ライフサイエンスコーパス: inverse agonist

1 RO-alpha (an agonist) but not with IP-10 (an inverse agonist).

2 racterize a T2R endogenous antagonist and an inverse agonist.

3 the growth plate, enabling ICI to act as an inverse agonist.

4 that is important for ORG27569 to act as an inverse agonist.

5 b) acted on the US28 receptor as a nontoxic, inverse agonist.

6 imonabant, the first clinically approved CB1 inverse agonist.

7 nal change in H5 and therefore it acts as an inverse agonist.

8 full agonists, two partial agonists, and an inverse agonist.

9 otoswitchable tethered neutral antagonist or inverse agonist.

10 expressed salamander cone opsins, acting an inverse agonist.

11 ype receptor, which was reversed by T140, an inverse agonist.

12 lethynyl-pyridine (MPEP), an mGluR5-specific inverse agonist.

13 grelor has the pharmacological profile of an inverse agonist.

14 o that of the highly stable ghrelin receptor inverse agonist.

15 sing JD5037, a peripherally restricted CB1 R inverse agonist.

16 ds, spanning the range of full, partial, and inverse agonists.

17 tionality switch from agonist to antagonists/inverse agonists.

18 ating the effect of cannabinoid CB1-receptor inverse agonists.

19 iors as full agonists, partial agonists, and inverse agonists.

20 forskolin-induced cAMP production acting as inverse agonists.

21 ith agonists and positive cooperativity with inverse agonists.

22 ologically confirmed as a new class of CB(2) inverse agonists.

23 ith efficacy but negative cooperativity with inverse agonists.

24 mediating the beneficial effects of beta-AR inverse agonists.

25 ible mechanism for the functional effects of inverse agonists.

26 s TRPM3 responses can be potentiated by GPCR inverse agonists.

27 Five of these molecules were inverse agonists.

28 a "sensitized" state was tested using CB(1) inverse agonists.

29 rol cellular acidification, in the manner of inverse agonists.

30 vel mechanism providing pain relief by CB(1) inverse agonists.

31 ock-out (KO) mice as well as selective CB(1) inverse agonists.

32 ferent classes of ligands including full and inverse agonists.

33 n dose selection for clinical trials of CB1R inverse agonists.

34 iological effects of muscarinic agonists and inverse agonists.

35 e binding modes of agonists, antagonists and inverse agonists.

36 agonized by CB1 and CB2 receptor antagonists/inverse agonists.

37 nities only CXCL12 and synthetic antagonists/inverse agonists.

38 ding to a functional switch from agonists to inverse agonists.

39 rally distinct from the first-generation CB1 inverse agonists.

40 are the first to demonstrate that RORgammat inverse agonists: 1) inhibit Tc17 cell differentiation,

41 Light transforms the inverse agonist 11-cis-retinal into the agonist all-tran

42 eceptor as it utilizes a covalently tethered inverse agonist (11-cis-retinal) as the native ligand.

43 would predict, we found that binding for the inverse agonist, 11-cis-retinal (11CR), slowed when the

44 K properties to afford the non-CNS penetrant inverse agonist 22 (AZ-GHS-22) and the CNS penetrant inv

45 the partial agonist arecoline (ARC), and the inverse agonist 3-quinuclidinyl-benzilate (QNB), in the

46 agonist 22 (AZ-GHS-22) and the CNS penetrant inverse agonist 38 (AZ-GHS-38).

47 ersed by coincubation with A(2A)AR-selective inverse agonist 4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo

48 We generated a new CB1 inverse agonist, (4-(bis(4-fluorophenyl)methyl)piperazin

49 H2), a neutral antagonist that inhibited the inverse agonist action of naltrexone.

50 e context-dependent antagonist, agonist, and inverse agonist activities.

51 o efficacy better than functional antagonist/inverse agonist activities.

