ライフサイエンスコーパス: antagonist

1 g as full or partial agonists, and one as an antagonist.

2 sened by mecamylamine, a selective nicotinic antagonist.

3 , 4,447 +/- 1,128 dpm/mg of tissue) with the antagonist.

4 ypes, and is thought to act as an allosteric antagonist.

5 ce of 4 mum SCH23390, a dopamine D1 receptor antagonist.

6 ay and negated by TLR4-specific antibody and antagonist.

7 g administration of a dopamine D2/3 receptor antagonist.

8 onist and only 4 had a weak binding with the antagonist.

9 R-overexpressing cells, thus, it acted as an antagonist.

10 ation was also blocked by ryanodine receptor antagonist.

11 e peptide-1 receptor (GLP-1R) noncompetitive antagonist.

12 have many more sst2 sites measured with the antagonist.

13 , although GB88 has been described as a weak antagonist.

14 xamide derivatives developed as CB1 receptor antagonists.

15 eral medulla (RVLM) using selective receptor antagonists.

16 with a combination of aspirin and vitamin K antagonists.

17 f their genomes, that often act as host cell antagonists.

18 fter application of OEA and PEA and relevant antagonists.

19 ould be relevant for patients receiving VEGF antagonists.

20 ot seen for classical nicotinic agonists and antagonists.

21 eability, both of which were reduced by PAR1 antagonists.

22 ed potent dual acting A1AR agonists and A3AR antagonists.

23 ignificantly with an excessive amount of GRP antagonists.

24 ations that persisted after addition of CavL antagonists.

25 ow internalization, as expected for receptor antagonists.

26 whether pituitary cells secrete BMPs or BMP antagonists.

27 e by either nicotinic or muscarinic receptor antagonists.

28 teracts with Wnt ligands, as well as the Wnt antagonists.

29 existing clinical availability of complement antagonists.

30 -like symptoms, than other dopamine receptor antagonists.

31 This interaction can be disrupted by CXCR4 antagonists.

32 se (Sostdc1)/sclerostin (Sost) family of Wnt antagonists.

33 A radiolabeled small-molecule GPR44 antagonist, [(11)C]AZ12204657, was evaluated for visuali

34 iopharmaceutical therapy with the novel NTR1 antagonist (177)Lu-3BP-227.

35 907 patients with AF treated with vitamin K antagonists (3,865 patient-years), to assess CVEs, inclu

36 were MC3R agonists (EC50 < 1000 nM) and MC4R antagonists (5.7 < pA2 < 7.8).

37 Antagonist 5d not only blocked exendin-4-stimulated insu

38 The glutamine antagonist 6-diazo-5-oxo-l-norleucine (DON, 14) attenuat

39 hase I/II study to evaluate the sst receptor antagonist (68)Ga-OPS202 ((68)Ga-NODAGA-JR11; NODAGA = 1

40 cological characterization of 5-HT6 receptor antagonist 7 indicates high affinity and selectivity ove

41 nuclear receptor's activity using a chemical antagonist abrogated not only the alterations in PPARgam

42 in penetrance, elicited potent in vitro CB1R antagonist activities and iNOS inhibitory activities.

43 ished endocrine disruptor with mixed agonist/antagonist activity acting via endogenous estrogen recep

44 TMBPF did not show estrogen-agonist or antagonist activity in the estrogen receptor-transactiva

45 In a functional assay, 1b displayed full antagonist activity with IC50 = 6 +/- 2 muM.

46 y remained suppressed (<1 mug/L per h) on MR antagonists (adjusted HR [2.83 [95% CI 2.11-3.80], and 1

47 NY), a platelet-derived growth factor (PDGF) antagonist, administered in combination with the anti-va

48 Competitive antagonists against N-methyl-D-aspartate (NMDA) receptor

49 proopiomelanocortin gene transcript, and two antagonists, agouti-signaling protein (ASP) and agouti-r

50 of PGE2-G were prevented by EP1/EP2 receptor antagonist AH-6809 but not the EP4 antagonist ONO-AE2-22

51 tty acid/glycerol ratio increased during the antagonist alone and in combination with GIP.

