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

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

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

12 development of well tolerated GluN2B subunit-selective antagonists.

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

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

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

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

17 ill require development of high affinity and selective antagonists.

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

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

20 2X4 function led us to pursue the search for selective antagonists.

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

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

23 bolished upon coapplication with the AA site-selective antagonist 2,3,5,6MP-TQS (cis-trans-4-(2,3,5,6

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

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

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

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

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

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

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

31 nkgolides-some of which are glycine-receptor-selective antagonists(8).

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

33 For the first time, we demonstrate that P2X-selective antagonists act differentially as inhibitors o

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

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

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

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

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

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

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

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

42 rdings, we found that the alpha3beta4* nAChR-selective antagonist alpha-conotoxin AuIB almost complet

43 By contrast, the alpha3beta2* nAChR-selective antagonist alpha-conotoxin MII only partially

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

53 Using selective antagonists and dopamine D1 and D2 receptor kn

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

55 Selective antagonists and neurons from knock-out mice de

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

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

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

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

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

61 674042 (OX1 selective antagonist), EMPA (OX2 selective antagonist), and others.

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

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

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

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

66 Opioid receptor selective antagonists are important pharmacological prob

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

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

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

70 omatic residues in the kappa opioid receptor selective antagonist arodyn (Ac[Phe(1,2,3),Arg(4),d-Ala(

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

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

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

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

75 we have mapped the binding site of the P2X7R-selective antagonist AZ11645373 to the known allosteric

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

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

78 nist scopolamine as well as the more subtype-selective antagonists biperiden (M1) and tropicamide (M4

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

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

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

87 We further observed that P2X1- and P2X7-selective antagonists can act differentially as inhibito

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 EP receptor knockdown and subtype-selective antagonists demonstrated EP2 and EP4 receptor

95 The use of selective antagonists demonstrated the involvement of do

96 ere replicated by application of the K(v)1.1 selective antagonist, Dendrotoxin-K, in several L-DRG su

97 EP4 -selective antagonists did not affect the PGE2 inhibition

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

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

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

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

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

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

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

107 The development of selective antagonists for glutamate receptor subtypes is

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

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

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

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

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

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

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

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

116 ly bind A(2B)AR, with a number of potent and selective antagonists further confirmed by functional cy

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

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

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

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

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

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

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

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

125 Selective antagonists have been used to define the roles

126 (2+) concentration that was inhibited by the selective antagonists HC030031, AP18, and HC067047, resp

127 alpha3beta2beta3 and is the most alpha3beta2-selective antagonist heretofore reported.

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

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

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

131 whereas 0.1 mum of the beta(2) -adrenoceptor selective antagonist ICI-118,551 had no effect.

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

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

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

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

136 y at GluN1/2B/2D receptors, including GluN2B-selective antagonists, ifenprodil, EVT-101 and CP-101-60

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 e direct implications for the use of subunit-selective antagonists in neuroscience research and envis

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

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

143 orthosteric binding sites, obtaining highly selective antagonists is a challenging but critical task

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

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

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

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

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

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

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

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

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

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

154 Thus, alpha1D-selective antagonists might mediate coronary vasodilatio

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

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

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

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

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

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

165 limited HIV-1 productive infection, but P2X-selective antagonists (NF449 and A438079) significantly

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

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

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

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

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

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

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

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

174 AChRs was 100-fold lower, R8 appears to be a selective antagonist of alpha9alpha10 nAChR.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

193 R321 is a potent and selective antagonist of the CCR3 signaling cascade.

194 Mavorixafor is an oral small molecule selective antagonist of the CXCR4 receptor that increase

195 ula is an inhibitor cystine-knot peptide and selective antagonist of the human Nav1.7 channel.

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

197 -sensing ion channels, ASICs) and AMG8910 (a selective antagonist of the transient receptor potential

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

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

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

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

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

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

204 Both tPyQB and tkP3BzPB were selective antagonists of alpha7.

205 ncreases and these increases were blocked by selective antagonists of both adenosine A2A and A2B rece

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

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

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

209 signals to control naive and memory T cells, selective antagonists of CD28-CD80/86 interactions have

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 Non-selective antagonists of metabotropic glutamate receptor

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

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

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 tivator of caspase (SMAC) mimetics (SMs) are selective antagonists of the inhibitor of apoptosis prot

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

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

225 Designing potent and selective antagonists of these receptors, especially of

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

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

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

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

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

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

232 0.1, 0.3 or 1 nmol/side), OXO plus the M(1) selective antagonist pirenzepine (PIRENZ; 0.3 nmol/side)

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

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

235 obes were designed around the known hA(2A)AR selective antagonist preladenant (SCH 420814).

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 GluN2B-selective antagonists produce robust inhibition of GluN1

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

263 2Y(2) receptor, but not by NF-157, a P2Y(11)-selective antagonist, suggesting a role for the P2Y(2) r

264 1-expressing cells were treated with PKCbeta-selective antagonists, supporting our previous observati

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

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

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

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

269 Subunit-selective antagonists that discriminate between the glyc

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

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

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

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

274 L, which serves as an endogenous alphavbeta3-selective antagonist to maintain glomerular filtration.

275 Administration of a COX-1-selective antagonist to mice completely prevented the ge

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

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

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

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

280 ined in adult male Lister-hooded rats, using selective antagonists to determine the role of oxytocin

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

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

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

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

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

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

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

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

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

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

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

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

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

294 rate a series of human Frizzled (Fz) subtype-selective antagonists with extensive shape complementary

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

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

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

298 determined the site of action for the P2X7R-selective antagonists ZINC58368839, brilliant blue G, KN

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