52 novel dual-target compounds with antagonist/inverse agonist activity at cannabinoid receptor type 1

53 de, DIIADDEPLT (Pep19), with slightly better inverse agonist activity at cannabinoid type 1 receptors

54 mpetitive antagonism, consistent with either inverse agonist activity at MC-R or interaction with a d

55 tor antagonists MRS1706 and DPCPX with known inverse agonist activity at the A(2B) subtype inhibited

56 Seventeen compounds also possessed inverse agonist activity at the MC5R, the first report o

57 However, complete blockade or inverse agonist activity by some full mGlu5 NAM chemotyp

58 s and it was suggested that antagonists with inverse agonist activity could promote activation of mas

59 Inverse agonist activity of mant-dATP was found at the W

60 icity could be used to partially explain the inverse agonist activity of some members of the series,

61 n good overall yields and screened for their inverse agonist activity on the US28 receptor of human c

62 These results suggest SR141716A exerts inverse agonist activity through the stabilization of bo

63 id receptors; however, measurements of delta inverse agonist activity within this series illustrated

64 , which switched partial agonist activity to inverse agonist activity, and optimized physicochemical

65 (mant-deoxy-ATP [dATP], mant-deoxy-ADP) with inverse agonist activity.

66 the mechanism by which SR141716A exerts its inverse agonist activity.

67 d by enhanced agonist affinity and decreased inverse agonist affinity consistent with an active confo

68 ite profile: diminished agonist and enhanced inverse agonist affinity.

69 ing hormone (alpha-MSH) and to an antagonist/inverse agonist, agouti-related peptide (AgRP), which ar

70 H3 receptor antagonists/inverse agonists also may be useful for treating cogniti

71 activation (agonist, neutral antagonist and inverse agonist) also stabilize distinct conformations o

72 diet-induced obese mice treated with the CB1 inverse agonist AM251 [1-(2,4-dichlorophenyl)-5-(4-iodop

73 The CB1 antagonist/inverse agonist AM251 [N-1-(2,4-dichlorophenyl)-5-(4-iod

74 new inhibitors, and the apparent bias toward inverse agonists among the docking hits, have implicatio

75 ded receptor as well as receptor bound to an inverse agonist, an agonist, and a G-protein-mimetic nan

76 A small-molecule inverse agonist and a neutral antagonist inhibited TSH-s

77 evealed key positions for the switch between inverse agonist and agonist response.

78 Surprisingly, both weak inverse agonist and antagonists that display binding sel

79 inopropane (DOI), antagonist ketanserin, and inverse agonist and antipsychotic drug clozapine.

80 ized in a lipid environment when bound to an inverse agonist and in complex with a Fab that binds to

81 receptor activity, indicating that it is an inverse agonist and that the ECD can negatively regulate

82 d recently with significant interest both in inverse agonists and in protean agonists (i.e., compound

83 eversed by prazosin, a selective alpha(1)-AR inverse agonist, and mimicked by chronically treating wi

84 k cancer cells in vitro, thus acting here as inverse agonists, and subsequent angiogenesis in vivo.

85 ed a binding mode similar to that of the CAR inverse agonist androstenol.

86 abinoid (CB1) receptor and exhibits a potent inverse agonist/antagonist activity.

87 .032-0.1 mg/kg/h, intravenous) or the 5-HT2A inverse agonist/antagonist pimavanserin (0.32-10 mg/kg p

88 monkeys with the cannabinoid CB(1) receptor inverse agonist/antagonist rimonabant [N-piperidino-5-(4

89 ell-investigated histamine H3 receptor (H3R) inverse agonist/antagonist, showing an exclusively high

90 inical utility of 5-HT2C agonists and 5-HT2A inverse agonists/antagonists alone or in combination as

91 Recently, several synthetic CB1 receptor inverse agonists/antagonists, such as SR141716A, AM251,

92 ults indicate that the effects of beta(2)-AR inverse agonists are caused by inhibition of beta(2)-AR

93 in which voltage, temperature, agonists and inverse agonists are independently coupled, either posit

94 H1-receptor inverse agonists are used effectively for treating sever

95 Interestingly, all previously reported CAR inverse-agonists are also activators of PXR, rendering t

96 ected toward the discovery of selective RORc inverse agonists as potential treatments of inflammatory

97 novel histamine 3 receptor (H3R) antagonists/inverse agonists as treatment for such disorders.

