ライフサイエンスコーパス: D3 receptor

1 HT2B, 5-HT6, 5-HT7, and dopamine D2-long and D3 receptors).

2 ffinities at the sub-nanomolar level for the D3 receptor.

3 ated by the D1 receptor and inhibited by the D3 receptor.

4 indicate a direct action of dopamine at the D3 receptor.

5 tent and competitive antagonist at the human D3 receptor.

6 ly mediated by the prominence of dopamine D2/D3 receptors.

7 d in CHO cells expressing either human D2 or D3 receptors.

8 n our hybrid molecular template targeting D2/D3 receptors.

9 receptors and AtT-20 cells expressing human D3 receptors.

10 receptors and AtT-20 cells expressing human D3 receptors.

11 molecules developed earlier for dopamine D2/D3 receptors.

12 receptors and AtT-20 cells expressing human D3 receptors.

13 affinity at 5HT1A, 5HT1B, 5HT1C, D1, D2, or D3 receptors.

14 ounds with high affinity and selectivity for D3 receptors.

15 d for high-affinity and selective binding to D3 receptors.

16 arkedly different cellular distribution than D3 receptors.

17 r-species differences in the distribution of D3 receptors.

18 r (PAM) of the rat and human dopamine D2 and D3 receptors.

19 tiate [(3)H]-dopamine binding at both D2 and D3 receptors.

20 se disorder reverses deficits in striatal D2/D3 receptors.

21 ; D2 = 3.23 and D3 = 1.41 nM) at both D2 and D3 receptors.

22 values were determined for D(2L), D(2S), and D3 receptors.

23 and evaluated as ligands for the dopamine 3 (D3) receptor.

24 opamine synthesis ([(18)F]DOPA), dopamine D2/D3 receptors ([(11)C]raclopride), and serotonin transpor

25 scular consequences of the disruption of the D3 receptor, a member of the family of D2-like receptors

26 ir3) channels is strongly implicated because D3 receptors activate channels composed of GIRK2 subunit

27 We then tested whether D3 receptors activate GIRK currents in SN dopamine neuro

28 motor cortex that differs from predominantly D3 receptor activation and that the kind of plasticity-i

29 D3 receptor activation differentially affected dopamine

30 eceptor functions, we examined the effect of D3 receptor activation on GABAA receptor (GABAAR)-mediat

31 vesicle trafficking dye FM1-43, we show that D3 receptor activation significantly inhibits spontaneou

32 Together, our results suggest that D3 receptor activation suppresses the efficacy of inhibi

33 Within these neurons, D3 receptor activation was found to regulate low-voltage

34 different properties with respect to vitamin D3 receptor activation, anti-inflammatory activity, and

35 e products were compared in terms of vitamin D3 receptor activation, anti-inflammatory, and antiproli

36 n homo-oligomers and are consistent with the D3 receptor adopting a beta1-adrenoreceptor-like quatern

37 to have a major influence on (sub)nanomolar D3 receptor affinity and D2/D3 selectivity, which was op

38 class of compounds with the goal to improve D3 receptor affinity and selectivity.

39 are also oppositely regulated by the D1 and D3 receptors after repeated exposure to cocaine.

40 ent study, we developed the (18)F-labeled D2/D3 receptor agonist (R)-(-)-2-(18)F-fluoroethoxy-N-n-pro

41 enic, and behavioral effects of the dopamine D3 receptor agonist 7-OH-DPAT (7-hydroxy-N,N-di-n-propyl

42 Furthermore, a D3 receptor agonist increased choice of the disadvantage

43 We conclude that a dopamine D3 receptor agonist preferentially affects brain activit

44 e systemic administration of the dopamine D2/D3 receptor agonist quinpirole (0.05 mg/kg).

45 and the anti-parkinsonian effects of the D2/D3 receptor agonist ropinirole.

