ライフサイエンスコーパス: full agonist

1 = 47.9 nM) as a moderately A(1)AR-selective full agonist.

2 cted phenotype in which PNU-120596 acts as a full agonist.

3 f simple competition between a partial and a full agonist.

4 ist induces a smaller cleft closure than the full agonist.

5 In some cases, Dex is no longer a full agonist.

6 n (+)-cannabidiol; abnormal-cannabidiol is a full agonist.

7 ociates as rapidly as possible yet remains a full agonist.

8 those measured previously for the analogous full agonist.

9 and converted it from a partial agonist to a full agonist.

10 mus-to-ms timescale dynamics when bound to a full agonist.

11 gnaling); also, here aplaviroc switched to a full agonist.

12 scein, is decreased 15-20% upon binding of a full agonist.

13 previously observed with SPPARgammaMs versus full agonists.

14 ene-regulatory responses, in comparison with full agonists.

15 ities of 70 SPPARgammaMs and seven PPARgamma full agonists.

16 eft closure are observed between partial and full agonists.

17 stability when bound to partial relative to full agonists.

18 annel activation with lower probability than full agonists.

19 least for antagonists, and intermediate for full agonists.

20 idues in helix 12 that are characteristic of full agonists.

21 heart weight gain associated with PPARgamma full agonists.

22 om adopting the closed conformation seen for full agonists.

23 hydrophobic contacts that are distinct from full agonists.

24 finity for other GnRHs and converted them to full agonists.

25 to the (N)-methanocarba nucleoside series of full agonists.

26 e less efficient at opening the channel than full agonists.

27 aturable and specific manner and represented full agonists.

28 t burst lengths were reduced relative to the full agonists.

29 st(4)-transfected cells, therefore acting as full agonists.

30 toward the active state as efficaciously as full agonists.

31 ydrolysis in mouse brain was compared to two full agonists.

32 possible by targeting hGPR40 with partial or full agonists.

33 boxamides as a novel class of CB(2) receptor full agonists.

34 ipid accumulation in HepG2 cells than potent full agonists 1 and 3 (WAY-254011) but were comparable i

35 ures of the human P2Y12R in complex with the full agonist 2-methylthio-adenosine-5'-diphosphate (2MeS

36 f great interest to develop an (18)F-labeled full agonist 5-HT(1A) receptor radiotracer.

37 ynamics adopted by the receptor bound to the full agonist 5-HT, the partial agonist LSD, and the inve

38 )tryptamine (11q) is a high affinity, potent full agonist (5-HT6 Ki = 2 nM, EC50 = 6.5 nM, Emax = 95.

39 ng whole cell functional assays, lead to the full agonist 9a at RXR (pEC50 of 8.2) and RXR-Nurr1.

40 CCR5 antagonist aplaviroc was converted to a full agonist (a so-called efficacy switch).

41 ct either as antagonist, partial agonist, or full agonist according to the receptor, the enantiomer,

42 ed robust enhancements in the potency of the full agonists, acetylcholine (ACh), carbachol, and oxotr

43 ChRs from different species, and compare the full agonist ACh with the weak agonist choline.

44 ffinity (Ki, D2 = 16.4 nM, D3 = 1.15 nM) and full agonist activity (EC50 (GTPgammaS); D2 = 3.23 and D

45 The F51L, I69T, and A219V hMC4Rs possessed full agonist activity and significantly decreased endoge

46 ubtype, only the chloro derivative 2a showed full agonist activity and submicromolar potency (EC(50)

47 RE), displaying various levels of partial to full agonist activity at ERalpha, while antagonizing est

48 ivatives showed high potency for binding and full agonist activity for Ca(2+) release.

