ライフサイエンスコーパス: partial agonist

1 tion of the first selective and potent TAAR1 partial agonist.

2 a-containing GABARs acutely, where GABA is a partial agonist.

3 is recapitulated by GTS-21, an alpha7 nAChR partial agonist.

4 he potential for evaluating the bias of very partial agonists.

5 sks molecular actions of classically defined partial agonists.

6 amoxifen, as well as other antiestrogens, as partial agonists.

7 NH(2)), naloxone, and naltrexone behave like partial agonists.

8 etitive antagonists CNQX and DNQX acted as a partial agonists.

9 g domain in the presence of several full and partial agonists.

10 , and equalization of efficacies of full and partial agonists.

11 MPA) and kainate receptors bound to full and partial agonists.

12 ially discriminate between full agonists and partial agonists.

13 with varenicline or lobeline, which are both partial agonists.

14 red the signaling initiated by the available partial agonists.

15 ally in target tissues where LABAs behave as partial agonists.

16 including novel antibodies, antagonists, and partial agonists.

17 a series of high-affinity dopamine receptor partial agonists.

18 onist 5,7-dichlorokynurenic acid (DCKA), the partial agonists 1-amino-1-cyclobutanecarboxylic acid (A

19 Potent GPR55 partial agonists (14b, 18b, 19b, 20b, and 21-24) have be

20 For GABA and the partial agonists 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyrid

21 BAA receptor subtype selectivity of the weak partial agonist, 5-(4-piperidyl)isoxazol-3-ol (4-PIOL),

22 HT and 5-carboxamido-tryptamine, but not the partial agonist 8-OH-DPAT, triggered internalization of

23 and can distinguish between agonists (cAMP), partial agonists (8-chlorophenylthio-cAMP), and super ag

24 le is an antipsychotic drug characterized by partial agonist activity at D(2) receptors to normalize

25 d abuse, with both activities relying on its partial agonist activity at mu opioid receptors.

26 gulated kinase (ERK) 1/2 phosphorylation and partial agonist activity for beta-arrestin recruitment,

27 tor (GR)-mediated gene induction, reduce the partial agonist activity of an antagonist, and increase

28 ), the potency of agonists (EC(50)), and the partial agonist activity of antisteroids (PAA).

29 ecular dynamics simulations suggest that the partial agonist activity of GQ-16 results from the compo

30 e mode of AF2ER activation is similar to the partial agonist activity of OHT for WT-ERalpha.

31 our results revealed complexities including partial agonist activity of TRPA1 antagonists, bidirecti

32 ecific substructural changes, which switched partial agonist activity to inverse agonist activity, an

33 Several showed partial agonist activity, with potency of 0.8-76 nM, mim

34 matically shift signaling from antagonist to partial agonist activity.

35 ate human AT1R bound to an AngII analog with partial agonist activity.

36 The partial agonists also displayed full antagonist activity

37 Typical for partial agonists, amorfrutins 1, 2, and B bind helix H3

38 alpha4beta2 nicotinic acetylcholine receptor partial agonist and alpha7 receptor full agonist varenic

39 D(2)-like receptors) compounds with diverse partial agonist and antagonist profiles, falling into th

40 nt agonist NS6740 converts to a conventional partial agonist and appreciably opens the channel in the

41 3-pyr-Cyt is a very weak alpha4beta2* nAChR partial agonist and like cytisine and varenicline has an

42 e, in an activated/pre-open state bound with partial agonists and a positive allosteric modulator, an

43 Both dopamine D3 receptor (D3R) partial agonists and antagonists have been implicated as

44 These IL-2 analogs acted as partial agonists and differentially affected lymphocytes

45 Our approach helps identify partial agonists and highlights allosteric interactions

46 (3)AR-selective nucleosides are low efficacy partial agonists and novel, nuanced modulators of the A(

47 ginning to reveal the mechanism of action of partial agonists and suggest new models for the mechanis

48 or with the allosteric inhibitor, Ro25-6981, partial agonists and the ion channel blocker, MK-801.

49 The NOP partial agonists and their SAR reported here may be usef

50 ne (a full opioid agonist), buprenorphine (a partial agonist), and naltrexone (an opioid antagonist).