98 zed [(3)H]RO6957022, a highly selective CB2R inverse agonist, as a radiolabeled tool compound.

99 VUF11211 acts as an inverse agonist at a constitutively active mutant of CXC

100 s an agonist for Galpha(o) activation and an inverse agonist at Galpha(i1) and Galpha(i2).

101 -carboline-3-carboxamide (FG-7142; a partial inverse agonist at the benzodiazepine allosteric site on

102 a receptor-saturating dose of rimonabant, an inverse agonist at the CB(1) receptor.

103 n agonist" (functioning as an agonist and an inverse agonist at the same receptor) at the 5-HT3AB rec

104 allosteric site for rho-conopeptide TIA, an inverse agonist at this receptor.

105 riments, assessed that they behave as potent inverse agonists at the hA2A AR.

106 ng such mutants with the muscarinic receptor inverse agonist atropine increased cellular levels and r

107 etagamma interface, whereas it appears as an inverse agonist based on its SPR response thus indicatin

108 Consistent with inverse agonist behavior, increased cell surface localiz

109 kin-8), both classes of nanobodies displayed inverse agonist behavior.

110 ucture of beta2AR-T4L provides insights into inverse-agonist binding and the structural changes requi

111 -OHT structure was similar to other reported inverse agonist bound structures, showing reorientation

112 trinsic instability, as compared to inactive inverse agonist-bound states.

113 These studies show that unliganded and inverse-agonist-bound beta2AR exists predominantly in tw

114 beta2-adrenergic receptor (beta2AR): 1), the inverse-agonist-bound inactive state; 2), the agonist-bo

115 conformational heterogeneity in agonist- and inverse-agonist-bound preparations.

116 lated persistent IP1 production, whereas the inverse agonist but not the neutral antagonist inhibited

117 le for docking of a range of antagonists and inverse agonists but also indicate that additional ligan

118 been determined in complex with two partial inverse agonists, but the global impact of additional li

119 ducing signaling by empty receptors, beta-AR inverse agonists can also activate signaling by novel pa

120 For many of these GPCRs, drugs classified as inverse agonists can suppress basal activity.

121 lysozyme fusion protein bound to the partial inverse agonist carazolol at 2.4 angstrom resolution.

122 tive and inactive state conformations, while inverse agonist carazolol selects only inactive state co

123 man beta(2) adrenergic receptor bound to the inverse agonist carazolol using the technique of amide h

124 isplayed differential binding preference for inverse agonists comparable with the P269A, H270A, and I

125 absence of agonist, the aggregators acted as inverse agonists, consistent with a direct receptor inte

126 Mutational screening in the presence of the inverse agonist, CP-376395, resulted in the identificati

127 ired continuously activated receptors, as an inverse agonist decreased persistent signaling by 60%.

128 for very short times or the addition of the inverse agonist did not significantly affect the organiz

129 ization, selective agonists, antagonists and inverse agonists, dimerization with other neurotransmitt

130 d-bound RORgammat reveal that binding of the inverse agonists disrupts critical interactions that sta

131 radoxical hypothesis that the alpha-receptor inverse agonist doxazosin might produce beneficial effec

132 The CB(1) inverse agonists elicited concentration-related inhibiti

133 Rather unexpectedly, the inverse agonist EXP3174-bound AT(1)R generated different

134 rough beta-arrestin, while functioning as an inverse agonist for adenylyl cyclase activation.

135 also decreases basal signaling, acting as an inverse agonist for the G protein-mediated signaling pat

136 2c) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.

