ライフサイエンスコーパス: kappa receptor

1 uced U50,488H-induced internalization of the kappa receptor.

2 lines expressing mRNA specific for the human kappa receptor.

3 tant role in potency and selectivity for the kappa receptor.

4 higher affinity for the delta than the mu or kappa receptor.

5 carboxamide (8d) with K(e) = 0.037 nM at the kappa receptor.

6 on of 8k had subnanomolar K(e) values at the kappa receptor.

7 the mu receptor and a K(i) of 0.03 nM at the kappa receptor.

8 sessing high affinity and selectivity at the kappa receptor.

9 g6 and Arg7, were crucial for binding to the kappa receptor.

10 ly useful in further characterization of the kappa receptor.

11 without significant loss in affinity for the kappa receptor.

12 u and delta receptors and antagonists at the kappa receptor.

13 a receptor and 10 of 22 mutants of the human kappa receptor.

14 nonconserved acidic residue (Glu297) on the kappa receptor.

15 a position equivalent to that of E297 in the kappa receptor.

16 the anionic address subsite, Glu297, on the kappa receptor.

17 ith weaker agonist activity at the delta and kappa receptors.

18 t the ligand binding sites of delta, mu, and kappa receptors.

19 tagonists but not by antagonists of delta or kappa receptors.

20 ), retained high affinity (Ki = 0.19 nM) for kappa receptors.

21 astrointestinal functions via mu, delta, and kappa receptors.

22 r opioid agonist activity and for potency at kappa receptors.

23 ing and nonbursting TH neurons by activating kappa receptors.

24 l requirement for good affinity at micro and kappa receptors.

25 d 19 was a partial agonist at both micro and kappa receptors.

26 played reasonably good affinity at micro and kappa receptors.

27 resulting in good selectivity for micro and kappa receptors.

28 ]GTPgammaS binding mediated by the micro and kappa receptors.

29 rm heteromeric complexes with both delta and kappa receptors.

30 ought to consist of only the mu-, delta- and kappa-receptors.

31 ed with the delta opioid receptor (69%), the kappa receptor (63%), and opioid receptor-like (ORL1) (5

32 this study show that the aversive effects of kappa receptor activation required arrestin-dependent p3

33 ication of channel toxins, and the effect of kappa receptor activation was tested.

34 In rats, kappa-receptor activation in this brainstem nucleus sign

35 Experimental manipulations showed that kappa-receptor activation increases astroglial [Ca2+]i b

36 l as functionally by examining the effect of kappa-receptor activation on intracellular calcium ([Ca2

37 kappa-receptor activation, either by repeated forced swi

38 cotine CPP or the anxiogenic-like effects of kappa-receptor activation.

39 D-Asp6,Dap9]Dyn A-(1-13)NH2 showed both high kappa receptor affinity and potent agonist activity in t

40 n smooth muscle preparations as well as high kappa receptor affinity and selectivity in receptor bind

41 ibited decreased mu receptor affinity, while kappa receptor affinity was retained or improved.

42 second alkyl group at the N-terminus lowered kappa-receptor affinity and selectivity.

43 and the identity of the alkyl group affected kappa-receptor affinity, selectivity, and efficacy.

44 (dl)-22] resulted in a > 10-fold increase in kappa-receptor affinity.

45 of D1 effects in the absence of presynaptic kappa receptors, after 6-hydroxydopamine depletion of st

46 Microinfusions of a kappa receptor agonist into the VLPO region increased NR

47 Second, the kappa receptor agonist spiradoline (1-10 mg/kg) reduced

48 chemistry for dynorphin (Dyn, the endogenous kappa receptor agonist) or endomorphin 1 (EM1, the endog

49 alin, a mu receptor agonist, and U-69,593, a kappa receptor agonist, were also blocked by G beta and

50 The delta, mu, and kappa receptor agonists stimulated the binding of guanos

51 -stimulated cAMP formation by delta, mu, and kappa receptor agonists was partially blocked by G alpha

52 Although kappa-receptor agonists can produce analgesia, behaviour

53 rols spinal pain transmission, we found that kappa-receptor agonists presynaptically inhibited glutam

54 re compared to the kinetics of recovery from kappa receptor alkylation by beta-chlornaltrexamine.

