ライフサイエンスコーパス: selective ligand

1 1/5 responses, even to GDF5, a reported ALK6 selective ligand.

2 with tumor cells with Wy-14,643, a PPARalpha-selective ligand.

3 ydroxyphenyl)propanonitrile), a known ERbeta-selective ligand.

4 est and was interchangeable with an RARalpha-selective ligand.

5 rate a high-affinity (125)iodinatable sst(4)-selective ligand.

6 phenotype was partially reversed by ER-beta-selective ligand.

7 e not been reported because of the lack of a selective ligand.

8 is greatly hampered by a paucity of subtype selective ligands.

9 ll characterized in response to alpha7 nAChR-selective ligands.

10 (8), with the goal of turning them into more selective ligands.

11 hemistry can rapidly yield highly potent and selective ligands.

12 herapeutic benefit relative to highly target-selective ligands.

13 approach to design of novel hMC3R and hMC5R selective ligands.

14 ug design and in silico searches for subtype-selective ligands.

15 ences have stimulated the search for subtype-selective ligands.

16 e of the lack of high avidity antibodies and selective ligands.

17 kedly increased binding affinity for subtype-selective ligands.

18 of C1 domains has impeded the development of selective ligands.

19 own because of the lack of available galanin-selective ligands.

20 version of genistein in order to identify ER selective ligands.

21 termine the occurrence of plant-based ERbeta-selective ligands.

22 e of the lack of high avidity antibodies and selective ligands.

23 a series of estrogen receptor-beta (ERbeta) selective ligands.

24 n receptors, and may guide the design of new selective ligands.

25 because of the limited number of known MC3R selective ligands.

26 btype is unknown, due in part to the lack of selective ligands.

27 ides a platform for developing receptor type-selective ligands.

28 ression levels and the lack of M(5) receptor-selective ligands.

29 ion because of the lack of pharmacologically selective ligands.

30 pproach we have identified a number of BRS-3 selective ligands.

31 r their ability to attach to alpha(5)beta(1)-selective ligands.

32 een synthesized in an effort to develop more selective ligands.

33 981 are not necessary to generate potent and selective ligands.

34 has been hampered by a lack of alpha3 beta4-selective ligands.

35 ands ranged from 60- to 75-fold for the most selective ligands.

36 d WKY by measuring the binding of M1- and M2-selective ligands.

37 displays high affinity for both ETA- and ETB-selective ligands.

38 ceptors (ARs) with the goal to discover A3AR-selective ligands.

39 ntified highly potent and in some cases very selective ligands.

40 e development of new CB2 receptor potent and selective ligands.

41 buted to a limited number of identified MC3R selective ligands.

42 synthesized, and evaluated as potential MOR-selective ligands.

43 Thus, both groups behaved as functionally selective ligands.

44 ossibilities for the design of mAChR subtype-selective ligands.

45 eoretically leading to high-affinity subtype selective ligands.

46 for the rational design of novel potent and selective ligands.

47 The alpha7-nAChR selective ligand 1 (SSR180711) blocked the binding of [(

48 The MOR/KOR dual-selective ligand 10 showed no agonism and acted as a pot

49 ylmethylmorphinan (17) was found to be a KOR-selective ligand (150-fold over MOR and >10000-fold over

50 Surprisingly, both the ER-alpha selective ligand 16alpha-iodo-17beta-estradiol and the E

51 alpha5-Selective ligand 27 when injected directly into the hipp

52 Quantitative autoradiography of the PBR-selective ligand [(3)H]-(R)-PK11195 and [(125)I]-(R)-PK1

53 acological binding studies using the sigma-1-selective ligand [3H](+)-pentazocine showed a high-affin

54 k-) cells were characterized with the alpha5-selective ligand [3H]L-655,708 and compared with the pha

55 g experiments with the kappa opioid receptor selective ligand [3H]U69,593 led to the discovery of a n

56 antitative autoradiography with the alpha(1) selective ligand, [3H]zolpidem, and the non-selective be

57 terization of a putative D(1)-D(2) heteromer-selective ligand, 6-chloro-2,3,4,5-tetrahydro-3-methyl-1

58 The most selective ligands, 9 (NSC252359) and 5 (NSC123111), bind

59 results demonstrate that naltrexone-derived selective ligands achieve their selectivity via a combin

60 Selective ligands act as translation inhibitors by locki

61 Functional selective ligands, activating a specific G protein signa

62 based thiazolidenediones, which function as selective ligands against this receptor.