46 h the D3 receptor antagonist, U99194, or the D3 receptor agonist, 7-OH-DPAT, did not alter choice beh

47 -1, 4-oxazin-9-ol hydrochloride], a specific D3 receptor agonist, caused a significant reduction of G

48 Quinpirole, a D2/D3 receptor agonist, had no effect on evoked dopamine re

49 plasticity, and the D2/D3, but predominantly D3, receptor agonist ropinirol has a dosage-dependent no

50 Like low dopamine, the D3 receptor agonists pergolide and PD 128907 reduced MSR

51 species, the results are consistent with the D3 receptor also assuming a quaternary structure in whic

52 r the inhibition of Akt by dopamine and that D3 receptors also participate in this signaling potentia

53 genetic manipulations that affect prefrontal D3 receptors alter anxiety, social interaction, and reve

54 organization and potential stability of the D3 receptor and possibly other GPCR quaternary structure

55 ormed to quantify binding availability of D2/D3 receptors and dopamine transporters (DATs).

56 The disruption of the coupling between D2/D3 receptors and Galphai2 by AMPH is at least partially

57 of the third intracellular domain of D2 and D3 receptors and the carboxyl-terminal domain of protein

58 nverse relationship between dopamine (DA) D2/D3 receptors and vulnerability to cocaine abuse, althoug

59 ction with FLN-A was specific for the D2 and D3 receptors and was independently confirmed in pull-dow

60 3) and MC1288 (4), which bind to the vitamin D3 receptor, and R04 (5), an inhibitor bound to human rh

61 acebo or a single low dose (50 mg) of the D2/D3 receptor antagonist amisulpride, which is believed to

62 acebo or a single low dose (50 mg) of the D2/D3 receptor antagonist amisulpride, which is believed to

63 is hypothesis, we examined the effect of the D3 receptor antagonist nafadotride on sensitization.

64 In contrast, the dopamine D2/D3 receptor antagonist raclopride reduced the seeking of

65 kedly attenuated by infusion of the dopamine D3 receptor antagonist SB-277011-A into the amygdala (2

66 perties of cocaine, the potent and selective D3 receptor antagonist trans-N-[4-[2-(6-cyano-1,2,3,4-te

67 amined the influence of U-99194A, a dopamine D3 receptor antagonist, on ethanol's rewarding effect in

68 Treatment with the D3 receptor antagonist, U99194, or the D3 receptor agoni

69 Conversely, D3 receptor antagonists (GR 103691 and nafadotride) incr

70 Dopamine D3 receptor antagonists and partial agonists have been s

71 ort a class of potent and selective dopamine D3 receptor antagonists based upon tranylcypromine.

72 eased by systemic administration of dopamine D3 receptor antagonists.

73 Moreover, the D1 and D3 receptors are also coexpressed in the same neurons, p

74 nd FLAG-tagged D3 receptors, suggesting that D3 receptors are capable of forming homodimers.

75 dopamine transporters (DATs) and dopamine D2/D3 receptors are implicated in a variety of neurological

76 Agonists at dopamine D2 and D3 receptors are important therapeutic agents in the tre

77 Our data suggest that midbrain D2/D3 receptors are more susceptible to AMPH-induced altera

78 nts had reduced 11C-raclopride binding to D2/D3 receptors at rest in the bilateral striatum, consiste

79 ion and reduced 11C-raclopride binding to D2/D3 receptors at rest was seen.

80 gion of reduced 11C-raclopride binding to D2/D3 receptors at rest.

81 in 58 methamphetamine users) and dopamine D2/D3 receptor availability (binding potential relative to

82 paminergic genes associated with dopamine D2/D3 receptor availability (D2R), no study to date has inv

83 f significant case-control differences in D2/D3 receptor availability (despite the observed relations

84 suggests that exercise increases striatal D2/D3 receptor availability (measured as nondisplaceable bi

85 n that sleep deprivation reduced dopamine D2/D3 receptor availability (measured with PET and [(11)C]r

86 es of growth, nor did it influence DAT or D2/D3 receptor availability after 1 year of treatment.

