ライフサイエンスコーパス: full agonist

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

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

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

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

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

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

7 those measured previously for the analogous full agonist.

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

9 ilar affinity, but only 2-AG functioned as 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 = 47.9 nM) as a moderately A(1)AR-selective full agonist.

14 eft closure are observed between partial and full agonists.

15 stability when bound to partial relative to full agonists.

16 annel activation with lower probability than full agonists.

17 least for antagonists, and intermediate for full agonists.

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

19 heart weight gain associated with PPARgamma full agonists.

20 om adopting the closed conformation seen for full agonists.

21 hydrophobic contacts that are distinct from full agonists.

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

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

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

25 aturable and specific manner and represented full agonists.

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

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

28 toward the active state as efficaciously as full agonists.

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

30 Only ATP and 2 methylthio ATP were full agonists.

31 efficacies ranging from inverse agonists to 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 previously observed with SPPARgammaMs versus full agonists.

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

36 ities of 70 SPPARgammaMs and seven PPARgamma full agonists.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

55 s found that the new 3-keto analogues showed full agonist activity in the T47D assay, while the refer

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

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

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

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

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

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

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

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

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

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

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

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

68 t DNQX, the partial agonist kainate, and the full agonists AMPA and glutamate.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

85 4-Hydroxytamoxifen is a full agonist at a transforming growth factor alpha targe

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

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

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

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

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

91 attentional effects of SKF81297, a selective full agonist at dopamine D(1) receptors, was assessed in

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

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

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

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

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

97 D-Serine is a full agonist at the glycine site on the N-methyl-D-aspar

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

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

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

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

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

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

104 ctane-3,5'-oxazolidin-2'-one] (4a), a potent full agonist at the rat alpha 7 nicotinic receptor, whic

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

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

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

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

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

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

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

112 otonin 5-HT(2B) receptor and were partial to full agonists at the 5-HT(2B) receptor.

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

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

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

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

117 M) relative to 5-HT (K(i) = 75 nM) and was a full agonist, at least as potent (8: K(act) = 3.6 nM) as

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

119 In native mouse acini, JMV-180 acted as a full agonist (both stimulation and inhibition of amylase

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

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

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

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

124 nduce a response, 2) CD3zeta is required for full agonist but not antagonist responses, and 3) differ

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

126 xample, and all of the compounds tested were full agonists but with reduced functional potency at thi

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

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

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

130 Full agonists can form hydrogen bonds with two conserved

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

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

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

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

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

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

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

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

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

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

141 king several adverse effects associated with full agonist drugs.

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

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

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

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

146 the minimal NDP-MSH fragment that possesses full agonist efficacy at the hMC4R.

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

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

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

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

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

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

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

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

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

156 unds 8 and 10 were potent, selective, nearly full agonists for beta(3)-AR.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

176 -180 acts as a partial agonist in rats and a full agonist in mice.

177 certain physiological circumstances and as a full agonist in others.

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

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

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

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

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

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

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

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

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

187 ary-hCB2 membranes, HU210 and 2-AG were also full agonists in stimulating [(35)S]GTPgammaS binding (E

188 affinity and that the cannabinoids acted as full agonists in stimulating [(35)S]GTPgammaS exchange,

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

190 that the two ligands now behaved as close to full agonists in this assay system.

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

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

193 7 was critical for affinity and potency of a full agonist, it had progressively less effect as the bi

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

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

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

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

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

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

200 97 and PF-04756956, which are reported to be full agonist ligands.

201 e ligand is higher with ligands showing this full agonist-like pattern.

202 6, and non-selective benzodiazepine receptor full agonists, midazolam and lorazepam, in rhesus monkey

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

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

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

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

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

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

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

210 hese observations, troglitazone behaves as a full agonist of PPAR-gamma in 3T3L1 adipocytes.

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

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

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

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

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

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

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

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

219 2DM) therapeutics TZDs (thiazolidinediones), full agonists of PPARgamma with robust antidiabetic prop

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

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

222 ChaW, the antagonist hexapeptide, acted as a full agonist on the I116A mutant.

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

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

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

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

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

228 24 of CCK-33) of CCK analogues representing full agonist, partial agonist, and antagonist of this re

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

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

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

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

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

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

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

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

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

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

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

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

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

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

243 11 (AM4054) exhibited high CB1 affinity and full agonist profile.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

262 ural B2 receptor ligand and, consequently, a full agonist, stimulated PI hydrolysis at high and low l

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

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

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

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

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

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

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

270 1f and 1g, all the epibatidine analogues are full agonists (tail flick test) in producing antinocicep

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

272 Glutamate is a full agonist that elicits strongly desensitizing respons

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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.