63 d 7.39 were most important for binding CCK2R-selective ligand, although the effect of substitution of

64 l goal, to identify highly potent and sst(4)-selective ligands amenable to (125)iodination, could not

65 vation preferentially depending upon the TLR-selective ligand and TLR adapters.

66 al structures of human AT2R bound to an AT2R-selective ligand and to an AT1R/AT2R dual ligand, captur

67 tial for the discovery and design of pathway-selective ligands and may confer therapeutic advantages

68 Costimulation with TNFRI-selective ligands and soluble TNF further increased IL-6

69 terodimers through competition binding using selective ligands and the mitogen-activated protein kina

70 A great number of MT2-selective ligands and, more recently, several MT1-select

71 to discriminate between frequent hitters and selective ligands, and suggest a strategy for selective

72 itrile are among the highest ERbeta affinity-selective ligands, and they have an ERbeta potency selec

73 ydrobenzoxathiins as potent, ERalpha subtype selective ligands are described.

74 synthesis and characterization of chiral RXR selective ligands are described.

75 Selective ligands are lacking for many neuronal signalin

76 Selective ligands are needed for distinguishing the func

77 lso influence the activity of other targets, selective ligands are needed for the elucidation of TAAR

78 Many of the identified functionally selective ligands are potent selective KOR agonists that

79 the use of nonpsychotomimetic CB(2) receptor-selective ligands as a novel strategy for the control of

80 e likely to facilitate the design of new DIS selective ligands as potential antiretroviral agents.

81 se results illustrate the utility of subtype selective ligands as probes of nuclear receptor function

82 nonan-3-amine] is a high-affinity and highly selective ligand at alpha3beta4 nicotinic cholinergic re

83 new mechanistic information on functionally selective ligands at the pharmacologically important D2

84 luated the pharmacological effect of ER-beta-selective ligands (beta-LGNDs) in animal models of high-

85 ion for discrimination by naltrexone-derived selective ligands between the delta, mu, and kappa opioi

86 during therapy with the retinoid X receptor-selective ligand bexarotene led us to hypothesize that s

87 hy-mass spectrometry was utilized to confirm selective ligand binding and to demonstrate that prefere

88 tions in the active site of K69R ODC promote selective ligand binding during Schiff base formation.

89 or the detection of sequence- and structural-selective ligand binding to nucleic acids is described.

90 The molecular determinants that govern selective ligand binding to the rat D(4) dopamine recept

91 fluorescence competitive binding assay, the selective ligand binding was observed for AlinCSP4-6.

92 m structure of the nucleic acid required for selective ligand binding.

93 d offers a system for the study of structure-selective ligand binding.

94 gnaling of the receptor different upon using selective ligands, but the fate within the cells is also

95 )V211I) increased the affinities of alpha(5)-selective ligands by a approximately 20-fold and reduced

96 essful proof-of-concept for how functionally selective ligands can be discovered.

97 igands and raise the possibility that GluN2B-selective ligands can be divided into multiple classes.

98 ted that both G protein and arrestin pathway-selective ligands can promote beneficial effects in vivo

99 hown that retinoid X receptor-selective (RXR-selective) ligands can suppress serum TSH levels in vivo

100 platelets displayed enhanced GPVI and CLEC-2-selective ligands, collagen-related peptide (CRP), colla

101 rt here crystal structures of a G-quadruplex-selective ligand complexed with two human telomeric DNA

102 It has been proposed that selective ligands could bind to all three receptor types

103 These data suggest that use of ER-selective ligands could provide therapeutic benefit to r

104 icroM) inhibited Ca2+ currents, whereas the -selective ligands [D-Pen2,Pen5]-enkephalin (DPDPE) and d

105 At present, the only selective ligands described for FFA2 suffer from poor po

106 The latter derivatives are the most selective ligands described in the new series.

107 This may enable greater selective ligand design and development for mAChRs and f

108 iffusivity, extra-cellular interactions, and selective ligand destruction collectively shape the Noda

109 Analysis of binding of the site-selective ligands dimethyl-d-tubocurarine (DMT) and alph

110 e ligand, diminishing the coadministered RXR-selective ligand diminished both induced differentiation