52 proliferation; our data suggest that a TGR5 antagonist alone or concurrently with somatostatin recep

53 5-HT2C agonists and 5-HT2A inverse agonists/antagonists alone or in combination as candidate anti-co

54 tment practices-namely, using inhibitors and antagonists alone-and to develop immunoresolvents as ago

55 ANO1 antagonists also abolished SWs as well as transient depo

56 s or locally introducing DA or GABA receptor antagonists alters kinship preference.

57 administration of the cannabinoid receptor 2 antagonist AM630 (10 mg/kg) or inverse agonist JTE907 (3

58 unique CXCR2 agonist, GRObeta, and the CXCR4 antagonist AMD3100.

59 was attenuated by administration of a CXCR4 antagonist AMD3100.

60 o-controlled pharmacology [D2 receptor (D2R) antagonist amisulpride] in humans with resting-state fun

61 , we demonstrate here that the IL-1 receptor antagonist anakinra abrogates IL-22 production and reduc

62 t on IL-1beta secretion by the IL-1 receptor antagonist anakinra in phagocytes of patients with CGD.

63 man MMN, along with sensitivity to the NMDAR antagonist and agonist administration.

64 Derquantel behaved as a competitive antagonist and distinguished M-nAChRs activated by moran

65 addition, ATBF remained constant during the antagonist and increased only slightly in combination wi

66 Using TR antagonists and Thrb2 deletion, we examined the effects

67 nd mouse cells, two laminarins were Dectin-1 antagonists and two were Dectin-1 agonists.

68 ed calcium transients was blocked by the IP3 antagonist, and not observed in the absence of IP3 IP3 p

69 ended-release naltrexone (XR-NTX), an opioid antagonist, and sublingual buprenorphine-naloxone (BUP-N

70 eta blockers, and mineralocorticoid receptor antagonists, and advanced device therapies.

71 osuppression was with interleukin-2 receptor antagonists, and antithymocyte globulin in high-risk rec

72 were treated with the neurokinin 1 receptor antagonist aprepitant before SP stimulation.

73 that somatostatin receptor subtype 2 (sst2) antagonists are better tools to target neuroendocrine tu

74 's disease, are starting to emerge, and A2AR antagonists are important drug candidates for nondopamin

75 urodegeneration in MoCD and introduce NMDA-R antagonists as potential therapeutics for this fatal dis

76 ns, raising demand for new chemotypes of KOR antagonists as well as G-protein-biased agonists.

77 a low efficacy agonist, and diprenorphine an antagonist at the MOPr.

78 The OTR antagonist, atosiban, is currently used therapeutically

79 ion of beta2AR signaling with an aerosolized antagonist attenuates airway hyperresponsiveness (AHR),

80 Accordingly, treatment with global RAS antagonists attenuates cardiovascular risk and slows the

81 Antagonist AZ3451 binds to a remote allosteric site outs

82 Pretreatment with histamine receptor-1 antagonist, azelastine prevented the early effect of nas

83 potent and selective adenosine A2A receptor antagonists bearing substituted 1-methylcyclohexyl-carbo

84 WAY100635 plus GR127935 (5-HT1A/1B receptor antagonists), betaxolol plus ICI-118 551 (beta1 and beta

85 , we compare quantitatively (125)I-JR11 sst2 antagonist binding in vitro with that of the sst2 agonis

86 We propose that antagonist binding prevents structural rearrangements re

87 s evaluated in the mouse formalin test (A3AR antagonist blocked and A3AR agonist strongly potentiated

88 Combining CSF1R inhibitor with a CXCR2 antagonist blocked granulocyte infiltration of tumors an

89 GW9662, a potent PPARgamma antagonist, blocked the antileukemic effect of selenium

90 Thus, the LPAR antagonist BMS002 protects against GFR decline and atten

91 no clear distinction between the agonist and antagonist-bound complexes.

92 1N1) virus was an effective interferon (IFN) antagonist but could not inhibit general host gene expre

93 The remaining laminarin was a Dectin-1 antagonist, but when the low m.w. moieties were removed,

94 hat a receptor agonist can be switched to an antagonist by substituting one or more relevant residues

95 Small-molecule inhibitor of apoptosis (IAP) antagonists, called Smac mimetic compounds (SMCs), sensi

96 hibitor MDL 12330A, and the protein kinase A antagonist cAMPS-Rp.