51 f functionally different compounds (agonist, partial agonist, and antagonist) on 5-HT1B receptor (5-H

52 ave been used to interconvert GPCR agonists, partial agonists, and antagonists in order to achieve th

53 We designed a number of agonists, partial agonists, and antagonists of C3aR using our two-

54 ctivities, including cytokine superagonists, partial agonists, and antagonists, represent new ways of

55 tegorized our sigma-2 ligands into agonists, partial agonists, and antagonists.

56 ealing different behaviors as full agonists, partial agonists, and inverse agonists.

57 t KOP receptor selectivity acting as full or partial agonists, and one as an antagonist.

58 the activation helix (H12), consistent with partial agonist/antagonist actions.

59 We show that luteolin exhibits weak partial agonist/antagonist activity in transfections, in

60 ceptor agonists exhibiting low potency mGlu3 partial agonist/antagonist activity were identified.

61 endent breast cancer cell growth, but exerts partial agonist/antagonist behavior on gene expression.

62 and 3-methylcholanthrene, respectively, into partial agonists/antagonists.

63 o target the hormone receptors by the use of partial agonists/antagonists.

64 tion to a second agonist application for the partial agonists Ap5A and alphabetameATP, showed a compl

65 ngle all-atom GPCR simulation in the case of partial agonist ARC binding to the M2 receptor.

66 tetrol and Selective Human Estrogen-Receptor Partial Agonists are being evaluated in endocrine-resist

67 No KOR-selective partial agonists are currently available, and preclinica

68 y as alpha7 nicotinic acetylcholine receptor partial agonists are described.

69 bound by the full agonist iperoxo (IXO), the partial agonist arecoline (ARC), and the inverse agonist

70 f dopaminergic medications, including the DA partial agonist aripiprazole (APZ), have been inconsiste

71 The dopamine partial agonist aripiprazole is increasingly used to tre

72 Here we explore the use of a GABA partial agonist as a selective chemical tool in three di

73 ta2-nicotinic acetylcholine receptor (nAChR) partial agonists as novel antidepressants having a uniqu

74 The feasibility to design G protein-biased partial agonists as putative novel therapeutics was demo

75 s side effects, guiding the future design of partial agonists as selective GR modulators with an impr

76 It was also a less potent and weaker (18%) partial agonist at alpha4beta2 nAChRs.

77 Varenicline is a clinically available, partial agonist at alpha4beta2* and alpha6beta2* nicotin

78 e voltage clamp technique showed GHB to be a partial agonist at alphabetadelta- but not alphabetagamm

79 2 is associated with surface AMPARs, CNQX, a partial agonist at AMPARs associated with Type I TARPs,

80 ve previously shown that MG is a competitive partial agonist at GABA-A receptors.

81 /2A (100% response compared with glycine), a partial agonist at GluN1/2B and GluN1/2D (10% and 27%, r

82 aining receptors compared with glycine and a partial agonist at GluN2B-containing receptors.

83 cyano-7-nitroquinoxaline-2,3-dione (CNQX), a partial agonist at TARP-associated AMPARs, enhanced spon

84 the CB2 receptor (pEC50, 7.7 +/- 0.1) and a partial agonist at the CB1 receptor, although with a dec

85 he authors examined whether D-cycloserine, a partial agonist at the glutamatergic N-methyl-d-aspartat

86 supplementary use of D-cycloserine (DCS), a partial agonist at the glutamatergic N-methyl-D-aspartat

87 fluoroacetate trifluoroacetate), acting as a partial agonist at the hH(3)R [pEC(50) (reporter gene) 8

88 6'-guanidinonaltrindole (6'-GNTI), a potent partial agonist at the KOR receptor for the G protein ac

89 C acts as a full agonist at the M2AChR and a partial agonist at the M1 and M4 receptors, with full an

90 remained modest for most of these, one was a partial agonist at the M3 receptor without measurable M2

91 EuD was a partial agonist at the maximal doses tested.

92 d-cycloserine, a partial agonist at the N-methyl-d-aspartate receptor in

93 xcellent subtype selectivity while acting as partial agonists at alpha4beta2-nAChRs.