111 For either tazarotene or an RARalpha-selective ligand, diminishing the coadministered RXR-sel

112 This analysis identified selective ligand docking regions within the conserved zi

113 This pathway-selective ligand does not promote the classic actions of

114 on of per se inactive RXR-selective with RAR-selective ligands efficiently regulates growth inhibitio

115 ent with those reported earlier for the lead-selective ligand ETH 5493, and all response functions we

116 eening can guide fragment-based discovery of selective ligands even if the structures of both the tar

117 p-1-en -3-yl) nortropane (IACFT) is a highly selective ligand for dopamine transporter (DAT) sites in

118 that E-selectin ligand-1 (ESL-1) is a highly selective ligand for E-selectin on hematopoietic progeni

119 gue (38) of mazindol was the most potent and selective ligand for HEK-hDAT cells (DAT K(i) = 1.1 nM;

120 TFLLR-amide, a selective ligand for PAR-1 sites, mimicked the effects o

121 NT131 (formerly T131 and AMG131) as a potent selective ligand for PPAR gamma that is structurally and

122 e 3 (GSK3787) was identified as a potent and selective ligand for PPARdelta with good pharmacokinetic

123 1-Dodecanethiol (1-DDT, 5 mM) was used as selective ligand for quantitative extraction under ultra

124 eport the development of a high-affinity and selective ligand for Sn that is an analogue of the natur

125 d 5d expectedly produced the most potent and selective ligand for the DAT (DAT (IC(50)) = 3.7 nM, DAT

126 the DAT (K(i) = 0.125 muM) and was the most selective ligand for the DAT over mu-opioid receptors (m

127 Aptiganel hydrochloride is a novel and selective ligand for the ion-channel site of the N-methy

128 rther support of this finding, we describe a selective ligand for the lipid-binding protein nucleobin

129 47) was identified to be a high affinity and selective ligand for the MCH1 receptor.

130 s been recently purified and identified as a selective ligand for the parathyroid hormone 2 receptor.

131 he SERT (K(i) = 0.0072 muM) and was the most selective ligand for the SERT over the DAT (DAT/SERT = 1

132 rived neurotrophic factor (BDNF), which is a selective ligand for TrkB, caused suppression of the who

133 inflammatory protein-1alpha and eotaxin (the selective ligands for CCR1 and CCR3, respectively); and

134 efforts have been made to develop potent and selective ligands for certain human melanocortin recepto

135 In addition to providing some of the first selective ligands for Cr(VI), these studies highlight th

136 has been an important target for developing selective ligands for different PKC isoforms.

137 The identification of selective ligands for each phorbol ester receptor class

138 ot precluded using this structure to develop selective ligands for either CCK(1) or CCK(2) receptors.

139 Just recently, the first selective ligands for FKBP51 were reported based on an i

140 ted acridine derivatives that are potent and selective ligands for G-quadruplex DNA.

141 or the medicinal chemist to discover pathway-selective ligands for GPCRs.

142 Biarylpyrimidines are characterized as selective ligands for higher-order nucleic acid structur

143 ng this hypothesis has been a lack of highly selective ligands for individual mAChR subtypes.

144 Fibroblast adhesion response to selective ligands for integrins alpha5beta1 and alphavbe

145 studies raise the exciting possibility that selective ligands for mGluR5 may provide a novel approac

146 The recent identification of selective ligands for p75(NTR), novel isoforms of this r

147 ound 17 can provide potent alpha4beta2-nAChR-selective ligands for possible use in treatment of neuro

148 ,14-prostaglandin J2 can function as subtype-selective ligands for PPARalpha and PPARgamma, respectiv

149 In the process of developing selective ligands for PrP, we found using a single-stran

150 t composition complicates the development of selective ligands for specific subtypes, since the five

151 This is the first report of highly potent, selective ligands for the 5-HT1A/B/D receptors with low

152 However, truly selective ligands for the alpha3beta4 nAChR have not bee

153 Here, we describe highly potent and selective ligands for the bromodomain module of the huma

154 of 1a-1d resulted in a series of potent and selective ligands for the DAT (analogues 5-28).

