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1 c ER agonist) or genistein (ERbeta-selective agonist).
2 rs gating independently of activation by any agonist.
3 ugmented by the addition of a long-acting ss-agonist.
4 ified as either a full or partial muscarinic agonist.
5 ioid receptor antagonists, while 6 was a MOR agonist.
6 ccharide (LPS), a Toll-like receptor (TLR)-4 agonist.
7 exposed to spinal administration of a D1/D5 agonist.
8 g in its activity as a kappa-opioid receptor agonist.
9 low m.w. moieties were removed, it became an agonist.
10 re labeled with the antagonist than with the agonist.
11 didate for the treatment of T2DM as a GLP-1R agonist.
12 in cis, that is shared with a BTLA antibody agonist.
13 d by thermal pain or a kappa opioid receptor agonist.
14 arget neuroendocrine tumors (NETs) than sst2 agonists.
15 but variable aggregation defects with other agonists.
16 which requires intracellular delivery of its agonists.
17 tial between soluble and membrane-bound CD40 agonists.
18 Some flavones are also T2R agonists.
19 e Dectin-1 antagonists and two were Dectin-1 agonists.
20 a functional switch from agonists to inverse agonists.
21 or resting receptors activate and then bind agonists.
22 athways similar to those activated by opioid agonists.
23 as a new series of potent and selective TLR7 agonists.
24 hanges in vascular tone induced by vasomotor agonists.
25 to impart full efficacy to the partial GABA agonists.
26 creased SOCE, particularly at lower doses of agonists.
27 ning the range of full, partial, and inverse agonists.
28 c administration of mu-opioid receptor (MOR) agonists.
29 gonists compared with clinically widely used agonists.
30 hannels, and this occurred in the absence of agonists.
31 designed as potential liver X receptor (LXR) agonists.
34 systemically administered fluorescent GLP-1R agonist accesses the LDTg and is juxtaposed with neurons
35 ther as antagonist, partial agonist, or full agonist according to the receptor, the enantiomer, and t
37 we identify that cold temperatures and Adrb3 agonists activate distinct cellular populations that exp
39 5-HT2C agonist with potent 5-HT2B and 5-HT2A agonist activities, which is approved for treating obesi
41 covery of a minor enantiomeric impurity with agonist activity led to the finding that enantiomers (R,
42 ed using PAMs that also exhibited allosteric agonist activity, leaving open the possibility that dire
50 , these studies identify tapinarof as an AhR agonist and confirm that its efficacy is dependent on Ah
51 tate cancers, none had sst2 binding with the agonist and only 4 had a weak binding with the antagonis
52 atorial treatment incorporating soluble CD40 agonist and pharmacological inhibition of Trx-1 was func
54 review the cardiovascular actions of GLP-1R agonists and DPP-4 inhibitors, with a focus on the trans
55 lled despite treatment with long-acting beta-agonists and medium-to-high doses of inhaled glucocortic
56 e use of pathogen recognition receptor (PRR) agonists and the molecular mechanisms involved have been
58 blood, stimulated with Toll-like receptor 7 agonist, and analyzed by means of extracellular flux ana
59 ficacy agonist, buprenorphine a low efficacy agonist, and diprenorphine an antagonist at the MOPr.