137 we previously identified several classes of inverse agonists for RORgammat.

138 lve 5-HT(4) receptors because the antagonist/inverse agonist, GR 125487, caused comparable decreases

139 activation is elevated and sensitive to the inverse agonist, GR113808 in the PFC of CK2alpha KO mice

140 CB2R agonists and inverse agonists have emerged as neuroprotective agents,

141 The 11-cis retinoid chromophore, the inverse agonist holding rhodopsin inactive, is well-reso

142 (18)F]MK-9470 is a selective, high-affinity, inverse agonist (human IC(50), 0.7 nM) for the cannabino

143 H3 receptor inverse agonists (IAs) may be efficacious in the treatme

144 st alprenolol increasing (22 +/- 1%) and the inverse agonist ICI 118,551 decreasing (19 +/- 2%) basal

145 ve suppression of beta2-AR basal activity by inverse agonist ICI 118,551 requires ionic interactions

146 than the prototypical delta opioid receptor inverse agonist ICI 174,864 (22).

147 The inverse agonist ICI prevents formation of the beta(2)AR-

148 ve-like conformation, whereas binding of the inverse agonist ICI-118,551 favors the inactive conforma

149 amine; a very weak agonist, catechol; and an inverse agonist, ICI-115881.

150 ered beta(2)AR construct in complex with two inverse agonists: ICI 118,551 (2.8 A), a recently descri

151 including the catecholamine agonists and the inverse agonist ICI118551, led to a decrease in FRET bet

152 erestingly, AGN211334 behaved as an apparent inverse agonist in CDS assays involving TM cells but as

153 The beta-blocker bucindolol was an inverse agonist in failing Arg, but not Gly, ventricles,

154 The antagonist BD1063 behaved as an inverse agonist in sigma-1R cells, whereas C-fragment wa

155 onsistent with the function of retinal as an inverse agonist in the dark state.

156 t that is in contrast to 1, which acts as an inverse agonist in this same assay.(1) These results sug

157 low intrinsic level of the MOP receptor were inverse agonists in reducing the greater level of consti

158 ential of SR1001, a synthetic RORalpha/gamma inverse agonist, in mouse models of atopic dermatitis an

159 f pimavanserin, a selective serotonin 5-HT2A inverse agonist, in this population.

160 In contrast, the inverse agonist increases the frequency of deactivation

161 d with nonpeptide ligand signaling activity; inverse agonists inhibited and agonists enhanced CRF bin

162 inhibition by bicuculline, which acts as an inverse agonist inhibiting GABA-independent gating.

163 Agonists and inverse agonists interact differentially with these path

164 ar, the beta-ionone ring of the retinylidene inverse agonist is crucial for the activation mechanism.

165 This efficient inverse agonist is rapidly converted to an agonist, the

166 f novel acyclic amide cannabinoid-1 receptor inverse agonists is described.

167 tivation and inhibition of basal activity by inverse agonists is poorly understood and difficult to s

168 tantly, CB1b shows stronger affinity for the inverse agonist JD-5037 than for rimonabant compared to

169 id receptor 2 antagonist AM630 (10 mg/kg) or inverse agonist JTE907 (3 mg/kg) during immunization hei

170 inding studies showed a high affinity of the inverse agonist K-(d-1-Nal)-FwLL-NH(2) at the ghrelin re

171 ession of MOR constitutive activity with the inverse agonist KC-2-009 enhanced GABAergic neurotransmi

172 onist 5-HT, the partial agonist LSD, and the inverse agonist Ketanserin.

173 ication of the alpha5 subunit GABAA receptor inverse agonist L-655,708 did not modulate the current.