55 ester group, had affinity at both micro and kappa receptors almost identical to that of the parent l

56 s of the adult expression patterns of mu and kappa receptors already have been established.

57 mide (8e) with K(e) values of 0.03 nM at the kappa receptor and (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-

58 mide ( 3) with a K e value of 0.03 nM at the kappa receptor and 100- and 793-fold selectivity relativ

59 ompared to the Ke = 0.02 nM for JDTic at the kappa receptor and were highly selective for the kappa r

60 These mice expressed kappa receptors and delta receptors at near wild-type le

61 binding to the C7.38S mutants of the mu and kappa receptors and the wild-type delta receptor was rel

62 -13)NH2 showed moderate binding affinity for kappa receptors and was the most kappa selective ligand

63 orphine, a primary mu agonist, also binds to kappa-receptors and the analgesic effectiveness of morph

64 3 gave both high affinity and selectivity at kappa receptor, and N-2-phenylethyl analogue 18 exhibite

65 In most cases, high affinity at micro and kappa receptors, and lower affinity at delta receptor wa

66 Using a kappa receptor antagonist as a selective tool to test th

67 increase in nicotine CPP was blocked by the kappa-receptor antagonist norbinaltorphimine (norBNI) ei

68 th kappa opioid receptors, we tested whether kappa receptor antagonists could reverse ibogaine's effe

69 edures, the authors tested effects of mu and kappa receptor antagonists on ethanol reinforcement in n

70 lgesia were blocked by intra-RVM mu, but not kappa, receptor antagonists.

71 a key mediator of dysphoria, and emphasizes kappa-receptor antagonists as promising therapeutics.

72 l analogues 24 and 16 were moderately potent kappa-receptor antagonists in the [(35)S]GTPgammaS assay

73 ompounds in the development of peptide-based kappa-receptor antagonists.

74 e blocked spinally by mu- and delta- but not kappa-receptor antagonists.

75 The results imply that activation of mu and kappa receptors, apparently acting jointly, is necessary

76 Small molecule drugs that activate the kappa receptor are nonaddictive and safe to administer i

77 L6.56, V6.57, E6.58, A6.59, and L6.60 of the kappa receptor are on the water-accessible surface of th

78 48 acted similarly in human intestine, where kappa receptors are again expressed within its nervous s

79 e regulation of individual micro, delta, and kappa receptors are not understood.

80 We conclude that opioid mu, delta, and kappa receptors are selectively coupled to Gi2 and G(o)

81 the idea that the organization of delta and kappa receptors as heterodimers gives rise to delta(1) a

82 results in long-term alterations in mu- and kappa-receptor as well as POMC mRNA expression in the MB

83 nes (8, 13) had greatest selectivity for the kappa receptor, as predicted from consideration of the m

84 f the thalamus exhibit a surge in density of kappa-receptors at the time of the PT4 surge, while the

85 that chronic food restriction alters mu and kappa receptor binding in several regions of the rat for

86 Delta-, kappa1- and total kappa-receptor binding was present in all brain regions

87 in these two structures is a consequence of kappa receptor blockade.

88 ignificant agonist activity at the delta and kappa receptors but displayed moderate to potent antagon

89 Recovery of cultures after alkylation of kappa receptors by beta-chlornaltrexamine was significan

90 ining of cells transfected with the delta or kappa receptor cDNA, and by the abolition of staining wh

91 the effects of opiate agonists selective for kappa receptors, consistent with a major role for diacyl

92 The kappa-receptor containing cell groups are not identifiab

93 hese results also indicate that postsynaptic kappa receptors contribute to the inhibition of the D1 r

94 ceptors indicated that mu and delta, but not kappa, receptors contributed to the inhibitory effect of

95 rmined at putative subtypes of the delta and kappa receptors: deltacx-1 (mu-like), deltacx-2 (delta-l

96 ree daily injections produced an increase in kappa receptor density in the cingulate cortex, nucleus

97 Opioid (mu, delta, and kappa) receptor density and G-protein activation were no

98 robust agonist-mediated endocytosis, whereas kappa receptors do not.