94 to create novel antidepressants that act as partial agonists at alpha4beta2-nicotinic acetylcholine

95 Although partial agonists at DA D2 receptors (D2Rs), like aripipr

96 We explain why strong antagonists behave as partial agonists at low concentration and predict that t

97 Most 3-benzylaminomorphinan derivatives were partial agonists at MOR and full agonists at KOR in the

98 ine acted as superagonists at the DmOctR but partial agonists at the BiOctR, and the two species dive

99 amma receptors but somewhat lower potency as partial agonists at the GABA(A)-rho(1) receptor.

100 eries of N-hydroxypyrazole-5-glycine (NHP5G) partial agonists at the GluN2 glutamate binding site as

101 units influence the pharmacology of full and partial agonists at the kappa opioid receptor.

102 sistently demonstrate efficacy; however, two partial agonists at the NMDA coagonist site, d-cycloseri

103 As partial agonists at trace amine-associated receptor 1 (T

104 duced when the receptor is stimulated by the partial agonist AZ10419369 and not by the antagonist GR1

105 The 5-HT1BR partial agonist AZ10419369 elicited a dose-dependent bip

106 g pocket, which might help shed light on its partial agonist behavior.

107 SSR180711, an alpha7-nAChR-selective partial agonist, blocked (18)F-ASEM binding in the baboo

108 , zoledronate, and POM2-C-HMBP, but not by a partial agonist BTN3 antibody.

109 ctivities, the antagonist diprenorphine, the partial agonist buprenorphine, and the full agonist phen

110 chieved through a combination of a mu-opioid partial agonist, buprenorphine (BUP), and a potent mu-op

111 461, a combination of a mu- and kappa-opioid partial agonist, buprenorphine, and a mu-opioid antagoni

112 The known mu-opioid receptor (MOR) partial agonist, buprenorphine, was structurally elabora

113 Administration of the serotonin receptor 1A partial agonist buspirone prevented the isolation-induce

114 ine), which at high concentrations acts as a partial agonist, but can be blocked by an open channel b

115 Unlike the dual D(2)R/D(3)R partial agonist cariprazine, compound 38 showed selectiv

116 e of the full agonist cAMP, but not with the partial agonist cGMP.

117 uoro 3,4-dideoxy-GalCer analogues appears as partial agonists compared to KRN7000 for iNKT cell activ

118 ta2-nicotinic acetylcholine receptor (nAChR) partial agonist (compound 5) was acquired.

119 d that the SSRI fluoxetine and the nicotinic partial agonist cytisine have synergistic effects in a m

120 d for 48 h to the full agonist nicotine, the partial agonist cytisine, or the competitive antagonist

121 d with bath application of the NMDA receptor partial agonist D-cycloserine (DCS).

122 e previously reported that the NMDA receptor partial agonist d-cycloserine administered after pavlovi

123 e psychoactive constituent of marijuana, the partial agonist Delta(9)-tetrahydrocannabinol (Delta(9)-

124 r to worsen dyskinesia expression, these NOP partial agonists did not attenuate or worsen dyskinesia

125 ppocampal neurons, but not LLC-PK1 cells and partial agonist displayed an effect only in serotonergic

126 n of peptide Hr10 and a modified form of the partial agonist drug tirofiban that act as "pure" antago

127 0 and modified tirofiban are as effective as partial agonist drugs in inhibiting vascular thrombosis

128 [betaCpe(34)]-NPY-(25-36) is a Y4R selective partial agonist (EC50 41 +/- 6 nM, Emax 71%) that binds

129 , suggesting that the toxicity is due to the partial agonist effect at M1 and M3 mAChRs, leading to D

130 subtype; calcium mobilization tests revealed partial agonist effects at M1 and M3 and antagonist acti

131 However, TM1 swaps increased partial agonist efficacy at both chimeras, and this was

132 d no effect on agonist potency but increased partial agonist efficacy at P2X2-1N and decreased it at

133 Swapping TM2 had reciprocal effects on partial agonist efficacy.

134 u-opioid receptor agonists, (eg, methadone), partial agonists (eg, buprenorphine), and alpha2-adrener

135 olone sulfate found in ICP can function as a partial agonist for FXR, resulting in the aberrant expre

136 ether, these data indicate that fisetin is a partial agonist for HCN2 channels.