60 thrombin and factor Xa, which are known PAR agonists, and cause microthrombosis in liver microcircul
63 tive, suggesting new modes of binding at the agonist-antagonist site and perhaps an allosteric action
64 n established endocrine disruptor with mixed agonist/antagonist activity acting via endogenous estrog
69 Glucagon-like peptide 1 receptor (GLP-1R) agonists are increasingly being used as treatment for ty
70 Radiolabeled somatostatin (sst) receptor agonists are integral to the diagnosis of gastroenteropa
71 hyperlipidemia and hypothalamic injury, MC4R agonists are nevertheless more effective to reduce food
72 norphine-naloxone (BUP-NX), a partial opioid agonist, are pharmacologically and conceptually distinct
74 e potential therapeutic application of a p53 agonist as a treatment to accelerate this process in pat
76 ociated with surface AMPARs, CNQX, a partial agonist at AMPARs associated with Type I TARPs, evoked w
78 % response compared with glycine), a partial agonist at GluN1/2B and GluN1/2D (10% and 27%, respectiv
83 f two pathways that connect to form a cycle: Agonists bind to resting receptors that then become acti
85 on and recycling to the plasma membrane with agonist binding inducing receptor retention along the in
90 med that norbuprenorphine is a high efficacy agonist, buprenorphine a low efficacy agonist, and dipre
92 ively, our data support the idea that opioid agonists can be combined with peripheral MOR antagonists
93 (DCS), which is a glycine site NMDA receptor agonist, can enhance extinction of conditioned fear resp
98 ling and contrasted with responses to an end agonist chemoattractant (C5a), for which a stable gradie
99 elial cell cultures and intestine after cAMP agonists, cholera toxin, or heat-stable enterotoxin of E
100 n channel whose deactivation is sensitive to agonist concentrations that do not directly activate the
101 rovide evidence that ASICs show such steeply agonist-dependent deactivation because of strong coopera
102 f 18 compounds (mixture of anabolics, beta-2 agonists, diuretics, stimulants, narcotics, and beta-blo
104 th C-terminal CB1R domains that could affect agonist-driven, beta-arrestin-mediated internalization o
105 erial infusion of phenylephrine (PE; alpha1 -agonist) during ATP or control vasodilatator infusion, b
107 s discovery of nine compounds that were MC3R agonists (EC50 < 1000 nM) and MC4R antagonists (5.7 < pA
108 arallel manner without affecting the maximum agonist effect (Emax) but antagonized insurmountably (su
110 nsory neurons contributes to this low deltaR agonist efficacy in vivo by limiting surface deltaR expr
112 brain barrier-impermeant PPARgamma-selective agonist, elicited antidepressant- and anxiolytic-like be
113 ) but antagonized insurmountably (suppressed agonist Emax) in signaling events such as guanosine 5'-3
114 derived DCs enabled benchmarking of the TLR8 agonist-encapsulating polymersome formulations against c
118 ollowing intra-PVT delivery of either GLP-1R agonist, exendin-4 (Ex4), or GLP-1R antagonist, exendin-
125 of the clinical use of nicotine and related agonists for treating cognitive deficits, these data sug
127 assay, we observed that several constrained agonists generated by a cycloaddition reaction displayed
128 ecessary for the effects of exogenous GLP-1R agonists (GLP-1RA) or endogenous GLP-1 on these paramete
132 obilization regimen utilizing a unique CXCR2 agonist, GRObeta, and the CXCR4 antagonist AMD3100.
133 Here, we show that a highly selective TLR7 agonist, GS-9620, activated HIV from peripheral blood mo
134 an osmotic gradient and the selective TRPV4 agonist GSK1016790A, enhanced TRPV4 activation was obser
135 , a glucagon-like peptide-1 (GLP-1) receptor agonist, has been shown to reduce food intake and to inc
138 In animal models of FXS and of ASD, GABA-B agonists have improved both brain and behavioral phenoty
140 prevented by combination with T-cell immune agonist immunotherapies resulting in superior therapeuti
142 On treatment with the toll-like receptor 7 agonist imquimod (IMQ), Trim32 knockout mice displayed c
144 antagonist for cell migration and a partial agonist in other assays to a full agonist in all assays.
146 g concentration-response curves of all three agonists in a parallel manner for all signaling pathways
147 s (binding free energies) of these and other agonists in adult-type mouse AChRs having a mutation(s)
148 st) receptor antagonists perform better than agonists in detecting neuroendocrine tumors (NETs).
149 ggest a therapeutic potential of alpha7nAChR agonists in early re-programming of microglia in neonate
150 onclude that increased effectiveness of MC4R agonists in obesity may be an unexpected outcome of neur
152 m donors with highly responsive platelets to agonists in vitro assessed by flow cytometry (high-respo
153 AJs are sensitive to pressure and vasomotor agonists in VSMCs and support a functional role of N-cad
154 nduced by injection of several different TLR agonists, including those for TLR2, TLR7, and TLR9.