155 re hexahydropyrazinoquinolines as potent and selective ligands for the dopamine 3 subtype receptor us

156 Pathway-selective ligands for the estrogen receptor (ER) inhibit

157 opyrano[3,4-f]quinolines as a novel class of selective ligands for the glucocorticoid receptor is des

158 A novel series of selective ligands for the human glucocorticoid receptor

159 These compounds are potent and selective ligands for the human prostaglandin F receptor

160 cological profile indicates that 2 and 3 are selective ligands for the mGluR5a metabotropic glutamic

161 ively relocate to the nucleus in response to selective ligands for the PPAR isotype which they activa

162 PPARgamma) activators, whereas rexinoids are selective ligands for the retinoid X receptors (RXRs).

163 h the aim of conferring enhanced affinity of selective ligands for their nonpreferred receptor types.

164 ptors expressed in the brain and the lack of selective ligands for this receptor.

165 predictive power in enriching known receptor-selective ligands from related decoys, indicating a high

166 and provide a means for distinguishing GPR55 selective ligands from those interacting with cannabinoi

167 ated that 17beta-estradiol (E2) and the GPER-selective ligand G-1 triggered a GPER/EGFR/ERK/c-fos sig

168 tis elegans via the EXP-1 receptor, a cation-selective ligand-gated ion channel.

169 udies indicate that GABA may activate cation-selective ligand-gated ion channels in some cell types,

170 bitory neurotransmission by activating anion-selective ligand-gated ion channels.

171 c acetylcholine receptors (nAChR) are cation-selective, ligand-gated ion channels of the cysteine (Cy

172 d hormone receptor-beta--selective (TR-beta--selective) ligand, GC-1, to determine by a pharmacologic

173 6alpha-iodo-17beta-estradiol and the ER-beta selective ligand genistein failed to elicit ERK phosphor

174 A structurally novel opioid kappa receptor selective ligand has been identified.

175 iscovering dopamine D2-like receptor subtype-selective ligands has been a focus of significant invest

176 t both receptor families, the development of selective ligands has been proven difficult, exposing pa

177 fter 2 decades of intense research, numerous selective ligands have been developed to target this rec

178 genous ligands are unknown, and many have no selective ligands, hindering the determination of their

179 We demonstrate that PPARalpha-selective ligands (i.e., clofibrate, GW7647) significant

180 lpha-CTx) RgIA, one of the few alpha9alpha10 selective ligands identified to date, is 300-fold less p

181 However, it is difficult to develop a selective ligand if the point mutation is not associated

182 y for kappa receptors and was the most kappa selective ligand in this study, but this peptide exhibit

183 CREB phosphorylation utilizing alpha7 nAChR-selective ligands in PC12 cells endogenously expressing

184 ified the signaling profiles of several NOPR-selective ligands in upstream GPCR signaling (G protein

185 Retinoid X receptor-selective ligands, in contrast, did not regulate these r

186 Modelling of other important kappa-OR-selective ligands, including the morphinan-derived antag

187 An ER-beta-selective ligand increased markers of tricarboxylic acid

188 This selective ligand-induced surface stabilization was paral

189 BD elements outside the C-helix that control selective ligand interaction and channel gating steps by

190 The most potent and selective ligand is compound 23, which displayed a K(i)

191 cancer therapies, and the discovery of CA IX selective ligands is imperative for the development of t

192 d from telomeric DNA, by means of quadruplex-selective ligands, is a means of inhibiting the telomera

193 The latter (8) is one of the most DAT selective ligands known.

194 The putative somatostatin5 receptor-selective ligand L-362,855, unlike somatostatin-14 and s

195 s the high-affinity interactions with the D4-selective ligand L750,667 [3-[[4-(4-iodophenyl) piperazi

196 RXR-selective ligands led to tetramer dissociation, but also

197 re responsive to a retinoid X receptor (RXR)-selective ligand (LG100268), a retinoic acid receptor (R

198 These data demonstrate that the RXR-selective ligand LGD1069 is a highly efficacious therape

199 s-retinoic acid, and the retinoid X receptor-selective ligand LGD346 on the activity of the thyrotrop

200 ch work has been focused on designing highly selective ligands, little attention has been paid to the

201 opment and examined the effects of an ERbeta-selective ligand (LY3201) with a combination of global a

202 have given way to a myriad of novel receptor-selective ligands, many of which have observable anorect

203 A biased or functionally selective ligand may be able to distinguish between diff

204 Tazarotene used with RXR-selective ligand may thus be a useful antineoplastic age

205 e of biased signaling, and further, the NOPR selective ligands MCOPPB [1-[1-(1-methylcyclooctyl)-4-pi

206 ethyl]-1H-pyrrolo[2,3-b]pyridine] and the D2-selective ligands methylspiperone, aripiprazole, and its

207 ork overlap is maximized and the size of the selective ligands minimized.