137 RTI-102, a strong partial agonist for HS alpha4beta2 receptors, was effect

138 Here, we show that cAMP is a partial agonist for PKG, and we elucidate the mechanism

139 Phi-O-Me-cAMP is a weak partial agonist for purified Epac, but functioned as an

140 Buspirone is an anxiolytic drug and is a partial agonist for the serotonin 5-HT(1A) receptors as

141 Aiming to design partial agonists for a G-protein-coupled receptor based

142 its of TC-5619 and alpha7 nicotinic receptor partial agonists for cognitive dysfunction and negative

143 o) protein signaling, but are simultaneously partial agonists for D2R/betaArr interactions.

144 ts for the recruitment of Galpha(i1) but are partial agonists for Galpha(o), that the agonist activit

145 development of D3R-selective antagonists and partial agonists for substance abuse remains critically

146 dines as a novel chemotype of non-nucleoside partial agonists for the A2A adenosine receptor (A2AAR).

147 Hence, we have established that USSN are partial agonists for the TCR complex because of inductio

148 nism-based strategy for engineering cytokine partial agonists for therapeutic immunomodulation.

149 In light of the clarified partial agonist function of Ang2, we propose that clarit

150 ist to treat BC is potentially superior to a partial agonist given BPTPE's delayed induction of UPR a

151 operties, tandospirone, a selective 5-HT(1A) partial agonist, haloperidol, a D(2) antagonist, and pim

152 Partial agonists have emerged as attractive therapeutic

153 D3R antagonists and partial agonists have shown especially promising results

154 amino and carboxyl termini to the action of partial agonists (higher potency and efficacy of BzATP a

155 from an antagonist for cell migration and a partial agonist in other assays to a full agonist in all

156 15 was a partial agonist in vitro (hA(3)AR, cAMP inhibition, 31%

157 describe methods for estimating the CRCs of partial agonists in receptors that have a correlation be

158 cooperativity between the full agonists and partial agonists in various functional assays (in vitro

159 Furthermore, the effects of the nicotinic partial agonists in VSDi assays are significantly correl

160 T-126, a selective alpha7 nicotinic receptor partial agonist, in stable patients with schizophrenia.

161 studies, amphiregulin (AREG) functioned as a partial agonist, inducing only about half as much total

162 We discover that the activity of a partial agonist is heavily dependent upon the GABAA rece

163 s that are potent, selective 5-HT2C receptor partial agonists is described.

164 annel (GluCl) in complex with the allosteric partial agonist ivermectin, which provided insights into

165 diated currents-the relative efficacy of the partial agonist kainate (I(KA)/I(Glu) ratio 0.4) and a g

166 2-TARP gamma2 complex in the presence of the partial agonist kainate or the full agonist quisqualate

167 On GluA2(A621G), the partial agonist kainate showed efficacy similar to a ful

168 ural properties with an antagonist (CNQX), a partial agonist (kainate), and two full agonists (glutam

169 ect donecopride as a valuable dual (h)5-HT4R partial agonist (Ki = 10.4 nM; 48.3% of control agonist

170 r (KOR) agonist and mu opioid receptor (MOR) partial agonist ligands have been put forward as potenti

171 receptor bound to the full agonist 5-HT, the partial agonist LSD, and the inverse agonist Ketanserin.

172 These receptor models bound with partial agonists may be useful for structure-based desig

173 In contrast to antagonists, partial agonists may cause fewer side effects since they

174 in KOPr/dynorphin tone, especially with KOPr partial agonists, may hold potential for the treatment o

175 Antagonist and partial agonist modulators of the dopamine D3 receptor (

176 A partial agonist molecule (-)-34 (EC50 (GTPgammaS); D2 =

177 of the non-selective benzodiazepine receptor partial agonist MRK-696, and non-selective benzodiazepin

178 The smoking cessation agent varenicline, a partial agonist of alpha4beta2 nAChRs, reduces alcohol i

179 l (Delta(9)-THC), a cannabis constituent and partial agonist of brain cannabinoid receptor 1.