97 s that subunit selectivity of glutamate-site antagonists can be mediated by mechanisms in addition to

98 A cholestanol-conjugated antagonist, CGRP8-37, accumulated in CLR-containing endo

99 of the neurokinin-1 receptor with a specific antagonist (CJ-12,255) would improve survival in the cec

100 le CpomOR6a responds to the strong pheromone antagonist codlemone acetate (E,E)-8,10-dodecadien-1-yl

101 d using unilateral intra-PFC infusions of DA antagonists combined with contralateral inactivation of

102 geting by novel somatostatin receptor (SSTR) antagonists compared with clinically widely used agonist

103 s, which is an attractive feature for a PAR2 antagonist competing against a tethered ligand.

104 atic effects were achieved by adding the EP1 antagonist compound (SC-51322) to AGN 197727 in the syst

105 peutic target upstream of WNT3A, where WNT3A antagonists could be novel agents for the treatment of m

106 f non-obese diabetic mice with a Y1 receptor antagonist delays the onset of diabetes.

107 infusion of the ETA antagonist did not completely block the increase in bloo

108 GABA or glutamate receptor antagonists did not block the ethanol effect.

109 AR-C25118925XX (P2Y2 antagonist) did not inhibit MSU crystal-stimulated NET r

110 Use of the beta2-selective nAChR antagonist, dihydro-beta-erythroidine, suggests that los

111 The EAAT2-specific antagonist dihydrokainate (DHK) was microinjected into t

112 Rats receiving PPAR-gamma antagonists displayed proteinuria and increased podocyte

113 15 mg/kg), a nonspecific adenosine receptor antagonist, dose-dependently and at high doses completel

114 eas patients who were treated with higher MR antagonist doses and had unsuppressed renin (>/=1 mug/L

115 However, multiple integrin antagonist drug candidates have failed to show efficacy

116 The next-generation AR antagonist, enzalutamide, prolongs survival, but resista

117 r GLP-1R agonist, exendin-4 (Ex4), or GLP-1R antagonist, exendin-9-39 (Ex9).

118 +)-1d, or cis-(-)-1d, which behave as sigma1 antagonists, exhibited a sigma1 agonist profile.

119 eated with vehicle solution, a PAC1 receptor antagonist (experiment 2), or a PACAP agonist (experimen

120 ssion of forkhead box protein O1 (FoxO1), an antagonist for activated Stat3, specifically in beta-cel

121 g histidine of CCR2 converts J113863 from an antagonist for cell migration and a partial agonist in o

122 owledge, this is the first report of peptide antagonist for prokaryotic NaVs.

123 he natural ligands; however, the RGD-mimetic antagonists for alphaIIbbeta3 have been shown to cause p

124 F secretion from DCs is reversed by receptor antagonists for EP2 and EP4, indicating PGE2 action.

125 of chemically simple, potent, and selective antagonists for the hA3AR, and exemplifies the benefits

126 ls from C57BL6 mice, with or without the S1P antagonist FTY720; we then studied HSC mobilization and

127 Mice given the S1P antagonist (FTY720) with HSCs had increased hepatic rete

128 otably, administration of a ghrelin receptor antagonist further reduced blood glucose levels into the

129 nhibited by the mechanosensitive ion channel antagonists gadolinium, ruthenium red and D-GsMTx4.

130 nhibited by Piezo2 small interfering RNA and antagonists (Gd(3+) and D-GsMTx4).

131 sequence near the gremlin 1, DAN family BMP antagonist gene (GREM1) originally described in Ashkenaz

132 kade of AhR using a clinically available AhR antagonist greatly enhanced the in vitro generation of i

133 e) was improved in the neurokinin-1 receptor antagonist group during the first 6 hours of sepsis, and

134 4-155 and TG6-10-1, but not by EP4 selective antagonist GW627368X.

135 lpha silencing and PPARalpha blockade by the antagonist GW6471 abolish the effect of clofibrate on ra

136 was blocked by the dopamine D2-like receptor antagonist haloperidol.

