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 alpha4beta2 nicotinic acetylcholine receptor partial agonist.

4 agonist CP55,940 acts as a GPR55 antagonist/partial agonist.

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

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

7 sks molecular actions of classically defined partial agonists.

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

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

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

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

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

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

14 ially discriminate between full agonists and partial agonists.

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

16 red the signaling initiated by the available partial agonists.

17 of the effects of stargazin on responses of partial agonists.

18 ft closure and transmembrane separation than partial agonists.

19 All these are partial agonists.

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

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

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

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

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

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

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

27 Unlike nicotine, this partial agonist acted without inducing tachyphylaxis.

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

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

30 ) in terms of binding affinity, although the partial agonist activity in the transrepressive assays d

31 class of PPARgamma ligand with both full and partial agonist activity in vitro and in vivo.

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

33 vity: the potency of agonists (or EC and the partial agonist activity of antisteroids (or PAA).

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

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

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

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

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

39 an activator to an inhibitor, revealing its partial agonist activity.

40 matically shift signaling from antagonist to partial agonist activity.

41 The partial agonists also displayed full antagonist activity

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

43 tartrate, a relatively specific alpha4beta2 partial agonist and antagonist, on key biomarkers that a

44 3-pyr-Cyt is a very weak alpha4beta2* nAChR partial agonist and like cytisine and varenicline has an

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

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

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

48 Our approach helps identify partial agonists and highlights allosteric interactions

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

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

51 ide clues as to the functional properties of partial agonists and to the conformational changes assoc

52 in generating a maximal signaling response (partial agonists) and possessed significantly decreased

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

54 pe of the receptor by two full agonists, two partial agonists, and an inverse agonist.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

69 nism has thrown light on the question of why partial agonists are not efficacious at keeping the chan

70 Partial agonists are useful tools for studying the activ

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

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

73 The dopamine partial agonist aripiprazole is increasingly used to tre

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

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

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

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

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

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

80 2 is associated with surface AMPARs, CNQX, a partial agonist at AMPARs associated with Type I TARPs,

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

82 /2A (100% response compared with glycine), a partial agonist at GluN1/2B and GluN1/2D (10% and 27%, r

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

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

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

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

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

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 examined multiple dosages of tropisetron, a partial agonist at the nAChR, for short-term effects on

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

110 461, a combination of a mu- and kappa-opioid partial agonist, buprenorphine, and a mu-opioid antagoni

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

112 agonists do not bind to the same site as the partial agonists but exhibit positive heterotropic coope

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

114 l transitions that determine the efficacy of partial agonists can provide information on the trigger

115 etic attributes and safety, two lead 5-HT(4) partial agonist candidates 2d and 3 were chosen for clin

116 a reduction in the currents elicited by the partial agonist cGMP.

117 ACh, and approximately 1.7 x 10(-4) with the partial-agonist choline.

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

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

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

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

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

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

124 systemic administration of the NMDA receptor partial agonist D-cycloserine, under the same behavioura

125 ning administration of the glycineB receptor partial agonist, D-cycloserine (DCS), has been shown to

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

127 s the competitive antagonist SR-95531 into a partial agonist, demonstrating that this linker is a key

128 tylfarnesylcysteine (AFC) as both a full and partial agonist depending on the PPARgamma target gene (

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

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

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

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

133 f transfected neurons to UFP-101 resulted in partial agonist effects.

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

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

136 Swapping TM2 had reciprocal effects on partial agonist efficacy.

137 terestingly, alpha1(K312E) exhibited reduced partial agonist efficacy.

138 e ligand-mimetic integrin antagonists act as partial agonists, eliciting similar activating conformat

139 ivated by the full agonist, glutamate, and a partial agonist, fluorowillardiine.

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

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

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

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

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

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

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

147 onists of G(i)-regulated cAMP production and partial agonists for D(2)R/beta-arrestin-2 interactions.

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

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

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

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

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

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

154 , a nicotinic acetylcholine receptor (nAChR) partial agonist, has been shown to reduce alcohol consum

155 Partial agonists have emerged as attractive therapeutic

156 D3R antagonists and partial agonists have shown especially promising results

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

158 ues of 25.3 and 66.2 nM) and two others were partial agonists (IC(50) values of 15.4 and 26.1 nM).

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

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

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

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

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

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

165 esulted in conversion of two AhR antagonists/partial agonists into full AhR agonists.

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

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

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

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

170 2-TARP gamma2 complex in the presence of the partial agonist kainate or the full agonist quisqualate

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

172 tivated by the full agonist glutamate or the partial agonist kainate, consistent with conductance sta

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

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

175 y ligand binding is greatest for willardiine partial agonists, least for antagonists, and intermediat

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

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

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

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

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

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

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

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

184 ts were incorporated into this region of the partial agonist [N-benzylTyr(1)]Dyn A-(1-11).

185 ss of the sensory inhibition pathway to this partial agonist, nor cause receptor upregulation, at the

186 gard to Adrp, Angptl4, and AdipoQ, but was a partial agonist of aP2, a PPARgamma target gene associat

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

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

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

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

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

192 been shown to exert pleiotropic effects as a partial agonist of nuclear peroxisome proliferator-activ

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

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

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

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

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

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

199 2-Me-5HT and tryptamine have been defined as partial agonists of 5-HT3 receptors on the basis of macr

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

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

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

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

204 We report that NO(2)-FA act as partial agonists of PPARgamma and covalently bind PPARga

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

206 Partial agonists of the alpha4beta2 nicotinic acetylchol

207 ymethyl)diarylhydantoin analogues as potent, partial agonists of the human androgen receptor.

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

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

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

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

212 brane helix 5 (Ser(5.42) and Ser(5.46)), but partial agonists only interact with Ser(5.42) (superscri

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

214 ands are classified as either full agonists, partial agonists or antagonists, depending on whether th

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

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

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

218 X, a competitive antagonist; kainate, a weak partial agonist; or when desensitization was blocked by

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

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

221 t was observed for acetylcholine and for the partial agonist pilocarpine.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

239 f binding of glutamate and kainate (full and partial agonists, respectively) to a soluble ligand-bind

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

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

242 The TAAR1 partial agonist RO5203648 was evaluated for its binding

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

244 The TAAR1 partial agonist RO5263397 also promoted wakefulness and

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

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

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

248 The uphill step in the partial agonist salbutamol induced activation is distinc

249 The binding of agonist norepinephrine or partial agonist salbutamol leads to the selection of a s

250 agonists carmoterol and isoprenaline and the partial agonists salbutamol and dobutamine.

251 A weakly cross-reactive partial agonist self-peptide could similarly induce thym

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

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

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

255 One possibility is that partial agonists sterically block full lobe closure but

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

257 As expected for a partial agonist, subsaturating concentrations of bupreno

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

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

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

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

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

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

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

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

266 Cytisine, a partial agonist that binds with high affinity to the alp

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

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

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

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

271 Weak partial agonists that promote a desensitized state of th

272 ond differences in efficacy between full and partial agonists, the complexities of the single channel

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

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

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

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

277 activation pathways for several agonists and partial agonists, using a Monte Carlo algorithm, and the

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

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

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

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

282 5800-fold mMC3R selective antagonist/slight partial agonist versus a 760 nM mMC4R full agonist (liga

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

284 5-HT3 receptor antagonist and an alpha7nAChR partial agonist, we found that it also binds to the ecto

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

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

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

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

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

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

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

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

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

294 4-phenylthiomorpholin-1-ium triflate, a weak partial agonist with a sulfonium isostere of the ammoniu

295 esensitizing responses, whereas kainate is a partial agonist with responses that are often described

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

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

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

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

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