87 cial group have significant elevations in D2/D3 receptor availability and are less vulnerable to coca

88 and limbic networks, they had equivalent D2/D3 receptor availability and equivalent increases in end

89 elease occuring in the setting of reduced D2/D3 receptor availability and raise the possibility that

90 The relationship between D2/D3 receptor availability and vulnerability to cocaine re

91 ssociated with baseline striatal dopamine D2/D3 receptor availability and with methylphenidate-induce

92 methylphenidate (measured as decreases in D2/D3 receptor availability compared with placebo) did not

93 With the placebo, D2/D3 receptor availability in left caudate was lower (P <

94 quantify individual differences in putative D3 receptor availability in rodents trained on a novel t

95 Neither DAT nor D2/D3 receptor availability in the caudate nucleus and puta

96 We corroborated a decrease in D2/D3 receptor availability in the ventral striatum with sl

97 However, after washout, the D2/D3 receptor availability of MPH-treated animals did not

98 DA D2/D3 receptor availability significantly increased in fema

99 DA D2/D3 receptor availability was assessed in female cynomolg

100 ing with striatal regions showing reduced D2/D3 receptor availability, except for a cluster in the le

101 system possibly due to decreased striatal D2/D3 receptor availability.

102 eport computational homology modeling of the D3 receptor based upon the high-resolution X-ray structu

103 levels (using microdialysis) and dopamine D2/D3 receptor binding (using positron emission tomography)

104 Several analogues demonstrated superior D3 receptor binding affinities and selectivities as comp

105 ophilicity (c log D = 6.94) while optimizing D3 receptor binding affinity and D2/D3 selectivity.

106 of 20 compounds selected for testing in the D3 receptor binding assay.

107 24 appears suitable for quantification of D2/D3 receptor binding in vivo, and the results encourage e

108 We tested the hypothesis that D3 receptor binding is above normal in methamphetamine (

109 describes the binding of ligands at a single D3 receptor binding site and offers insights into the bi

110 DA D2/D3 receptor binding was altered both in mice and in huma

111 1)C]raclopride competes with dopamine for D2/D3 receptor binding) or receptor downregulation.

112 was correlated with striatal but not OFC D2/D3 receptor binding.

113 nucleus and a corresponding reduction in D2/D3 receptor binding.

114 Thus, D3 receptor blockade attenuates both the rewarding effec

115 response to ethanol and further suggest that D3 receptor blockade increases ethanol reward.

116 w that we have identified PAMs of the D2 and D3 receptors both in vitro and in vivo.

117 s of the 8-week interventions on striatal D2/D3 receptor BPND.

118 acer, [(11)C]raclopride, for the dopamine D2/D3 receptor by carbonylation with excellent radiochemica

119 assay in which binding to and activation of D3 receptors by [(3)H]dopamine was prevented.

120 t with HEK-293 cells expressing either D2 or D3 receptors by using tritiated spiperone as radioligand

121 lts not only support the hypothesis that the D3 receptor can regulate secretory activity but also pro

122 introduced into the stable cell line either D3 receptors carrying an hemagglutinin (HA) epitope tag,

123 Of particular interest, dopamine D3 receptors contribute to the beneficial influence of d

124 The dopamine D1 receptor-D3 receptor (D1R-D3R) heteromer is being considered as a

125 dies on the dopamine system have used D2 and D3 receptor (D2/D3) antagonists such as (11)C-raclopride

126 ressed the role of striatal dopamine (DA) D2/D3 receptor (D2/D3R) function in chronic non-neuropathic

127 We investigated whether striatal dopamine D2/D3 receptor (D2R) binding assessed by (123)I-iodobenzami

128 d analogues of sumanirole (1), a dopamine D2/D3 receptor (D2R/D3R) agonist, were synthesized.