49 variants demonstrated increased affinity and full agonist activity for NPR-A, whereas one was as pote

50 aza-ADP-ribose (3-deaza-cADPR[CH(2)]) showed full agonist activity for release of Ca(2+) ions from se

51 gonist, all of the cyclic peptides exhibited full agonist activity in the adenylyl cyclase assay usin

52 ffinity for kappa-opioid receptors exhibited full agonist activity in the adenylyl cyclase assay usin

53 ghlighting the importance of this region for full agonist activity of this peptide hormone.

54 The preferred compounds showed full agonist activity on FFA4 and complete selectivity o

55 al GTPgammaS binding assay, (-)-34 exhibited full agonist activity with picomolar affinity for D3 rec

56 Y(1) receptor with high affinity and exhibit full agonist activity, measured as inhibition of forskol

57 ation-dependent manner with full or close to full agonist activity.

58 Increasing the concentration of the full agonist adenosine from 10 to 100 micromol/L, howeve

59 Also the efficacy of the endogenous full agonist adrenaline was reduced by depolarization.

60 ant receptor still activated G proteins with full agonist affinity.

61 ite bind to the metastin receptor and act as full agonists, albeit with reduced potency compared to t

62 xperimental strategy included the use of the full agonist, Alexa488-CCK, bound to these receptors as

63 s in a proportional manner for both weak and full agonists alike, and this was despite the lack of in

64 GPR40 full agonists AM-1638 and AM-6226 stimulate GLP-1 and GI

65 s of the binding domain in the presence of a full agonist, an antagonist, and several partial agonist

66 In this work, we have utilized full agonist analogues of cholecystokinin (CCK) with Ala

67 ar receptor PPARgamma induced upon binding a full agonist and a partial agonist.

68 ural and computational analysis suggests the full agonist and modulator complex harbors an ion-permea

69 y a range of efficacies, with PbTx-1 being a full agonist and other derivatives acting as partial ago

70 Special cases include combinations of two full agonists and a full agonist plus a competitive anta

71 a series of pyrrolidine or piperidine based full agonists and attempted optimization to give compoun

72 ositive functional cooperativity between the full agonists and partial agonists in various functional

73 as shown to potentially discriminate between full agonists and partial agonists.

74 rm that may be applied to mixtures including full agonists and partial agonists.

75 ssembly for ligands previously classified as full agonists and reduced assembly for ligands previousl

76 novel pharmacology in that UTP and ITP were full agonists and UTP was more potent and efficacious th

77 agonist kainate showed efficacy similar to a full agonist, and competitive antagonists CNQX and DNQX

78 androgen receptor (AR) ligands, Cl-4AS-1, a full agonist, and TFM-4AS-1, which is a SARM.

79 inding domain is weaker for partial than for full agonists, and efficacy is correlated with the stabi

80 The apo, full agonist-, and arrestin-bound states of Y2R were pre

81 ing domain due to the binding of partial and full agonists are also observed in this functional recep

82 nsitizing activity that is characteristic of full agonists as well as mitigation of the effects leadi

83 4-Hydroxytamoxifen is a full agonist at a transforming growth factor alpha targe

84 Compound 28 was a full agonist at A2B and A2AARs and a low efficacy partia

85 tinic acetylcholine receptors (nAChRs) and a full agonist at alpha7 nAChRs.

86 is remarkable that varenicline is a potent, full agonist at alpha7 receptors with an EC50 of 18 +/-

87 UTP is a potent full agonist at both the human P2Y(4) (hP2Y(4)) and rat

88 e, we examined the effects of Win 55212-2, a full agonist at CB(1) receptors, and Delta(9)-tetrahydro

89 ors while C4beta-methyl analogue 9 acts as a full agonist at each of these targets.

90 asses with high affinity and functioned as a full agonist at each.

91 h higher affinity, but lower efficacy than a full agonist at equal receptor occupancy.

92 AICP is a full agonist at GluN1/2A (100% response compared with gl

93 imilar to N/OFQ, suggesting that MT7716 is a full agonist at NOP receptors.

94 chemotype APH199 (17) was found to act as a full agonist at the D(4) receptor showing significant bi

95 omeric neuronal nicotinic receptors, it is a full agonist at the homomeric alpha7 receptor.