137 y across the PAR isoforms, discovery of PAR2 antagonists has been less successful, although GB88 has

138 Recently, laropiprant, a DP1 receptor antagonist, has been used in combination with niacin to

139 While agonists and antagonists have traditionally been pursued to target GP

140 Previously studied selective KOP-r antagonists have unusual pharmacodynamic and pharmacokin

141 agents (serotonin and neurokinin-1 receptor antagonists) have increased efficacy but are expensive.

142 ide (AH-7614), has been described as an FFA4 antagonist; however, its mechanism of antagonism remains

143 e resulting stable and potent FPR2-selective antagonists (i.e., RhB-(Lys-betaNphe)n-NH2; n = 4-6) are

144 The B2 receptor antagonist icatibant is approved for treatment of attack

145 ction of the natural inhibitor IL-1 receptor antagonist (IL-1Ra) and shifts production toward the hig

146 s tightly regulated by the specific receptor antagonist (IL-1Ra) and the decoy receptor IL-1 receptor

147 active protein (CRP), interleukin-1 receptor antagonist (IL-1Ra), and soluble interleukin-6 receptor

148 modulated in vivo by its naturally occurring antagonist, IL-18 Binding Protein (IL-18BP).

149 -releasing factor receptor 1 (CRF1 receptor) antagonist in adult women with PTSD.

150 cells, identifies a role for KLF7 as a KLF4 antagonist in corneal epithelial cell differentiation, a

151 TRA2P-TIMI 50 (Thrombin Receptor Antagonist in Secondary Prevention of Atherothrombotic I

152 s required for the therapeutic effect of SMO antagonists in AML samples and restoration of GLI3R supp

153 suggest potential therapeutic utility of OXR antagonists in reducing psychostimulant-induced motor im

154 hysiological reversal of the effects of NMDA antagonists in rodents.

155 useful for developing and triaging new hA3R antagonists in the early phase of drug discovery.

156 upport a potential role for HIF1A or ADORA2B antagonists in the treatment of IPF.

157 dependent translation, pre-treatment with AR antagonists including bicalutamide increased eIF4E phosp

158 -catenin signaling by directly targeting Wnt antagonists, including Dkk1.

159 e also found that Rap1B knockdown or an EPAC antagonist increases endothelial permeability and that V

160 -acting beta2-agonist/long-acting muscarinic antagonist indacaterol/glycopyrronium 110/50 mug with tw

161 ogen-activated protein kinase (MAPK) pathway antagonists induce profound clinical responses in advanc

162 e not detected in bones treated with a CXCR4 antagonist infusion.

163 ections of NPY or an NPY receptor Y1 (NPY1R) antagonist into PVN or DMH decreased or increased SSNA,

164 iral vectors (AAVs) encoding ligand-specific antagonists into the tibialis anterior (TA) muscles of C

165 ionships of novel dual-target compounds with antagonist/inverse agonist activity at cannabinoid recep

166 atment with S 38093, a novel brain-penetrant antagonist/inverse agonist of H3 receptors, on AHN (prol

167 ogical interactions like coevolution between antagonists is a matter of active debate.

168 is, we show that gabazine, a GABA-A receptor antagonist, is antihyperalgesic in primed mice exposed t

169 istration of the kappa-opioid receptor (KOR) antagonist JDTic (30 mg/kg, i.p.) before CSDS reduced st

170 histamine, IL-17, IL-21 and IL-22, and a H4R antagonist (JNJ7777120), the gene expression H4R and RAN

171 l agonist properties; like the NMDA receptor antagonist ketamine GLYX-13 produces rapid antidepressan

172 ic dose of the N-methyl-D-aspartate receptor antagonist ketamine may work to correct these neuroadapt

173 ry deficits caused by the nonselective NMDAR antagonist ketamine.

174 uption, we examined the effects of the NMDAR antagonist, ketamine, on predictive coding during vocali

175 e pretreated with the A2A receptor-selective antagonist KW-6002, inducing full blocking.

176 temic administration of an OT receptor (OTR) antagonist L-368,899 on social behavior in male and fema

177 sed drug design to identify novel agonist or antagonist leads.