129 her alone or in combination with FLAG-tagged D3 receptors, D3nf exhibited a punctate perinuclear dist

130 A series of potent and selective D3 receptor (D3R) analogues with diazaspiro alkane cores

131 e has inspired investigation of the dopamine D3 receptor (D3R) as a target for therapeutic interventi

132 The dopamine D3 receptor (D3R) has an anatomic distribution that sugg

133 The dopamine D3 receptor (D3R) has been implicated in substance abuse

134 Subtype-selective agents for the dopamine D3 receptor (D3R) have been considered as potential medi

135 d partial agonist modulators of the dopamine D3 receptor (D3R) have emerged as promising therapeutics

136 The crystal structure of the human dopamine D3 receptor (D3R) in complex with the small molecule D2R

137 The dopamine D3 receptor (D3R) is a molecular target for both first-g

138 The dopamine D3 receptor (D3R) is a promising target for the developm

139 The dopamine D3 receptor (D3R) is a target for developing medications

140 The dopamine D3 receptor (D3R) is crucial in the regulation of blood

141 ffinity and selectivity at the dopamine (DA) D3 receptor (D3R) is described.

142 The dopaminergic D3 receptor (D3R) is emerging as an antagonist of sensit

143 Both dopamine D3 receptor (D3R) partial agonists and antagonists have

144 ive allosteric ligands of the human dopamine D3 receptor (D3R) using two optimized crystal-structure-

145 binding of a novel APD and DA to a dopamine D3 receptor (D3R) was investigated by looking at electro

146 eased dorsal striatal levels of the dopamine D3 receptor (D3R), a gene downstream of BDNF, via activa

147 t and long isoform variants (D2SR and D2LR), D3 receptor (D3R), and D4 receptor (D4R), with several p

148 hese effects were dependent on functional DA D3 receptor (D3R), because nicotine was inactive both in

149 The structural similarities between dopamine D3 receptor (D3R)-selective molecules that display bitop

150 rd intracellular loop of the limbic dopamine D3 receptor (D3R).

151 tamine required functionally intact dopamine D3 receptors (D3R), as its effects were abolished by sel

152 ing ligands that bind both D2Rs and dopamine D3 receptors (D3Rs), questioning the role of D3Rs in the

153 exercise training can ameliorate striatal D2/D3 receptor deficits in methamphetamine users, and warra

154 Here, we show that D3 receptors define a unique population of glutamatergic

155 Striatal dopamine (DA) D3 receptor density (measured by quantitative receptor a

156 In symptomatic cats, D3 receptor density was significantly decreased in all r

157 eeking by conditioned reinforcers depends on D3 receptor-dependent dopamine transmission in the amygd

158 y a negative allosteric modulator of D2- and D3-receptor dimers, thus identifying the first allosteri

159 d H- (nine repeats)] on striatal dopamine D2/D3 receptor (DRD2) availability and on dopamine release

160 mal studies support the role of the dopamine D3 receptor (DRD3) in alcohol reinforcement or liking.

161 ch a dysfunctional signaling of the dopamine D3 receptor (Drd3) is hypothesized.

162 cules with preferential agonist activity for D3 receptor (EC(50) (GTP gamma S); D3 = 0.52 nM; D2/D3 (

163 )-19b as two potent agonists for both D2 and D3 receptors (EC(50) (GTPgammaS); D2 = 4.51 and 1.69 nM

164 These results suggest that the D1 and D3 receptors elicit opposite regulation of target gene e

165 ressed in HEK 293 cells, FLAG- and HA-tagged D3 receptors exhibited a similar plasma membrane distrib

166 terized for their binding to dopamine D2 and D3 receptors expressed in HEK-293 cells.

167 D3-receptor-expressing neurons send axonal projections t

168 D3-receptor-expressing pyramidal neurons are electrophys

169 ncation fragment reduces the level of D2 and D3 receptor expression at the plasma membrane.