174 4-(heptyloxy)phenol (AC-45594), a prototype inverse agonist lead, was used to show that SF-1 constit

175 In contrast, binding of inverse agonists leads to significant increases in FRET

176 -coupled receptor (GPCR) that stabilizes its inverse agonist ligand, 11-cis-retinal (11CR), by a cova

177 drenergic receptors (ARs) in complex with an inverse agonist ligand, carazolol, provide three-dimensi

178 des of discovery, the clinical importance of inverse agonist ligands is still speculative because thi

179 ng of the agonist angiotensin II (AngII) and inverse agonist losartan in wild-type AT1R changed the a

180 Our results suggest that LXR inverse agonists may be an effective cancer treatment ap

181 evated basal activity in vitro, and as such, inverse agonists may be therapeutically beneficial compa

182 Therefore, beta-AR inverse agonists may produce their beneficial chronic ef

183 Treatment with CB(1) inverse agonists may promote desensitization of the chan

184 rs, specifically beta-adrenoceptor (beta-AR) inverse agonists, may be useful in the chronic treatment

185 In contrast, the inverse agonist metoprolol suppresses interactions with

186 Thus, inverse agonists might prove to be effective therapies f

187 Overall, these novel inverse agonists might represent potential drug candidat

188 as blocked by pretreatment with a potent CB1 inverse agonist, MK-0364.

189 This is similar to the inverse-agonist model of ethylene receptor signaling pro

190 lity in the discovery of new antagonists and inverse agonists modulating signaling of this important

191 f any complete aGPCR ECR, in complex with an inverse-agonist monobody, revealing a GPCR-Autoproteolys

192 roxypropyl)cyclohe xan-1-ol (CP55940) or the inverse agonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-

193 ponse to the benzodiazepine receptor partial inverse agonist N-methyl-beta-carboline-3-carboxamide (F

194 ys, ORG27569 can displace the CB1 antagonist/inverse agonist, N-(piperidiny-1-yl)-5-(4-chlorophenyl)-

195 en given the preferential mu-opioid receptor inverse agonist naloxone, suggesting the participation o

196 duced hyperalgesia was reinstated by the MOR inverse agonist naltrexone (NTX), but not by its neutral

197 ARBs, including olmesartan derivatives with inverse agonist, neutral antagonist, or agonist activiti

198 Treatment with an RARgamma-selective inverse agonist (NRX205099) or overexpression of dominan

199 (IOM; 3.7 mug/kg), an antagonist and partial inverse agonist of benzodiazepine receptor.

200 of CB1 have largely targeted rimonabant, an inverse agonist of CB1.

201 ntrasubthalamic microinjections of either an inverse agonist of D5Rs, flupenthixol, or a D2R antagoni

202 S 38093, a novel brain-penetrant antagonist/inverse agonist of H3 receptors, on AHN (proliferation,

203 on of a mouse Sertoli cell line, TM4, and an inverse agonist of PPARD (DG172) rescued this effect.

204 iously, it was shown that the small molecule inverse agonist of RORgamma SR1555 [1-(4-((4'-(1,1,1,3,3

205 n antagonist ligand, AIP-II, functions as an inverse agonist of the kinase activity.

206 Candesartan, an inverse agonist of the type 1 angiotensin II receptor (A

207 arkinson's disease and that administering an inverse agonist of these receptors may lessen motor symp

208 Drugs that act as inverse agonists of cannabinoid CB1 receptors in the bra

209 Some inverse agonists of cannabinoid receptor type 1 (CB1) ha

210 Inverse agonists of CB(1)R (SR141716 and AM251) and inhi

211 ysfunction and degeneration of rods, whereas inverse agonists of ERRbeta trigger rapid rod degenerati

212 Only a few inverse agonists of P2Y(12) have been described.

213 OH)D3 and 20,23(OH)2D3 act as antagonists or inverse agonists of RORalpha and RORgamma, that opens ne

214 nazolines] that were found to be antagonists/inverse agonists of the alpha2-adrenoceptor.