178 trol muscles during leg swing, and increased antagonist leg muscle coactivation during limb loading i

179 d two synthetic compounds), (2) a novel TGR5 antagonist (m-tolyl 5-chloro-2-[ethylsulfonyl] pyrimidin

180 escalation study indicates that an optimized antagonist mass might further improve the safety window

181 A TLR7 antagonist may mitigate atherosclerosis.

182 These results suggest that CDK6 antagonists may be a promising therapeutic approach for

183 e findings also suggest that selective TRPA1 antagonists may be useful to counteract HQ-induced skin

184 utes to ALD development and suggest that PXR antagonists may provide a new approach for ALD therapy.

185 C-glycosidic antagonists may serve such a purpose.

186 with 15 mug/kg GHRH agonist, MR-409, or GHRH antagonist, MIA-602.

187 he nonselective glucocorticoid receptor (GR) antagonist mifepristone has been approved in the U.S. fo

188 TION: Treatment with a neurokinin 3 receptor antagonist (MLE4901) could be practice changing as it sa

189 fectiveness of an oral neurokinin 3 receptor antagonist (MLE4901) on menopausal hot flushes.

190 ts treated with a mineralocorticoid receptor antagonist (MRA).

191 nus and striking coactivation of agonist and antagonist muscles.

192 our attempt to optimize the lead HIV-1 entry antagonist, NBD-11021, we present in this study the rati

193 Systemic and ocular treatment with the TR antagonists NH-3 and 1-850 increased cone density by 30-

194 RVFV virulence depends on the interferon antagonist non-structural protein (NSs), which remains p

195 Methyllycaconitine (MLA), an antagonist of alpha7 nAChR, could efficiently block thes

196 ard enhanced synthesis of kynurenic acid, an antagonist of both alpha7 nicotinic acetylcholine and N-

197 Here, we identify TIAM1 as a critical antagonist of CRC progression through inhibiting TAZ and

198 y for intracellular delivery of a nucleotide antagonist of eIF4E in mantle cell lymphoma (MCL) cells.

199 pilocarpine can act as either an agonist or antagonist of M3R, depending on the cell type, expressio

200 The muscle phenotype can be rescued by an antagonist of muscarinic acetylcholine receptors.

201 representing an uncompetitive/fast off-rate antagonist of NMDA-type glutamate receptors.

202 Ubp2 is an antagonist of Rsp5, which promotes synthesis of the fatt

203 rt that a potent and specific small molecule antagonist of the CCR6 chemokine receptor, CCX2553, was

204 GIP(3-30)NH2, was recently identified as an antagonist of the human GIP receptor.

205 we show that mice treated with anakinra, an antagonist of the interleukin (IL)-1beta receptor (IL-1R

206 AT-IAP, a potent, orally bioavailable, dual antagonist of XIAP and cIAP1 and a structurally novel ch

207 ediated by 5-HT because they were blocked by antagonists of 5-HT2A and 5-HT1A receptors, respectively

208 of oligoquinolines was screened to identify antagonists of Abeta oligomerization, amyloid formation,

209 Functionally, selective competitive antagonists of apelin receptor were shown to be safe and

210 Antagonists of GABA or VIP signaling or action potential

211 Previous studies suggest that antagonists of group II metabotropic glutamate (mGlu) re

212 of the hedgehog pathway have yielded several antagonists of the GPCR-like smoothened receptor.

213 rmation is through a counter-gradient of BMP antagonists, often along with ligand shuttling to genera

214 centrally administered orexin receptor (OXR) antagonists on measures of impulsive-like behavior in ra

215 receptor antagonist AH-6809 but not the EP4 antagonist ONO-AE2-227.

216 er types which do not respond to either EGFR antagonist or DR agonist monotherapies.

217 s treated with a tumor necrosis factor-alpha antagonist or placebo and a modest increase in vascular

218 This was reversible using either A2AR antagonists or genetic targeting of A2AR using shRNA.

219 Either ADORA2A or ADORA2B antagonists or the PKA inhibitor mPKI blocked these effe

220 tions up to 10 muM, while others were weaker antagonists (or partial agonists) on these receptors.