208 e discovery of a novel kappa opioid receptor selective ligand, N- inverted question mark(2'S)-[3-(4-h

209 ty for the kappa receptor relative to the mu-selective ligand, (+)-N-[trans-4-phenyl-2-butenyl]-(3R,

210 e 14-desoxy analogues (7 and 9) of the delta-selective ligands, naltrindole (1, NTI) and spiroindanyl

211 In this study, development of a selective ligand of the fifth BRD of polybromo protein-1

212 tituted benzoxazoles (Table 5) were the most selective ligands of both azole series, with ERB-041 (11

213 de that CCL17 and CCL22 are conformationally selective ligands of CCR4 and interact with the receptor

214 Pathway selective ligands of the estrogen receptor inhibit trans

215 transfer biosensor to screen for functional selective ligands of the human oxytocin (OT) receptor.

216 Biased ligands (also known as functionally selective ligands) of G protein-coupled receptors are va

217 Combining the frameworks from two selective ligands often results in large, complex dual l

218 biochemical analysis of the effect of sigma2 selective ligands on cells grown in culture.

219 n part explain the different effects of CB2R-selective ligands on cocaine self-administration in mice

220 ical processes remain unknown due to lack of selective ligands or identification of its natural ligan

221 Our previous studies have shown that RXR-selective ligands (or "rexinoids"), including LGD1069, c

222 ts of rat pancreatic polypeptide (rPP), a Y4-selective ligand, or NPY, a nonselective ligand, adminis

223 monocytes were stimulated with TLR4, TLR7/8-selective ligands, or respiratory syncytial virus (RSV)

224 The method uses a combination of selective ligand (P,P'-di(2-ethylhexyl) methanediphospho

225 ms remain untested because of the lack of D3-selective ligands, paucity of appropriate model secretor

226 affinity of the receptors for D(1) and D(2)-selective ligands, perhaps reflecting altered packing of

227 ere we report that the less G-quadruplex DNA selective ligand PIPER can unwind double-stranded, close

228 specific binding for several radioactive D3-selective ligands, possibly reflecting their critical ro

229 of ERalpha activation, using the ER subtype-selective ligand propylpyrazoletriyl (PPT), on skeletal

230 The development of biased (functionally selective) ligands provides a formidable challenge in me

231 Comprehensive studies that consolidate selective ligands, quantitative comparisons of G protein

232 The binding of the D(1)-selective ligand R-(+)-7-chloro-8-hydroxy-3-methyl-1-phe

233 Based on treatments with RAR isoform-selective ligands, RARalpha is the major isoform respons

234 ing responses, along with binding data for a selective ligand (RCP-168), further validated the biosen

235 We show that retinoic acid receptor (RAR)-selective ligands reduce EGFR level and the magnitude an

236 We demonstrate here that RXR-selective ligands (referred to as rexinoids) function as

237 Estrogen receptor beta (ER-beta) and its selective ligand reprogrammed preadipocytes and precurso

238 o-proximal NO switch could contribute to the selective ligand responses in gas-sensing hemoproteins.

239 Similarly, treatment with mu-selective ligands results in a significant increase in t

240 ls with extremely low doses of certain delta-selective ligands results in a significant increase in t

241 r alone or in combination, and using subtype selective ligands revealed that concurrent stimulation i

242 We identified several KOR-selective ligand scaffolds with a range of signaling bia

243 o identify an aptamer for testing as a tumor-selective ligand, SELEX (systematic evolution of ligands

244 With the appreciation that CB2-selective ligands show marked functional selectivity, th

245 Treatment with RAR- and RXR-selective ligands showed that RARalpha synergized with R

246 crylonitrile (DG172), a novel PPARbeta/delta-selective ligand showing high binding affinity (IC(50) =

247 most likely because the retinoid X receptor-selective ligand suppresses thyrotropin secretion.