170 chniques, and electrophysiology to show that D3 receptor expression defines a novel subclass of layer

171 These alterations in D3 receptor expression may play an important role in the

172 evelopment of highly selective compounds for D3 receptor (for (-)-40K(i), D3 = 1.84 nM, D2/D3 = 583.2

173 appears to result in the mislocalization of D3 receptors from the plasma membrane to an intracellula

174 needed to establish whether normalization of D3 receptor function could reduce vulnerability to relap

175 D2 receptors in vivo precludes the study of D3 receptor function in the brain and necessitates the u

176 the potential cellular mechanism underlying D3 receptor functions, we examined the effect of D3 rece

177 addition, a Ser9Gly variant in the dopamine D3 receptor gene on 3q13 has been suggested to be a risk

178 tors and in vivo with mice bearing disrupted D3-receptor genes.

179 like lead compounds with selectivity for the D3 receptor has been challenging because of the high seq

180 Pharmacological activation of the dopamine D3 receptor has been shown to trigger neurogenesis in th

181 A physiological role for the D3 receptor has not been identified, but an activation o

182 oncentrations of dopamine transporter and D2/D3 receptors have been observed in the amygdaloid comple

183 Both the dopamine D1 and D3 receptors have been shown to mediate gene expression

184 To study the involvement of the D3 receptor in brain mechanisms and behaviors commonly a

185 mputational approach implicates the dopamine D3 receptor in decision-making processes that are altere

186 m and genetic studies implicate the dopamine D3 receptor in drug addiction.

187 However, the role of D3 receptors in adaptive, goal-directed behavior has not

188 ng results indicated highest selectivity for D3 receptors in compound (-)- 10 ( K i = 0.35 nM; D2/D3

189 , thus identifying a unique role of midbrain D3 receptors in decision-making processes.

190 ant tool with which to elucidate the role of D3 receptors in drug reinforcement in vivo.

191 These data suggest an important role for D3 receptors in mediating the addictive properties of co

192 ngs are consistent with the reported role of D3 receptors in mediating the facilitatory effects of cu

193 ing novel circuitry and cellular actions for D3 receptors in PFC.SIGNIFICANCE STATEMENT The D3 dopami

194 ne unique circuitry and cellular actions for D3 receptors in regulating PFC networks.

195 monstrate a previously unrecognized role for D3 receptors in select aspects of reinforcement learning

196 nist radioligand for imaging dopamine D2 and D3 receptors in the human brain with PET.

197 shed the interaction between Galphai2 and D2/D3 receptors in the midbrain while leaving striatal D2/D

198 ts are discussed with respect to the role of D3 receptors in the transport response and the nature of

199 s are consistent with a downregulation of D2/D3 receptors in ventral striatum with sleep deprivation

200 s reduced binding of [(11)C]raclopride to D2/D3 receptors) in detoxified cocaine abusers.

201 uggest that individual variation in midbrain D3 receptors influences flexible behavior.

202 We therefore hypothesized that tolerance of D3 receptor inhibition of locomotion contributes to the

203 the transport response and the nature of D2-D3 receptor interactions.

204 racellular helix VIII in the formation of D3-D3 receptor interfaces within homo-oligomers and are con

205 The dopamine D3 receptor is a class A, rhodopsin-like G protein-coupl

206 cycle in developing and adult brain, and the D3 receptor is known to play an important role in dopami

207 dopamine D3 receptor is preferentially localized to the mesocorti

208 anylcypromine has a low affinity for the rat D3 receptor (K(i) = 12.8 muM), our efforts have yielded

209 nds on spinal reflexes in wild-type (WT) and D3-receptor knock-out mice (D3KO).

210 emented by additional use of 123I-labeled D2/D3 receptor ligand co-injected to assess both pre- and p

211 creases (measured with [11C]raclopride, a D2/D3 receptor ligand with binding that is sensitive to end

212 have advantages over other dopamine (DA) D2/D3 receptor ligands because, as an agonist, it measures

213 task was uniquely sensitive to modulation by D3 receptor ligands, yet these drugs did not alter decis

214 ocaine and suggest that blockade of dopamine D3 receptors may constitute a new and useful target for

215 ed sensitivity of choice on the cued task to D3-receptor-mediated neurotransmission data suggest that

216 a, that dopaminergic activity at the related D3 receptor might, in contrast, be elevated and thereby

217 ans, because physiological effects of D2 and D3 receptors might differ.