156 rast, PKC activation caused a lower level of agonist-independent KOPR internalization, compared with
158 man B cells, BCR ligands that deliver a TLR9 agonist induce an initial proliferative burst that is fo
160 depletion from the PM was achieved either by agonist-induced activation of phospholipase C beta or wi
166 hat receptor internalization is required for agonist-induced phosphorylation of extracellular signal-
168 nth-old C57BL/6J mice with the FXR-TGR5 dual agonist INT-767 induced caloric restriction-like effects
169 injection of small amounts of GABAA-receptor agonists into an upper brainstem region named the mesopo
170 or alpha (Ppara), and treatment with a Ppara agonist is sufficient to rescue the loss of beige adipoc
173 tor 2 antagonist AM630 (10 mg/kg) or inverse agonist JTE907 (3 mg/kg) during immunization heightens t
174 ence showing that activation of PPARdelta by agonist L165041 in mice increased hepatic LPCAT3 mRNA ab
176 nduced by the gonadotropin-releasing hormone agonist, leuprolide acetate; leuprolide plus estradiol;
181 te/macrophage cells challenged with the TLR4 agonist LPS and TLR2 agonists lipoteichoic acid and zymo
183 ast, IL-1beta release stimulated by the TLR4 agonist LPS is independent of both pannexin-1 and P2X7 a
184 se studies suggest that an RARalpha specific agonist may afford a new strategy for lipid-lowering and
185 l proof of principle that an apelin receptor agonist may be of therapeutic use in PAH in humans.
186 mmunized with NPs containing TLR4 and TLR7/8 agonists mixed with soluble recombinant SIVmac239-derive
189 (the parent cysLT) or the selective CysLT2R agonist N-methyl LTC4 to allergen sensitized wild-type m
193 o treatment with either lithium chloride, an agonist of canonical Wnt signaling, or the DKK inhibitor
195 , a novel brain-penetrant antagonist/inverse agonist of H3 receptors, on AHN (proliferation, maturati
198 eal that TRV120027, a beta-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), st
199 -moderate AD, with other PDE4 inhibitors, an agonist of the aryl hydrocarbon receptor, Janus kinase i
201 throughput screen to identify small-molecule agonists of TFEB and discover three novel compounds that
202 as emerged as a new therapeutic target since agonists of this receptor induce rapid antidepressant-li
203 ce we now report that the effects of mGlu2/3 agonists on betaAR-mediated increases in cAMP accumulati
204 ith affinity for AChBP showed only two to be agonists on the alpha7-nAChR below 10 muM concentration.
207 , guanosine 5'-O-(thiotriphosphate) and GPCR agonists only weakly activate the TRPC5R593A mutant, whe
210 s show that pilocarpine can act as either an agonist or antagonist of M3R, depending on the cell type
211 hedgehog pathway by addition of a Smoothened agonist or by addition of exogenous Shh, or neutralizing
212 onal mimetics of H2-RLX with selective, full agonist or positive allosteric modulator activity agains
214 35625 that act either as antagonist, partial agonist, or full agonist according to the receptor, the
216 om human monocytes is stimulated by the TLR2 agonists Pam3CSK4 or FSL-1, as well as the TLR4 agonist
217 e shown that treatment with the KATP channel agonist pinacidil increases survival of bees while decre
218 elling and mutagenesis studies indicate that agonist positive allosteric modulators target the same g
220 lays significantly increased MOR binding and agonist potency and a distinct binding mode compared wit
225 surrogates present in the beta2-adrenoceptor agonists procaterol and BI-167107 (4), we designed and s
227 h subsaturating stimuli, indicating that the agonist promotes channel opening similar to that of volu
229 e (NMDA) modulator with glycine-like partial agonist properties; like the NMDA receptor antagonist ke
231 to the pathophysiology of FXS as the GABABR agonist (R)-baclofen rescued the imbalances between exci
232 ne phenylpropionate (Nandrosol) and the beta-agonist ractopamine administration in veal calves, and i
234 sed models demonstrate that commensal GPR119 agonists regulate metabolic hormones and glucose homeost
238 rofile to currently available GLP-1 receptor agonists, representing a potential treatment option for