96 runcation to uridine 5'-diphosphate (UDP), a full agonist at the human P2Y(14) receptor expressed in

97 results show that, in vitro, BuTAC acts as a full agonist at the M2AChR and a partial agonist at the

98 This probe, [Bpa(1),Ile(13)]motilin, was a full agonist at the motilin receptor that increased intr

99 We recently reported that tianeptine is a full agonist at the mu opioid receptor (MOR).

100 pha-cyclopropylmethylamino analogue 5h was a full agonist at the mu receptor with weaker agonist acti

101 T-12) in particular was shown to be a potent full agonist at the oxytocin receptor (OTR) in vitro wit

102 In contrast, ATP is a potent full agonist at the rP2Y(4) receptor but is a similarly

103 Cytisine and lobeline serve as full agonists at alpha4beta4-nAChR but are only partial

104 derivatives were partial agonists at MOR and full agonists at KOR in the [(35)S]GTPgammaS binding ass

105 Eu3+ -labeled S36057 and R2P were full agonists at MCHR1 when assessed by measurement of a

106 e receptors, partial agonists are as good as full agonists at opening the channel once flipping has o

107 is a unique finding since reports of natural full agonists at other voltage-dependent GPCRs only show

108 N(6)-Me analogue were also highly selective, full agonists at P2Y(1) receptors.

109 All of the proposed compounds were potent, full agonists at the A 2B AR in adenylate cyclase studie

110 (N)-methanocarba-5'-uronamide analogues were full agonists at the A(3)AR, as indicated by the inhibit

111 All compounds were full agonists at the calcitonin receptor with no activit

112 -amino and 7alpha-methylamino analogues were full agonists at the mu and delta receptors and antagoni

113 ha-d-glucopyranosyl 1,3,4-tris-phosphate are full agonists, being equipotent and 23-fold less potent

114 Generally, for full agonists BMS-986122 enhanced the binding affinity a

115 Furthermore, full agonist bound LBDs show faster dynamic motions betw

116 We suggest that the mobility of the full agonist-bound form primes the GPCR to couple to IBP

117 he cytoplasmic receptor side compared to the full agonist-bound nanobody-coupled form, suggesting tha

118 significant changes between the partial and full agonist-bound structures.

119 le of Tyr473 in mediating the interaction of full agonists but not SPPARgammaMs with the PPARgamma LB

120 yl ether of N-methylprolinol are alpha4beta2 full agonists, but only the latter is highly alpha4beta2

121 s were increased, and ATP was converted to a full agonist by replacing both the NH(2) terminus and EL

122 y axis of the channel in the presence of the full agonist cAMP, but not with the partial agonist cGMP

123 Moreover, the conformations induced by a full agonist can be distinguished from those induced by

124 Full agonists can form hydrogen bonds with two conserved

125 nergic receptor (beta(1)AR-m23) bound to the full agonists carmoterol and isoprenaline and the partia

126 stokinin receptor to the amino terminus of a full agonist CCK analogue.

127 unctional assay results indicated partial to full agonist characteristics of test compounds.

128 as the guinea pig isolated ileum, using the full agonist CP55940 as a positive control.

129 of mu-opioid receptors than exposure to the full agonist [D-Ala(2),N-MePhe(4),Gly-ol(5)]enkephalin (

130 rt, we demonstrate that SMRT is required for full agonist-dependent ERalpha activation.

131 ear receptor coregulators, compared with the full agonist dexamethasone and the antagonist RU486 (mif

132 We show that partial and full agonists differentially affect TM6 motions to regul

133 isostere of the potent dopamine D1-selective full agonist dihydrexidine.

134 inding interaction studies revealed that the full agonists do not bind to the same site as the partia

135 king several adverse effects associated with full agonist drugs.

