that Gal(3)-selective antagonists produce anxiolytic- and antidepres

240 ile in rat (r), 10d was a highly potent A(1)-selective antagonist (rA(1) 7.7 nM; rA(2A) 546 nM; rA(2B

241 unted for 77% of the evoked EPSC and an NR2B-selective antagonist reduced the NMDA receptor-mediated

242 for only 18% of the evoked EPSC and an NR2B-selective antagonist reduced the NMDA receptor-mediated

243 is of rational ligand design, a new class of selective antagonists, represented by (2S,4R)-4-(2-carbo

244 61, MRS1706, and VUF5574 (A2A-, A2B-, and A3-selective antagonists, respectively).

245 tion and cytokine expression, and only A(3)R selective antagonist restored B-cell functions.

246 treatment of wild-type mice with an Adora2b-selective antagonist resulted in enhanced liver injury,

247 In WT mice, treatment with an A2BAR-selective antagonist resulted in enhanced pulmonary infl

248 Docking of R-22, a D3R-selective antagonist, reveals an extracellular extension

249 (RPE) components of the BRB, and that TRPV4-selective antagonists (RN-1734 and GSK2193874) resolve B

250 NR2A-selective antagonist, whereas the NR2B-selective antagonist Ro-25-6981 only partially reduced G

251 he GluN2A-selective antagonist NVP or GluN2B-selective antagonist Ro25 was infused into IL-mPFC or nu

252 hippocampal slices, we found that the GluN2B-selective antagonist Ro25-6981 (Ro25) reduced synaptic N

253 ubunit expressed, LTP is blocked by the NR2B-selective antagonist Ro25-6981 [R-(R,S)-alpha-(4-hydroxy

254 ns following chronic treatment with the NR2B-selective antagonist, Ro25,6981, the NR2A-prefering anta

255 taining NMDARs by administration of the NR2B-selective antagonist Ro256981 directly into the NAc, und

256 The effects of the OX(1)-selective antagonist SB 334867 on brain stimulation-rewa

257 ary pharmacophores were derived from the D3R-selective antagonists SB269,652 (1) and SB277011A (2) wh

258 endent and non-dependent groups, whereas the selective antagonist SB612111 (1-10 mg/kg) elicited a cl

259 acrophages with CCX872, a novel Phase I CCR2 selective antagonist, significantly reduced TBI-induced

260 fication of a 0.13 nM potent 5800-fold mMC3R selective antagonist/slight partial agonist versus a 760

261 effects of two potent small-molecule, Gal(3)-selective antagonists, SNAP 37889 and the more soluble a

262 treated rats was blocked by the CB2 receptor-selective antagonist SR144528, indicating that CB2 recep

263 xperiments conducted with the CB(2) receptor-selective antagonist SR144528, inhibitors of the PI3K/Ak

264 the somatostatin receptor subtype 2 (SSTR2) selective antagonist sst2-ANT was determined to have a h

265 2Y(2) receptor, but not by NF-157, a P2Y(11)-selective antagonist, suggesting a role for the P2Y(2) r

266 1-expressing cells were treated with PKCbeta-selective antagonists, supporting our previous observati

267 ion of enhanced ERbeta activity by an ERbeta-selective antagonist suppressed mouse ectopic lesion gro

268 n the spinal cord and that an intrathecal B2-selective antagonist suppresses behavioral manifestation

269 fluorinated piperidine ( S)- 5, a potent and selective antagonist that displayed in vivo CNS efficacy

270 n conclusion, the peptide zyklophin is a KOR-selective antagonist that exhibits the desired shorter d

271 High-affinity and selective antagonists that are able to block the actions

272 Subunit-selective antagonists that discriminate between the glyc

273 Unlike AR-C 69931MX, a P2Y(12) receptor-selective antagonist, the GIRK channel blockers did not

274 tion NMDA receptor antagonists and some NR2B-selective antagonists, the present series of propanolami

275 Furthermore, VTA microinjection of the DOR selective antagonist TIPP-Psi increases drinking in low,

276 dopamine receptors as well as a D4 receptor-selective antagonist to address the function of each of

277 energic stress, thus functioning as a cardio-selective antagonist to beta-adrenergic activation.

278 Administration of a CRFR2 selective antagonist to WT mice resulted in a GTT profil

279 ter local micro-iontophoretic application of selective antagonists to AMPARs [NBQX (1,2,3,4-tetrahydr

280 s effect is also observed in the presence of selective antagonists to CCR5, CCR2, or CXCR2, whereas A

281 ssful translation of previously reported D3R-selective antagonists to clinical use for cocaine abuse.

282 T) dopamine subtype 2/3 receptor (D2/3R) non-selective antagonist tracers suggests that obese (OB) in

283 An S1PR1-selective antagonist, W146, blocked the neuroprotective

284 pounds from which a new subclass of receptor-selective antagonists was identified.

285 nsitivity of PVT-to-NAc synapses to CP-AMPAR-selective antagonists was not changed after withdrawal,

286 cked by the alpha1A-adrenergic receptor (AR) selective antagonist WB 4101 (30 nm) and mimicked by the

287 In a program to develop an OX1 selective antagonist, we designed and synthesized a seri

288 With the aide of subtype selective antagonists, we found that SNr neurons express

289 receptor immunocytochemistry, and the use of selective antagonists, we identified these receptors as

290 ersible and were also observed with the NR2A-selective antagonist, whereas the NR2B-selective antagon

291 mpared with NVP-AAM077, a widely used GluN2A-selective antagonist, which we show has 11-fold preferen

292 lated at the cell surface and bound to an A1-selective antagonist with an affinity indistinguishable

293 Here we describe a prototypical GluN2B-selective antagonist with an IC50 value that is 10-fold

294 ion led to the identification of a >100-fold-selective antagonist with nanomolar affinity from commer

295 e foundation for the future design of GTPase-selective antagonists with higher affinity to benefit of

296 ies we identified several LPA(1)- and LPA(3)-selective antagonists with IC(50) values in the nanomola

297 channels were favored as application of the selective antagonist XE991 mimicked and occluded efferen

298 ture of the human AT(1)R in complex with its selective antagonist ZD7155 at 2.9-A resolution.

299 wever, blocked by the A2A adenosine receptor-selective antagonists ZM241385 and SCH58261 (apparent pK

300 tor, in complex with a high-affinity subtype-selective antagonist, ZM241385, to 2.6 angstrom resoluti