218 eptor was modeled computationally using four D3 receptor models which were obtained from homology mod

219 ved FRET, the interfaces that allow dopamine D3 receptor monomers to interact were defined and used t

220 In contrast, D3 receptor mRNA expression was slightly elevated in sym

221 ons of newborn mice, effects not observed in D3 receptor null mutant mice mice.

222 gns was related to normalization of striatal D3 receptor number.

223 nding potential (BP) to striatal dopamine D2/D3 receptors on average by 29.2%, which was associated w

224 atin transcription responsive to the vitamin D3 receptor or to Gal4-VP16.

225 ic selectivity, (b) increase the affinity at D3 receptors, or (c) decrease the affinity at D2 recepto

226 nt influence on the regulation of DATs or D2/D3 receptors, or on standard measures of growth.

227 hat are >100-fold selective for the dopamine D3 receptor over dopamine D2 receptor (D2R), despite hig

228 e analogues showed exquisite selectivity for D3 receptors over >60 other receptors, further underscor

229 In the present report, the D3 receptor pharmacophore is modified in the 2,3-diCl- a

230 prove useful in the elucidation of the role D3 receptors play in the psychomotor stimulant and reinf

231 Dopamine D3 receptor positron emission tomography ligands have re

232 s of magnitude was determined for this novel D3-receptor-preferring ligand, compared to 1.

233 e receptors and used this cell line to study D3 receptor-protein interactions.

234 utoradiography with the putatively selective D3 receptor radioligand [3H]PD 128907.

235 hy and raclopride labeled with carbon 11 (D2/D3 receptor radioligand sensitive to competition with en

236 tomography and [11C]raclopride (dopamine D2/D3 receptor radioligand) and [11C]cocaine (dopamine tran

237 guanfacine with [(11)C]FLB457, a dopamine D2/D3 receptor radiotracer, and positron emission tomograph

238 These results demonstrate that D3 receptors regulate dopamine transporter function and

239 Whether D3 receptors regulate dopamine transporter function is u

240 tion and identify a novel mechanism by which D3 receptors regulate extracellular dopamine concentrati

241 However, the mechanisms by which D3 receptors regulate prefrontal circuits and whether D3

242 ors regulate prefrontal circuits and whether D3 receptors regulate specific prefrontal subnetworks re

243 Within these cells, we find that D3 receptors regulate the ability to generate high-frequ

244 Therefore, these data indicate that D3 receptors regulate the excitability of a unique, IT p

245 2.7 and 2.8 nM at the rat and human dopamine D3 receptors, respectively, and displays respective sele

246 ad K(i) values of 62.8 and 2.4 nM for D2 and D3 receptors, respectively.

247 n (K(i)) values of 1.8 and 0.2 nM for D2 and D3 receptors, respectively.

248 Kd = 1.32 nM) to the direct repeat 3 vitamin D3 receptor response element (DR3VDRE).

249 artite information weight matrix for vitamin D3 receptor/retinoid X receptor alpha (VDR/RXRalpha) bin

250 ons have been hampered by the lack of highly D3 receptor selective compounds that can be used in vivo

251 ts of buspirone were similar to those of the D3 receptor-selective antagonist PG01037 and qualitative

252 Here we have designed BP 897, the first D3-receptor-selective agonist, as assessed in vitro with

253 To address this problem, the potent and D3-receptor-selective antagonist NGB 2904 (1, 9H-fluoren

254 y play a role in both enantioselectivity and D3 receptor selectivity.

255 r smoking increases DA concentrations at the D3 receptor, speculated to have a role in nicotine's add

256 epitope tag, or an HA-tagged version of the D3 receptor splice variant D3nf.

257 D3 receptor stimulation activated phosphoinositide 3-kin

258 The dopamine D3 receptor subtype has been recently targeted as a pote

259 Dopamine D3 receptor subtypes have been hypothesized to play a pi

260 clues for the diversity in SAR at the D2 and D3 receptor subtypes.