136 The agonist efficacies were larger for the full agonists (E approximately 7-9) compared to the weak

137 Within a minute, full agonists (e.g., isoprenaline) stimulated large incr

138 onally constrained (S)-methanocarba-UDP is a full agonist (EC(50) = 0.042 microM).

139 This probe was a full agonist (EC(50) = 563 +/- 67 pm), stimulating cAMP

140 Interestingly, C5a(pep) exhibits full-agonist efficacy with respect to inhibiting lipopol

141 to discriminate 0.001 mg/kg of the nicotinic full agonist (+)-epibatidine ((+)-EPI).

142 estin recruitment of the hybrid ( S)-22, the full agonist epinephrine, and the beta(2)-selective, G p

143 er cell line, and results were compared with full agonists estrone, E(2), and estriol, a benchmark pa

144 hio and 2-chloromonophosphate analogues were full agonists exhibiting micromolar potency at P2Y(1) re

145 cotinic acetylcholine receptors (nAChRs) and full agonist for a7 nAChRs, has been approved for the tr

146 Each peptide was a full agonist for cAMP, but had a lower binding affinity

147 e most abundant endogenous cannabinoid and a full agonist for cannabinoid receptors (CB1 and CB2), is

148 We discover that C5a(pep) acts as a full agonist for Galpha(i) coupling as measured by cAMP

149 It is noteworthy that CYM-5442 was a full agonist for induction and maintenance of S1P(1)-dep

150 , the active metabolite of FTY720, acts as a full agonist for sphingosine-1-phosphate (S1P) receptors

151 h-affinity ligands ranged from antagonist to full agonist for the AR.

152 -melanocyte-stimulating hormone and ACTH are full agonists for all other MCRs.

153 , procaterol, and terbutaline which acted as full agonists for cAMP production but displayed very wea

154 ACh, carbachol and choline were full or near-full agonists for homomeric alpha7 receptor channels, bo

155 nilides are reported as potent and selective full agonists for the high affinity niacin receptor GPR1

156 t in this assay, piribedil and pergolide are full agonists for the recruitment of Galpha(i1) but are

157 nce of drug ligands show that binding of the full agonist formoterol shifts the conformational distri

158 e PKCdelta phosphorylation may distinguish a full agonist from a partial agonist for superoxide produ

159 range of agonist efficacies relative to the full agonist glutamate (<1-72%).

160 ng on whether channels were activated by the full agonist glutamate or the partial agonist kainate, c

161 omain conformation induced by binding of the full agonist glutamate or the partial agonist propyl-NHP

162 ry alpha-amine groups similar to that of the full agonist glutamate whose activation can be varied de

163 e probed the ligand-protein interactions for full agonists (glutamate and alpha-amino-5-methyl-3-hydr

164 (CNQX), a partial agonist (kainate), and two full agonists (glutamate and quisqualate) in the wildtyp

165 meric AMPA receptor (GluA3) activated by the full agonist, glutamate, and a partial agonist, fluorowi

166 re robust AMPA receptor (AMPAR) current than full agonists, glutamate or AMPA.

167 anecarboxylic acid (ACBC) and L-alanine, and full agonists glycine and D-serine.

168 We first found that unlike full agonists, Gq partial agonists were unable to trigge

169 he protein in a more closed-cleft form, with full agonists having a larger fraction in the closed-cle

170 sure as found in the complex with glycine, a full agonist, illustrating that the NR1 subunit provides

171 This compound profiled out as a full agonist in a cell-based transient transfection assa

172 n and a partial agonist in other assays to a full agonist in all assays.

173 , then deprotection afforded 10, which was a full agonist in Ca(2+)-release assays; its potency and b

174 o CB(1) or CB(2) receptors, yet it acts as a full agonist in relaxing rat isolated mesenteric artery

175 In functional studies, WAY-161503 was a full agonist in stimulating 5-HT2C-receptor-coupled [3H]

176 In contrast, activating Atr1a with full agonist in such a complex exhibited a positive allo

177 cADPR 7 was, unexpectedly, a weak but almost full agonist in SUH and was membrane-permeant in whole e

178 binding affinity (0.42 nM to MOR) and was a full agonist in the [(35)S]GTPgammaS binding assay.