215 ical role in the control of food intake, and inverse agonists of the ghrelin receptor (GHS-R1a) are w

216 ifluorophenyl)ur ea (Nelotanserin), a potent inverse-agonist of 5-HT(2A) that was advanced into clini

217 ation of sleep architecture, and antagonists/inverse-agonists of 5-HT(2A) have been shown to enhance

218 ructure of the human AT1R in complex with an inverse agonist olmesartan (Benicar(TM)), a highly poten

219 ts as an antagonist, whereas BCML acts as an inverse agonist on T2R4.

220 herein describe a series of phenyl pyrazole inverse agonists optimized for selectivity, aqueous solu

221 ly, while the chemokine CX3CL1 behaves as an inverse agonist or inhibitor of constitutive US28 signal

222 al APDs are also effective 5-HT(2C) receptor inverse agonists or neutral antagonists, 5-HT(6) or 5-HT

223 yl)-4-methyl-3-pyrazole carboxamide] (CB(1)R inverse agonist) paradigms, mutants display normal body

224 Binding of agonist or inverse-agonist peptides results in twisting of the link

225 vivo where Gi/o GPCRs agonists inhibited and inverse agonists potentiated TRPM3 mediated nociceptive

226 intaining a potent and highly selective RORc inverse agonist profile.

227 ration of alprenolol, a beta-blocker without inverse agonist properties, did not attenuate the asthma

228 aken together, indicate that this allosteric inverse agonist radioligand for CXCR3 may facilitate the

229 studied using PET with [(11)C]MePPEP, a CB1 inverse agonist radioligand.

230 understanding of structural determinants of inverse agonist-receptor interaction, this study screene

231 systemic administration of a 5-HT6 receptor inverse agonist reduces CREB phosphorylation in prefront

232 e during the posthyperalgesia state with MOR inverse agonists reinstated central pain sensitization a

233 es the molecular mechanism of action for the inverse agonists reported here.

234 However, the first generation of CB1 inverse agonists, represented by rimonabant (SR141716A),

235 we describe a novel series of selective CB2 inverse agonists resulting from introduction of a methox

236 have found that administration of beta(2)-AR inverse agonists results in attenuation of the asthma ph

237 following administration of the cannabinoid inverse agonist rimonabant (150 mug/kg, i.v).

238 ment in squirrel monkeys by the CB1-receptor inverse agonist rimonabant and by the recently developed

239 t this system using the cannabinoid receptor inverse agonist rimonabant were successful in producing

240 Similar to the CB1R antagonist/inverse agonist rimonabant, analogues 27 and 30 decrease

241 ion by all agonists tested as well as by the inverse agonist rimonabant.

242 as prevented by co-administration of the CB1 inverse agonist rimonabant.

243 nd had altered sensitivity to benzodiazepine inverse agonist RO 15-4513 (ethyl-8-azido-6-dihydro-5-me

244 be displaced by the 5-HT7 receptor selective inverse agonist SB-269970.

245 in but also by the CXCR2-specific allosteric inverse agonist SB265610.

246 1453), is described starting from an initial inverse agonist screening hit.

247 d 35e (an acyclic class human CB(1) receptor inverse agonist similar to MK-0364).

248 on, we administered in vivo a benzodiazepine inverse agonist specific for alpha5-subunit-containing e

249 Moreover, treatment with a RORalpha inverse agonist SR1001 effectively protected against pat

250 B1 cannabinoid receptors with the antagonist/inverse agonist SR141716A prevented the play-enhancing e

251 ished binding for several agonists but bound inverse agonists SR141716A, N-(piperidin-1-yl)-5-(4-iodo

252 ma, and extend these findings to develop the inverse agonist SR2595.

253 enic metabolism pathways, we designed an LXR inverse agonist SR9243 that induces LXR-corepressor inte

254 CRF-bound fully active state; 2) allosteric inverse agonists stabilize the inactive state, and allos

255 a mechanism for the inhibition of gating by inverse agonists such as bicuculline.

256 agonist (ZM241385) bound receptors, with the inverse agonist suppressing fast ps-ns timescale motions

257 ion with Rev-Erbalpha or addition of the ROR inverse agonist T0901317.