180 rt that the CB2 ligand GW405833 behaves as a partial agonist of GPR55 alone and enhances LPI signalin

181 Conversely, TAK-875 acted as a partial agonist of Gq/11-dependent GPR40 signaling relat

182 Notably, cCMP is a partial agonist of HCN channels, displaying an efficacy

183 is an orally available, potent and selective partial agonist of hGPR40 receptor, which reached phase

184 XMetA was found to function as a specific partial agonist of INSR, eliciting tyrosine phosphorylat

185 ministering multiple doses of tropisetron, a partial agonist of nAChR, for 1 day would affect cogniti

186 ded for its different behavior as a full and partial agonist of PPARalpha and PPARgamma, respectively

187 We identified amorfrutin B as a novel partial agonist of PPARgamma with a considerably higher

188 Unlike Rosi, VSP-51 is a partial agonist of PPARgamma with improved insulin sensi

189 Cytisine is a partial agonist of some nAChRs and has been used for smo

190 A novel partial agonist of the EPAC isoform 1 (EPAC1), I942, was

191 entration or applying d-cycloserine (DCS), a partial agonist of the GluN glycine binding site.

192 D-cycloserine (DCS), a partial agonist of the glycine co-agonist of the N-methy

193 mal eutomer - (R)-PZQ - which functions as a partial agonist of the human serotoninergic 5HT2B recept

194 We found that cinnabarinic acid acts as a partial agonist of type 4 metabotropic glutamate (mGlu4)

195 Acting as a partial agonist of vascular endothelial growth factor 2

196 2-Me-5HT and tryptamine have been defined as partial agonists of 5-HT3 receptors on the basis of macr

197 ands characterized in vitro as high-affinity partial agonists of D2R, antagonists of 5-HT6R, and bloc

198 less stable EGFR dimers than EGF-making them partial agonists of EGFR dimerization.

199 We show that bisphenols act as partial agonists of ERs by activating the N-terminal act

200 are low-potency (EC(50) = 80 muM to 2.1 mM), partial agonists of human Slo2.1 channels heterologously

201 Specific cGMP analogs are able to act as partial agonists of PfPKG.

202 Partial agonists of PPARgamma, such as INT131 (1), have

203 cribe our efforts to discover highly potent, partial agonists of S1P(1) with a shorter T(1/2) and inc

204 Partial agonists of the alpha4beta2 nicotinic acetylchol

205 oxidized analogue 7-hydroxymitragynine, are partial agonists of the human mu-opioid receptor and com

206 agynine and 7-hydroxymitragynine function as partial agonists of the human u-opioid receptor, while s

207 the analogs modified in position 8 were also partial agonists of the protein kinase C (PKC)-dependent

208 The effect of the V1a -AVP receptor partial agonist on PP was associated with an improvement

209 uM, while others were weaker antagonists (or partial agonists) on these receptors.

210 Varenicline acts as a nicotinic receptor partial agonist or antagonist depending on the presence

211 such as the thiazolidinediones and PPARgamma partial agonists or non-agonists.

212 and UCB35625 that act either as antagonist, partial agonist, or full agonist according to the recept

213 ct are asking whether agonists, antagonists, partial agonists, or channel blockers show the most prom

214 , responses to saturating concentration of a partial agonist, P4S, showed no rapid desensitization, s

215 oducing IP(3)-like molecules, referred to as partial agonists (PA), into the cell to determine the st

216 old selective for the MC3R over the muM MC4R partial agonist pharmacology.

217 antly increasing the maximal response to the partial agonist, pilocarpine.