179 CYM-5442 is a full agonist in vitro for S1P(1) internalization, phosph

180 trifluproxim (UCL 1470, 7) acted as a potent full agonist in vivo, having ED(50) = 0.6 +/- 0.3 mg/kg

181 ng has occurred, but are not as effective as full agonists in eliciting this early conformational cha

182 These compounds were also potent full agonists in relaxing electrically stimulated pig bl

183 All of the Z-compounds were full agonists in the uterotrophic assay, indicating that

184 the M2 muscarinic GPCR that is bound by the full agonist iperoxo (IXO), the partial agonist arecolin

185 e lipid bilayer and to follow the binding of full agonists (isoproterenol, epinephrine), a partial ag

186 7 was critical for affinity and potency of a full agonist, it had progressively less effect as the bi

187 h a mechanism in which choline is actually a full agonist, its maximum response being limited only by

188 tuated in distinct positions within a docked full agonist ligand and several acceptors distributed at

189 r conformation was probed with a fluorescent full agonist ligand, Alexa 488-conjugated Gly-[Nle(28,31

190 In vitro studies showed it to be a full agonist ligand, which selectively binds to OR with

191 slight partial agonist versus a 760 nM mMC4R full agonist (ligand 11).

192 a catechol ring found in all known dopamine full agonist ligands, suggesting that they may be novel

193 97 and PF-04756956, which are reported to be full agonist ligands.

194 The intravenous anesthetic propofol is a full agonist (maximal P(Open,peak) = 0.99).

195 6, and non-selective benzodiazepine receptor full agonists, midazolam and lorazepam, in rhesus monkey

196 (N)-methanocarba series (e.g., 3,4-difluoro full agonist MRS5698 31, K(i) 3 nM, human and mouse A(3)

197 Cells were exposed for 48 h to the full agonist nicotine, the partial agonist cytisine, or

198 lbutamol induced activation is distinct from full agonist norepinephrine, and originates from steric

199 r conformations of five different ligands, a full agonist, norepinephrine; a partial agonist, salbuta

200 physiologically relevant nucleotide AMP is a full agonist of A(1)R.

201 te both G(s) and G(i) proteins, fenoterol, a full agonist of beta(2)-adrenoceptor, selectively activa

202 2-Arachidonoylglycerol (2-AG) is acting as a full agonist of cannabinoid receptor 1 and 2.

203 Furthermore, ZK 756326 was a full agonist of CCR8, dose-responsively eliciting an inc

204 In comparison to fingolimod (1), a full agonist of S1P(1) currently marketed for the treatm

205 s of CVT-2759 and adenosine, a partial and a full agonist of the A1AdoR, on isoproterenol-stimulated

206 SEN78702, WYE-308775) a potent and selective full agonist of the alpha7 nAChR that demonstrated impro

207 ] amide (25, SEN15924, WAY-361789), a novel, full agonist of the alpha7 nAChR that was evaluated in v

208 Thus, taurine is a full agonist of the glycine receptors (GlyRs) in the VTA

209 -Deoxy-(S)-methanocarbaUDP was found to be a full agonist of the receptor and displayed a 10-fold hig

210 Some compounds became potent full agonists of beta-arrestin2 recruitment, while other

211 showed several compounds acted as partial or full agonists of delta or kappa receptors while retainin

212 N(6)-(3-substituted-benzyl), were nanomolar full agonists of human (h) A(3)AR and highly selective (

213 These triazololipopeptides are highly potent full agonists of KISS1R and are >100 selective over the

214 2DM) therapeutics TZDs (thiazolidinediones), full agonists of PPARgamma with robust antidiabetic prop

215 tent and selective series of isoxazole based full agonists of S1P1.