221 tagonist), R-propranolol (5-HT1A/1B receptor antagonist), or racemic propranolol in both male and fem

222 betaxolol plus ICI-118 551 (beta1 and beta2 antagonists), or S-propranolol alone.

223 A knockout, an antagonist, or a local silencing of MKP-1 attenuates dep

224 The use of non-vitamin K antagonist oral anticoagulants (NOACs) instead of vitami

225 Phase III trials comparing non-vitamin K antagonist oral anticoagulants (NOACs) with warfarin exc

226 N-accelerated lupus model, treatment with an antagonist Ox40:Fc fusion protein significantly delayed

227 ram of tissue (%IA/g), respectively, for the antagonist (P > 0.05), as compared with 17.8, 12.0, and

228 the J113863 and UCB35625 that act either as antagonist, partial agonist, or full agonist according t

229 hat radiolabeled somatostatin (sst) receptor antagonists perform better than agonists in detecting ne

230 izing Abs and the class A scavenger receptor antagonist polyinosinic acid inhibited phagocytosis of a

231 of MDSC depletion/blockade (anti-Gr-1 + CCR2 antagonist) prevented outgrowth of BRAFi-resistant tumor

232 nselective muscarinic acetylcholine receptor antagonist, produces rapid antidepressant effects in pat

233 e release and that bath application of a KOR antagonist provides full rescue of both LTP induction an

234 The orthosteric antagonists quinuclidinyl benzilate (QNB) and N-methylsc

235 olol (beta-adrenergic and 5-HT1A/1B receptor antagonist), R-propranolol (5-HT1A/1B receptor antagonis

236 & AIMS: Although tumor necrosis factor (TNF) antagonists reduce many clinical features of inflammator

237 nt or RARgamma agonist) or truncate (RARbeta antagonist) regenerating limbs.

238 Recent evidence suggests that NMDAR antagonists relieve depressive symptoms by forming new s

239 Moreover, selective NPY2 and NPY5 receptor antagonists restored vascular integrity and limited HSPC

240 an orthosteric-tethered ligand binding-site antagonist results in bleeding, possibly owing to the im

241 Addition of an AHR antagonist reversed 2,3,7,8-tetrachlorodibenzo-p-dioxin-

242 comparison, MRS2500 behaved as surmountable antagonist rightward-shifting concentration-response cur

243 inase A (PKA) pathway, inhibited by the CB1R antagonist rimonabant and Gi uncoupler pertussis toxin,

244 inhibition was reversed by the CB1 receptor antagonist rimonabant in naive rats but not in CFA-treat

245 rdingly, local injection of the CB1 receptor antagonist rimonabant into the rostral ventromedial medu

246 The CB1 antagonist rimonabant precipitated withdrawal in mice tr

247 Moreover, progesterone receptor antagonist RU-486 partially reversed the effects of P4 o

248 microinjection of the progesterone receptor antagonist, RU486, into the AVPV reversed the prolonged

249 We used the insulin receptor antagonist S961 to induce severe insulin resistance, hyp

250 cophores were derived from the D3R-selective antagonists SB269,652 (1) and SB277011A (2) whose struct

251 The D1/5 receptor antagonist SCH23390 had no effect on instrumental behavi

252 vitro studies have shown that ifenprodil, an antagonist selective for GluN2B-containing NMDARs, rever

253 with decreased secretion of the soluble WNT-antagonist SFRP4, in surgical specimen-derived DD myofib

254 secretion of glucagon, a functional insulin antagonist, significantly contributes to hyperglycemia.

255 ggesting new modes of binding at the agonist-antagonist site and perhaps an allosteric action for het

256 Aldosterone antagonists slow the progression of chronic kidney disea

257 lls or with much lower cell density) between antagonist strains swarming toward each other.

258 l expression of osteogenic markers, and RARG-antagonist strongly drives lamin-A-dependent osteogenesi

259 imulated Nrip1 expression, whereas a pan-RAR antagonist strongly reduced it.

260 n and puncture sepsis (neurokinin-1 receptor antagonist survival = 79% vs vehicle = 54%).