239 e or concurrently with somatostatin receptor agonists represents a potential therapeutic approach in
242 ression and enhanced responsiveness to GLP1R agonists, resulting in improved glucose tolerance, cAMP
243 nitrile, an estrogen receptor beta selective agonist, results in NRF2 activation, normalization of gl
246 imidazoquinoline Toll-like receptor (TLR) 8 agonists robustly activate newborn DCs but can result in
247 nteraction between this benzene ring and the agonist's quaternary ammonium (QA) and (2) AChRs respond
249 ression can promote autoimmunity by limiting agonist selection of self-reactive thymocytes into the T
250 MCs from MS patients stimulated with a TLR-9 agonist showed reduced expression of general control non
251 Poly(I:C)], TLR4 (LPS), and TLR7 (imiquimod) agonists showed decreased proliferation and a reduced to
252 a rapidly acting peripheral beta-adrenergic agonist similar to adrenaline, to induce sensations of p
253 c current was enhanced by dopamine or the D1 agonist SKF81297 but not quinpirole, whereas the amplitu
257 ng glucagon-like peptide-1/glucagon receptor agonists such as G49 represent a novel therapeutic appro
258 henylephrine (PE), a well known hypertrophic agonist, suppresses autophagy and that activation of foc
259 els, and cyst growth in response to (1) TGR5 agonists (taurolithocholic acid, oleanolic acid [OA], an
260 TPA release was not augmented by any of the agonists tested but urokinase was released by IL-1, TNF-
262 We engineered a mechanism-based SCF partial agonist that impaired c-Kit dimerization, truncating dow
263 iew evidence suggesting that low doses of DA agonists that effectively treat TS decrease both phasic
264 complex with iperoxo, we explored potential agonists that lacked the highly conserved functionalitie
266 series of potent non-prostanoid IP receptor agonists that showed oral efficacy in the rat monocrotal
267 are physiologic mediators and pharmacologic agonists that stimulate resolution of inflammation and i
270 rventions with demonstrated efficacy: opioid agonist therapy (OAT), needle and syringe programs (NSPs
271 pment sharing and lower prevalence of opioid agonist therapy were associated with HCV incidence in ci
274 e in the ability of mu-opioid receptor (MOR) agonists to inhibit sIPSCs in POMC neurons when MORs wer
276 sts alone-and to develop immunoresolvents as agonists to test resolution pharmacology and their role
278 Our results demonstrate how resistance to agonist toxins can evolve and that such genetic changes
279 he K(d)M282-90 CD8(+) T cell response in TLR agonist-treated neonates could be blocked with Abs again
281 ence, and is long-term maintenance of opioid agonist treatment associated with differences in efficac
282 We investigated responses to cholinergic agonist treatment vs. neurostimulation by electric field
285 Clinical Question: Are different opioid agonist treatments (eg, methadone vs buprenorphine) asso
286 We reported previously that the selective agonist U50,488H promoted phosphorylation of the mouse k
287 D3 or calcitriol), a naturally occurring VDR agonist, VDR 4-1 therapy even at high doses did not indu
289 sity, 844 +/- 168 dpm/mg of tissue) with the agonist whereas 12 had a high binding (mean density, 4,4
290 rmore, pharmacological treatment with a Drd3 agonist, which increases Drd3(LS) neuronal activity, nor
291 esponses to Toll-like receptor-2, -3, and -4 agonists, which associated with decreased reactive oxyge
292 tra-PL injection of corticosterone, the CB1R agonist WIN 55,212-2, or the monoacylglycerol lipase inh
293 doxically, the nonselective CB1/CB2 receptor agonist WIN55212 inhibited GABAergic mIPSCs in both naiv
294 thiomorpholin-1-ium triflate, a weak partial agonist with a sulfonium isostere of the ammonium pharma
295 that is mediated through the presence of an agonist with an appropriate vibrational state to accept
297 ects were observed with lorcaserin, a 5-HT2C agonist with potent 5-HT2B and 5-HT2A agonist activities
298 mproved or novel new compounds, including D1 agonists with better pharmacokinetics, functionally sele
299 the location and distribution of five beta2 agonists with distinct clinical durations and onsets of
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