216 such as MRS1898 and MRS2346, are examples of full agonists of the human A3 AR.

217 A series of small-molecule full agonists of the prostaglandin E(2) type 4 (EP(4)) r

218 ta2 antagonistic properties while behaved as full agonists on recombinant alpha7 and on SHSY5Y cells.

219 ide fragments containing this epitope act as full agonists on the secretin receptor despite their lac

220 cleft closure of 29-30 degrees upon binding full agonists, one of the largest observed in the glutam

221 a given d[X(4)]AVP analogue may behave as a full agonist or as a partial agonist.

222 unctional mimetics of H2-RLX with selective, full agonist or positive allosteric modulator activity a

223 at the conserved glutamate in loop 9, act as full agonists or requisite coagonists.

224 These ligands are classified as either full agonists, partial agonists or antagonists, dependin

225 production, revealing different behaviors as full agonists, partial agonists, and inverse agonists.

226 on of 15 compounds active at FFAR1 either as full agonists, partial agonists, or pure antagonists.

227 n and T cell functional responses induced by full agonist peptides.

228 , the partial agonist buprenorphine, and the full agonist phenethyl-orvinol.

229 We developed two high-affinity, full agonist photolabile GLP1 probes having sites of cov

230 veloped and characterized two high affinity, full-agonist photolabile GLP1 probes having sites for co

231 gs, because the currently marketed PPARgamma full agonists, pioglitazone and rosiglitazone, have been

232 lude combinations of two full agonists and a full agonist plus a competitive antagonist.

233 was tetrameric in both, and activation by a full agonist plus GTPgammaS reduced the oligomeric size

234 eptide library to discover molecules with nM full agonist potency and efficacy to the L106P, I69T, I1

235 Direct photoaffinity labeling with a full agonist probe confirmed the spatial approximation o

236 d conformation, reinforcing the concept that full agonists produce similar conformational changes.

237 old selectivity over the MT1 receptor, and a full agonist profile (GTPgammaS test), being the most po

238 11 (AM4054) exhibited high CB1 affinity and full agonist profile.

239 FKN was necessary for the high-affinity and full agonist properties of FKN at CX3CR1.

240 esence of the partial agonist kainate or the full agonist quisqualate together with a positive allost

241 Potencies of the full agonists R-(+)-beta-(aminomethyl)-4-chlorobenzenepr

242 The cannabinoid receptor full agonist [(R)-(+)-[2,3-dihydro-5-methyl-3[(4-morphol

243 The cannabinoid receptor full agonists [(R)-(+)-[2,3-dihydro-5-methyl-3[(4-morpho

244 e effect-associated genes, whereas PPARgamma full agonists regulated both gene sets proportionally.

245 S test), being the most potent MT2-selective full agonist reported to date.

246 gnalling induced by LTE4 but did not restore full agonist responses at the gene expression level.

247 second experiment, the effects of the TAAR1 full agonist RO5256390 and partial agonist RO5263397 on

248 cular adverse effect profile compared to the full agonist rosiglitazone.

249 Smo) protein as effectively as the known Smo full agonist, SAG.

250 ties into positions 2, 15, 20, 24, and 25 of full agonist secretin analogues.

251 In this work, we used two high-affinity, full-agonist, secretin-like photolabile probes having si

252 hly brain-penetrant LXRalpha-partial/LXRbeta-full agonist selectively kills GBM cells in an LXRbeta-

253 tation increased the apparent potency of the full agonist, serotonin (5-HT), and the partial agonist,

254 pendent activation and their expression of a full agonist signaling activation pattern, CD4+CD28- cel

255 In comparison with PPARgamma full agonists, SPPARgammaM 6 (MK0533) displayed diminish

256 The calculated pathways for the full agonists start with an energy downhill step leading

257 Each analog was shown to be a full agonist, stimulating cAMP accumulation in receptor-

258 Classical BZ full agonists such as diazepam, which maximally enhance

259 ns at the alpha-amine group are stronger for full agonists such as glutamate and AMPA as evidenced by