261 ridol or genetic ablation of dopamine D2 and D3 receptors, suggesting that blockade of D2-like signal

262 we coimmunoprecipitated HA- and FLAG-tagged D3 receptors, suggesting that D3 receptors are capable o

263 se responses were accompanied by dopamine D2/D3 receptor supersensitivity.

264 ful in determining how intrinsic activity at D3 receptors tested in vitro is related to behaviors in

265 nearly 5 times more potent antagonist at the D3 receptor than 1 (EC50 = 14.4 nM).

266 Recent studies using ligands for the vitamin D3 receptor, the peroxisome proliferator-activated recep

267 8) exhibited the highest affinity for D2 and D3 receptors, the (-)-isomer being the eutomer.

268 cells co-expressing dopamine transporter and D3 receptors, the D2/D3 agonist quinpirole produced a ra

269 We propose a functional model in which the D3 receptor tightly regulates neurotransmitter release a

270 s, and the weak and inconsistent coupling of D3 receptors to classical signal transduction pathways.

271 Thus, low dopamine activates D3 receptors to limit reflex excitability.

272 stimulation of mitogenesis at human dopamine D3 receptors transfected into Chinese hamster ovary (CHO

273 rs in the midbrain while leaving striatal D2/D3 receptors unchanged.

274 drug wanting." We conclude that the dopamine D3 receptor, unlike the D2 receptor, might be upregulate

275 ompounds were determined for dopamine D2 and D3 receptors using radioligand binding techniques.

276 duces its hormone signal through the vitamin D3 receptor (VDR), a ligand-modulated transcription fact

277 vitamin D3 [1,25(OH)2D3] through the vitamin D3 receptor (VDR).

278 ch immunostain for the 1,25-dihydroxyvitamin D3 receptor (VDR).

279 ted that retinoic acid (RAR-RXR) and vitamin D3 receptors (VDR-RXR) heterodimers recruit only one coa

280 nt study, binding of 29 known ligands to the D3 receptor was modeled computationally using four D3 re

281 he 5-hydroxy series, highest selectivity for D3 receptors was exhibited by compound (-)- 25 ( K i = 0

282 activation, which may impact on both D2 and D3 receptors, was exclusively associated with variations

283 s with endogenous dopamine for binding to D2/D3 receptors, we interpret the decreases in binding to r

284 These critical regions of the D3 receptor were highly homologous to those of the D2 re

285 D2 and D3 receptors were also found to interact with the highly

286 lly coupled to Galphai2, whereas striatal D2/D3 receptors were coupled equally to Galphai2 and Galpha

287 highest binding affinity and selectivity for D3 receptors were exhibited by (-)-34 (Ki=0.92 nM and D2

288 of choice behavior, while drugs that act on D3 receptors were ineffective.

289 ced into the stable D3-expressing cell line, D3 receptors were no longer visualized at the plasma mem

290 nstrated for the first time that midbrain D2/D3 receptors were preferentially coupled to Galphai2, wh

291 asures high-affinity, functionally active D2/D3 receptors, whereas the traditionally used radiotracer

292 The dopamine D3 receptor, which is highly enriched in nucleus accumbe

293 y relationships for this class of ligands at D3 receptors will provide new leads toward the developme

294 agonist activity with picomolar affinity for D3 receptor with high selectivity (EC50=0.08 nM and D2/D

295 at this compound is a partial agonist at the D3 receptor with no detectable activity at the D2 recept

296 t with HEK-293 cells expressing either D2 or D3 receptor with tritiated spiperone to evaluate inhibit

297 However, expression of D2 or D3 receptors with a protein 4.1N truncation fragment red

298 GTP sensitive and GTP insensitive states of D3 receptors with distinctive high and low affinity stat

299 t with HEK-293 cells expressing either D2 or D3 receptors with tritiated spiperone to evaluate inhibi

300 t with HEK-293 cells expressing either D2 or D3 receptors with tritiated spiperone to evaluate inhibi