258 d by grafting the CXCL12 N-terminus onto the inverse agonist T140.

259 ituted flavonoids were typically more potent inverse agonists than their related hydro derivatives.

260 12c was found to be a highly selective CB1R inverse agonist that reduced body weight and food intake

261 able, highly efficacious, and selective CB1R inverse agonists that caused food intake suppression and

262 agonists that promote receptor signaling and inverse agonists that reduce basal receptor activity.

263 We describe here a series of 5-HT(2A) inverse-agonists that when dosed in rats, both consolida

264 In the presence of inverse agonists, the conformation of ECL2 in the N111G

265 nd the potential therapeutic applications of inverse agonists, the molecular mechanisms underlying G

266 C terminus of EC2 differentiates agonist and inverse agonist; the P269A, H270A, and I271A receptors e

267 s new opportunities for developing novel CB1 inverse agonists through the optimization of molecular p

268 s used to identify potent and selective SF-1 inverse agonists through the screening of a chemical lib

269 5-HT(2A) receptor inverse agonists thus represent a potential new class of

270 e of the M3 receptor bound by the antagonist/inverse agonist tiotropium were then employed.

271 M1 and M4 muscarinic receptors bound to the inverse agonist, tiotropium.

272 ibe a novel, potent, and selective RORgammat inverse agonist (TMP778), and its inactive diastereomer

273 oughout the activation cycle, switching from inverse agonist to agonist after absorbing a photon.

274 Only 11- cis-retinal acts as an inverse agonist to the opsin.

275 Furthermore, the ability of 5-HT(2A) inverse agonists to normalize behavioral changes induced

276 ll molecule ghrelin receptor antagonists and inverse agonists to the clinic.

277 (2) antagonist, and pimavanserin, a 5-HT(2A) inverse agonist, to prevent the development of the PCP-i

278 Notably, the V2R-selective inverse agonists tolvaptan and satavaptan completely sil

279 identified some ligands that were selective inverse agonists toward Gq but not of G13.

280 e to many conformations, while binding of an inverse agonist traps the receptor in the inactive state

281 to what was observed with chronic beta(2)-AR inverse agonist treatment, namely, reductions in mucous

282 , which in theory would be better suited for inverse agonist treatment, this work is still a long way

283 ptor rationalized the pharmacology observed; inverse agonists, unlike neutral antagonists, cannot be

284 Their in vitro functional activity as inverse agonists was confirmed in vivo in the formalin t

285 s as selective cannabinoid-1 receptor (CB1R) inverse agonists was discovered through high throughput

286 To determine the mechanism of the beta-AR inverse agonists, we compared the asthma phenotype in be

287 roinjections of rimonabant (a CB(1) receptor inverse agonist) were studied on antinociceptive respons

288 on 2 resulted in highly potent and efficient inverse agonists, whereas the substitution of d-tryptoph

289 074, a potent and highly-selective RORgammat inverse agonist, which dose-dependently inhibited RORgam

290 Hence, the discovery of CB1 inverse agonists with a chemical scaffold distinct from

291 ose a general binding mode for this class of inverse agonists with CB2.

292 omise for developing peripherally active CB1 inverse agonists with fewer side effects.

293 eight compounds as potent and selective CB2 inverse agonists with high binding affinity (CB2K(i) < 1

294 s were developed and also confirmed as CB(2) inverse agonists with the highest CB(2) binding affinity

295 erence to bind to the active state receptor; inverse agonists (xanthine amine congener, ZM241385, SCH

296 In contrast, the inverse agonist ZM241385 does not interact with any of t

297 ation conferred on the receptor by the bound inverse agonist ZM241385.

298 hion to the chemically related region of the inverse agonist ZM241385.

299 acts with cholesterol only when bound to the inverse agonist ZM241385.

300 stantially differ between agonist (NECA) and inverse agonist (ZM241385) bound receptors, with the inv