261 op in intracellular Ca(2+) was attenuated by antagonists targeting multiple ionotropic and metabotrop

262 The effect of three antagonists, tetraiodoacetic acid (tetrac), triiodothyro

263 y our recently developed novel selective EP2 antagonists - TG4-155 and TG6-10-1, but not by EP4 selec

264 , many more sst2 sites were labeled with the antagonist than with the agonist.

265 Here, we identify ANGPTL4 as a Wnt signaling antagonist that binds to syndecans and forms a ternary c

266 hen WT mice were treated with a CB2-specific antagonist that caused a pronounced inhibition of HDM-in

267 t intravenous adenosine diphosphate-receptor antagonist that in the CHAMPION trials reduced the 48-ho

268 Sclerostin is an osteocyte-specific Wnt antagonist that inhibits bone formation.

269 , thus acting predominantly as a competitive antagonist that inhibits the cyclic-nucleotide dependenc

270 holog does not have significant affinity for antagonists that are able to block the human receptor.

271 hydro-5H-[1,2,3]triazolo[4,5-c]pyridine P2X7 antagonists that contain a synthetically challenging chi

272 in humans and the efficacy of CGRP receptor antagonists that evidently do no penetrate the CNS in ef

273 ys are inhibited by bis-indole-derived NR4A1 antagonists that inhibit nuclear export of the receptor

274 xoN activity.IMPORTANCE CoVs encode multiple antagonists that prevent or disrupt an efficient innate

275 As cimetidine is an H2 receptor antagonist, the authors hypothesize that this antiulcer

276 From a small library of sstr antagonists, the analog JR11 (Cpa-c[d-Cys-Aph(Hor)-d-Aph

277 Because of the lack of efficacious antagonists, the field has relied on synthetic peptides

278 INTERPRETATION: The current practice of MR antagonist therapy in primary aldosteronism is associate

279 been described as a low-permeant neutral CB1 antagonist, though its pharmacology is still unclear.

280 xperimental approach to identify novel hA3AR antagonists through succinct and efficient synthetic met

281 on of the RARG isoform and for RARG-specific antagonist to increase or maintain expression of lamin-A

282 atives as human adenosine A3 receptor (hA3R) antagonists to determine their kinetic profiles and affi

283 rovides a rationale for development of CXCR2 antagonists to inhibit or prevent metastatic spread of d

284 agonists can be combined with peripheral MOR antagonists to limit analgesic tolerance and OIH.

285 addition, focal application of GABA receptor antagonists to sensory ganglia triggered or exacerbated

286 FHV, whereas treatment with the KATP channel antagonist tolbutamide decreases survival and increases

287 ed with any of the following: 1) a vitamin K antagonist (VKA) throughout pregnancy; 2) low-molecular-

288 f low-dose aspirin, clopidogrel, a vitamin K antagonist (VKA), a direct oral anticoagulant, and combi

289 anticoagulants (NOACs) instead of vitamin K antagonists (VKAs) in patients with atrial fibrillation

290 Bleeding risk with vitamin K antagonists (VKAs) is closely related to the quality of

291 ction by HIV-2 and SIVsm encoding the SAMHD1 antagonist Vpx was insensitive to ETO treatment.

292 XEN-D0501 (a potent TRPV1 antagonist) was compared with SB-705498 in preclinical s

293 th at least one tumour necrosis factor (TNF) antagonist (which had failed in 96 [79%]).

294 he viral polyprotein or act as an interferon antagonist, which involves deubiquitinating and deISGyla

295 nd 5 were reported to be pan opioid receptor antagonists, while 6 was a MOR agonist.

296 NeoBOMB1 is a novel DOTA-coupled GRPR antagonist with high affinity for GRPR and excellent in

297 -tetrahydroisoquinoline-3-carboxamide, a pan antagonist with nanomolar affinity for all four subtypes

298 d selective A2A adenosine receptor (A2AAdoR) antagonist with reasonable ADME and pharmacokinetic prop

299 (Hor)-d-Aph(Cbm)-Lys-Thr-Cys]-d-Tyr-NH2), an antagonist with selectivity for sstr subtype 2, showed t

300 the hypothesis that a bradykinin B2 receptor antagonist would shorten time-to-resolution from ACE inh