248 combination with a retinoid X receptor (RXR)-selective ligand, tazarotene caused ERK activation, RB t

249 veness of these cells to either the beta 2AR-selective ligand terbutaline or the sympathetic neurotra

250 Alpha-conotoxin MII, a selective ligand that discriminates among a variety of n

251 re, TSA led to promoter activation by an RXR-selective ligand that was otherwise inactive in transcri

252 Diarylpropionitrile (DPN), an ERbeta selective ligand that we developed, is a chiral molecule

253 hat fragment hits can be advanced to furnish selective ligands that affect the activity of proteins h

254 ype-specific interactions and the ER subtype-selective ligands that can be derived from them should p

255 its functions has been slowed by a dearth of selective ligands that can distinguish it from the close

256 ovide tools for development of alpha6*-nAChR-selective ligands that could be important in the treatme

257 g a biological role for GPR55 requires GPR55 selective ligands that have been unavailable.

258 used for the rational design of functionally selective ligands that may eventually be developed into

259 Moreover, we developed receptor-selective ligands that provide tools to assess which rec

260 Selective ligands that specifically activate GPCR135 or

261 ed to these cells in combination with an RAR-selective ligand, the ability of these retinoids to indu

262 rily because of the lack of receptor subtype-selective ligands, the precise physiological roles of th

263 hand, IGFBP-3 enhanced the effect of an RXR-selective ligand to induce differentiation of HL-60 and

264 h the inability of the ER-alpha- and ER-beta-selective ligands to elicit ERK phosphorylation, and of

265 e designed and synthesized a novel series of selective ligands to explore the requirements necessary

266 used SST receptor knock-out mice and subtype-selective ligands to investigate the receptor subtype th

267 However, the potential of ER-beta-selective ligands to offset obesity is not clear.

268 kely play a role in the ability of E2 and ER selective ligands to protect the brain from ischemia.

269 isease-causing networks instead of designing selective ligands to target individual proteins, has eme

270 We studied binding of RXR- and RAR-selective ligands to the RXR-RAR heterodimer and subsequ

271 t determined the ability of EP(4)A, an EP(4)-selective ligand, to act as an antagonist.

272 XR alpha severely reduced the ability of RAR-selective ligands tRA and CD367 to induce epidermal mRNA

273 Selective ligand trapping by reversible disulfide format

274 d (LG100268), a retinoic acid receptor (RAR)-selective ligand (TTNPB), or 1,25(OH)2D3, while combinat

275 as a starting point for development of GluD2-selective ligands useful as tools in studies of the sign

276 nt study we have attempted to identify BRS-3 selective ligands using a strategy of rational peptide d

277 Using selective ligands (VEGF-E and placental growth factor) a

278 The most potent and selective ligand was identified as (R,R)-cis-diethyl THC

279 Thus, by using the ERbeta selective ligand, we have dissociated the antiinflammato

280 tor subtypes to discriminate between subtype-selective ligands, we constructed chimeric proteins in w

281 In a new approach to develop ER subtype-selective ligands, we have embellished the 1,1-diaryleth

282 To develop ERbeta-selective ligands, we synthesized a series of nonsteroid

283 To address the need for novel selective ligands, we synthesized two compounds potentia

284 Among these new compounds, some potent, NET-selective ligands were identified.

285 ned for hBRS-3, hGRPR, and hNMBR, and hBRS-3 selective ligands were tested for their ability to activ

286 39 were most important for binding the CCK1R-selective ligand, whereas residues 2.61 and 7.39 were mo

287 ER subtype-selective ligands, which bind to and activate these subt

288 osphorylation of Erk1/2 in response to CRFR1-selective ligands, which induce proliferation in primary

289 novel lead compound to develop MOR/KOR dual-selective ligands, which might possess unique therapeuti

290 Selective liganding with photoswitchable tethered agonis

291 nthesis of new bifunctional sigma-1 (sigma1)-selective ligands with antioxidant activity.

292 39, indirectly influence the interactions of selective ligands with conserved residues by altering th

293 hich could facilitate the rational design of selective ligands with distinct pharmacological profiles

294 demonstrated that all isomers are beta-nAChR selective ligands with Ki = 0.02-0.3 nM.

295 amine receptors results from interactions of selective ligands with nonconserved residues lining the

296 h-receptor and can be considered th-receptor selective ligands with PCP/th ratios of 13, 293, and 368

297 ficacy that can be used to design highly D3R-selective ligands with targeted efficacies.

298 rface, and may facilitate the development of selective ligands with therapeutic potential.

299 When it is difficult to develop selective ligands within a family of related G-protein-c

300 alpha-CtxArIB[V11L,V16D] is the most selective ligand yet reported for alpha7 nAChRs.