260 Results clearly indicate that full agonists such as glutamate and AMPA induce similar

261 PPARgamma activation by full agonists such as thiazolidinediones has shown poten

262 However, stimulation with a full agonist, such as nicotine, produces rapid tachyphyl

263 PPARgamma full agonists, such as thiazolidinediones (TZDs), are ef

264 1f and 1g, all the epibatidine analogues are full agonists (tail flick test) in producing antinocicep

265 intraepithelial lymphocytes (IELs), require full-agonist TCR interactions.

266 Glutamate is a full agonist that elicits strongly desensitizing respons

267 Each bifunctional probe was a full agonist that labeled the receptor specifically and

268 covery of a unique and potent class of GPR40 full agonists that engages the enteroinsular axis to pro

269 embers of two chemical series of partial and full agonists that have been identified, radioligand bin

270 ferator-activated receptor gamma (PPARgamma) full agonists that have been widely used in the treatmen

271 amate, AMPA, quisqualate, and 2-Me-Tet-AMPA, full agonists that vary in potency by up to two orders o

272 (RHS) carboxylate analogues were found to be full agonists that were modestly selective against beta(

273 Whereas the (S)-enantiomer behaved as a full agonist, the biased ligand (R)-4 induced poor G pro

274 he beta(2) adrenergic receptor is bound to a full agonist, the G protein coupling domain exists in tw

275 aMs interact with PPARgamma differently from full agonists, thereby providing a physical basis for th

276 the Hill slope, and converts taurine from a full agonist to a partial agonist; these data are consis

277 igand (K(i) = 56 +/- 8 nM) that was a potent full agonist to stimulate cellular cAMP (EC(50) = 236 +/

278 Our work concludes that the use of a full agonist to treat BC is potentially superior to a pa

279 by a diverse spectrum of drugs ranging from full agonists to partial agonists, antagonists, and inve

280 tial energy landscape of the receptor by two full agonists, two partial agonists, and an inverse agon

281 Although the full agonists U50,488, salvinorin A, nalfurafine, and dy

282 The bivalent ligands are H(2)R partial or full agonists, up to 2 orders of magnitude more potent t

283 receptor partial agonist and alpha7 receptor full agonist varenicline in rats that self-administered

284 rrent report, two potent and selective 5HT2C full agonists, WAY-163909 (2) and vabicaserin (3), were

285 anthranilide and cycloalkene carboxylic acid full agonists were discovered with excellent in vitro ac

286 hiazolidinedione (TZD) and non-TZD PPARgamma full agonists were reduced in a correlative manner.

287 Five TAS2R structurally distinct full agonists were studied to ascertain biasing away fro

288 Among them, 22 and 24 behaved as full agonists when compared to the endogenous GPR40 liga

289 and channel gating; AMPA is a high-affinity full agonist, whereas kainate is a low-affinity partial

290 Quisqualate is a high-affinity, full agonist which like AMPA and glutamate elicits maxim

291 f an indane based series of ghrelin receptor full agonists which led to a sustained increase of insul

292 rent efficacies, from inverse to partial and full agonists, which transduce cellular signals at diffe

293 0) values of 1 nM or less and functioning as full agonists while the (S)-enantiomers displayed modera

294 Thus, 11 is a potent full agonist with selectivity for the 5-HT2 receptor and

295 t have antidiabetic efficacy comparable with full agonists with improved tolerability in preclinical

296 Only a few compounds were full agonists with most of them possessing intrinsic act

297 -thiotriphosphate), and benzoyl ATP were all full agonists with potencies similar to those of ATP and

298 This series yields several non-imidazole full agonists with potencies varying with the alkyl subs

299 The latter and 19 behave as full agonists with regard to cAMP production and apelin

300 binding affinities for CXCR4 and are Galphai full agonists with robust chemotactic properties.