218 lation between P(o) and rectification with a partial agonist, piperidine-4-sulfonic acid, and a gatin

219 onist (pK(i) = 8.70) and a 5-HT(1A) receptor partial agonist (pK(i) = 9.25, pD(2) = 9.03, E(max) = 47

220 YX-13, a novel NMDAR glycine-site functional partial agonist, produces an antidepressant-like effect

221 w dual PPARalpha/gamma ligand, LT175, with a partial agonist profile against PPARgamma and interactin

222 methyl cannabinol analogue 24 (AM4089) had a partial agonist profile, with high affinity and moderate

223 ve NMDA receptor modulator with glycine-site partial agonist properties that produces rapid antidepre

224 that I942 and, to a lesser extent, I178 had partial agonist properties towards EPAC1, leading to act

225 sidone, an atypical APD with potent 5-HT(1A) partial agonist properties, tandospirone, a selective 5-

226 this crucial residue in STIM2 endows it with partial agonist properties, which may be critical for li

227 aspartate (NMDA) modulator with glycine-like partial agonist properties; like the NMDA receptor antag

228 binding of the full agonist glutamate or the partial agonist propyl-NHP5G, which is strikingly differ

229 lysis of the binding properties of these two partial agonists provides insight into differences with

230 e sensitivity of a highly selective 5-HT(1A) partial agonist radioligand [(11)C]CUMI-101 to changes i

231 aphy scanning with [(11)C]CUMI-101, a 5-HT1A partial agonist radioligand, and functional magnetic res

232 first selective serotonin receptor (5-HT1AR) partial agonist radiotracer for positron emission tomogr

233 t priming step is the rate-limiting step and partial agonists require an increased number of priming

234 matopoietic expansion revealed that this SCF partial agonist retained therapeutic efficacy while exhi

235 idelines to investigate the nicotinic alpha7 partial agonist RG3487 (formerly MEM3454) in CIAS; 215 p

236 The TAAR1 partial agonist RO5203648 was evaluated for its binding

237 With the first potent and selective TAAR1 partial agonist, RO5203648, we show that TAAR1 is implic

238 activity (LMA) and the efficacy of the TAAR1 partial agonist RO5263397 (0.1,1,10 mg/kg, p.o.) on slee

239 The TAAR1 partial agonist RO5263397 also promoted wakefulness and

240 ects of the TAAR1 full agonist RO5256390 and partial agonist RO5263397 on sleep/wake, locomotor activ

241 nt, mice were given three doses of the TAAR1 partial agonist RO5263397, caffeine, or vehicle p.o.

242 etrameric rat GluA2 receptor in complex with partial agonist (S)-5-nitrowillardiine.

243 and the beta(2)-selective, G protein-biased partial agonist salmeterol depends on specific hydrogen

244 zed that a selective human estrogen receptor partial agonist (ShERPA) at ERalpha would provide such a

245 tetrol (E(4)) and a model Selective Human ER Partial Agonist (ShERPA) BMI-135.

246 hthalene-2-yl)piperazin-1-ium (2NDEP) a weak partial agonist, showed particularly favorable docking a

247 oxopyridine/7-oxopyrimidines as CB2 receptor partial agonists, showing that the functionality of thes

248 viously defined types of agonists (agonists, partial agonists, silent agonists, and ago-PAMs).

249 In contrast, 2-Me-5HT is not a genuine partial agonist since priming is not dramatically affect

250 by the relatively small Ca(2+) release this partial agonist stimulated.

251 enicline), a selective alpha4beta2 nicotinic partial agonist, successful quit attempts have significa

252 Together, these data indicate that partial agonists, such as 4-PIOL, may be useful for modu

253 es share some structural features with other partial agonists, such as MRL-24 and PA-082, that have s

254 lphabeta T cells develop from DP cells after partial-agonist T cell receptor (TCR) interactions with

255 ptor (ER)-targeting therapies, including the partial agonist tamoxifen and the pure antagonist fulves

256 the effects of an alpha7 nicotinic receptor partial agonist, TC-5619, on cognitive dysfunction and n

257 We have generated SAR based on a novel D2R partial agonist, tert-butyl (trans-4-(2-(3,4-dihydroisoq

258 104)) led to a contrasting biased allosteric partial agonist that activated solely G proteins, induce

259 -controlled trials indicate that cytisine, a partial agonist that binds the nicotinic acetylcholine r

260 ) is an N-methyl-D-aspartate (NMDA) receptor partial agonist that facilitates extinction of condition

261 d receptor antagonist, kappa opioid receptor partial agonist that has recently been approved in Europ

262 We engineered a mechanism-based SCF partial agonist that impaired c-Kit dimerization, trunca

263 discovered compound 38 (MS1768) as a potent partial agonist that selectively activates the G(i/o) pa

264 a useful mechanism for analyzing the bias of partial agonists that exhibit extreme bias.

265 Weak partial agonists that promote a desensitized state of th

266 estingly, both l-glucose-derived ligands are partial agonists: they are among the least efficacious a

267 receptors revealed that the efficacy of the partial agonist THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]

268 h efficacy and agonist binding, and when the partial agonist THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]

269 eveloped as nociceptin opioid receptor (NOP) partial agonists to explore a pharmacological hypothesis

270 veloped beta-arrestin2 (betaarr2)-biased D2R partial agonists to simultaneously target hyper- and hyp

271 caused by the binding of cAMP and of cCMP, a partial agonist, to the apo-CBD of HCN4.

272 ists estrone, E(2), and estriol, a benchmark partial agonist triphenylethylene bisphenol (BPTPE), and

273 he orthosteric activation by 5-HT and by the partial agonist tryptamine, and the allosteric activatio

274 n immunized monkeys, whereas (+)-EPI and the partial agonist varenicline engendered, respectively, co

275 t dosed with the alpha4beta2-nAChR-selective partial agonist varenicline.

276 channel opening with limited efficacy by the partial agonist varenicline.

277 oral and functional effects of the nicotinic partial agonists varenicline and sazetidine-A during wit

278 5800-fold mMC3R selective antagonist/slight partial agonist versus a 760 nM mMC4R full agonist (liga

279 In contrast, the effectiveness of partial agonists was similar to P2X1 levels for both of

280 , a dopamine D(3)/D(2) and 5-HT(1A) receptor partial agonist, was found to be effective in treating b

281 5-HT3 receptor antagonist and an alpha7nAChR partial agonist, we found that it also binds to the ecto

282 ite at the alpha4/alpha4 interface behave as partial agonists, we conclude that the ability to engage

283 stigate functional differences between these partial agonists, we utilized voltage-sensitive dye imag

284 We first found that unlike full agonists, Gq partial agonists were unable to trigger beta-arrestin2 r

285 ne, a potent and selective alpha4beta2-nAChR partial agonist, were designed by opening dioxane and re

286 CAd (2, 3) and 1/BQCAd hybrids (4) act as M1 partial agonists, whereas 1/TBPBd hybrids (5) did not ac

287 cy: the (R)-enantiomers are antagonists/weak partial agonists, whereas the (S)-enantiomers are much m

288 zol]-2' -amine (BMS-902483), a potent alpha7 partial agonist, which improved cognition in preclinical

289 ctrophysiology studies, AT-1001 was a potent partial agonist with 65-70% efficacy at both human and r

290 herapeutic value of a new V1 a -AVP receptor partial agonist with a preferential splanchnic vasoconst

291 4-phenylthiomorpholin-1-ium triflate, a weak partial agonist with a sulfonium isostere of the ammoniu

292 eu-Arg-Tyr-NH(2) (1), reported to be a Y(4)R partial agonist with high affinity (pK(i) Y(4)R: 8.43).

293 CGP12177 acted as a simple partial agonist with similar KB and EC50 values in the b

294 ptide (Arg-Leu-Arg-Tyr-NH(2)), being a Y(4)R partial agonist with unchanged Y(4)R affinity (pK(i): 8.

295 tuents affected intrinsic activity to afford partial agonists with a range of efficacies.

296 g can be exploited in M1 receptors to design partial agonists with graded efficacy.

297 as the first noncationizable short peptide (partial) agonist with high mu-opioid receptor affinity a

298 , a nicotinic acetylcholine receptor (nAChR) partial agonist, with bupropion, a norepinephrine/dopami

299 idine-3,5-dicarbonitrile (LUF5834), a potent partial agonist without a ribose moiety, compared with t

300 xplore a pharmacological hypothesis that NOP partial agonists would afford a dual pharmacological act