99 JNK1 and that persistent inactivation of the kappa-receptor does not require sustained JNK activation

100 xhibited greatly reduced affinity for mutant kappa receptors (E297K and E297A).

101 In contrast, kappa receptors expressed in the same cells remain in th

102 ate gestation, the expression of both mu and kappa receptors extends to other brain regions that exhi

103 matched the regeneration rate of functional kappa receptors following irreversible antagonism and su

104 quirement of dopamine terminals (presynaptic kappa receptors) for the inhibitory action of dynorphin

105 nd 15,000-fold preference over the delta and kappa receptors) for the mu receptor.

106 d AtT-20 cells, agonist activation of either kappa receptor form produced equivalent activation of th

107 ent antagonist of excitatory mu-, delta- and kappa-receptor functions in naive and chronic morphine-t

108 onist norbinaltorphimine (norBNI, 1) and the kappa receptor have provided evidence that the selectivi

109 ed evidence for the bridging of spinal delta-kappa receptor heterodimers by KDN-21 and for their iden

110 Activation of the kappa-receptor hyperpolarizes neurons that are activated

111 oid antagonist activity and high affinity at kappa-receptors illustrates the importance of the 5'-pos

112 analogue) was 18-fold more selective for the kappa receptor in comparison to the delta receptor, whil

113 3a) had only 4-fold greater affinity for the kappa receptor in comparison to the delta receptor.

114 DTic, 10) demonstrated high affinity for the kappa receptor in the binding assay (kappa K(i) = 0.3 nM

115 CX and POA of females, but had no effects on kappa receptors in any of the examined brain regions in

116 ing affinity at the opioid delta, micro, and kappa receptors in brain membranes using radioligand bin

117 rmine the role of steric hindrance at mu and kappa receptors in promoting delta opioid receptor antag

118 hine exposure altered estrogen regulation of kappa receptors in the CX and POA of females, but had no

119 ited much higher affinity (Ki < 0.05 nM) for kappa receptors in the guinea pig cerebellum and greatly

120 lective involvement of mu and delta, but not kappa, receptors in EA-produced anti-hyperalgesia in rat

121 monstrated an involvement of RVM mu, but not kappa, receptors in EA-produced anti-hyperalgesia.

122 mu-opioid receptors, but the function of the kappa-receptor in opioid analgesia is unclear.

123 gher dose (10 micrograms) interacts with the kappa-receptor in regulation of Tb.

124 so of compensatory changes in mu-, delta- or kappa-receptors in the absence of ORL1 to be addressed.

125 o mask delta- and mu-receptors while mapping kappa-receptors in the nervous system, to provide an und

126 Mu-, delta-, kappa1- and total kappa-receptors, in adjacent coronal sections in fore- a

127 , gene knockout of JNK 1 selectively blocked kappa-receptor inactivation, whereas deletion of JNK 2 s

128 Using a model of the kappa-receptor, including the newly predicted EL2 turn-h

129 U50, 488H-induced human kappa receptor internalization was time- and concentrati

130 beta-arrestin, or dynamin I had no effect on kappa receptor internalization, co-expression of the dom

131 tion, etorphine, which did not promote human kappa receptor internalization, was able to fully activa

132 n from an inactive to an active state of the kappa-receptor involves a conformational change of TM6.

133 he reduced affinity upon modification of the kappa receptor is consistent with the ionic interaction

134 In addition, internalization of the kappa receptor is not required for activation of MAP kin

135 The overlap in distribution of mu- and kappa-receptors is considerable, but significant excepti

136 The distribution of kappa-receptors is more diffuse, and the densities are c

137 displaying excellent affinities at micro and kappa receptors (K(i) = 0.09-0.2 nM at micro and K(i) =

138 , as many as 50% of the astrocytes displayed kappa-receptor (KA8) immunoreactivity or exhibited incre

139 and more than 150-fold selectivity over the kappa receptor (KOR).

140 hosphoselective antibodies against activated kappa receptors (KOR-P) and against phospho-p38 MAPK.

141 e from the carboxyl terminus of a cloned rat kappa receptor (KT).

142 diated induction of dynorphin (an endogenous kappa receptor ligand) contributes to immobility behavio

143 estion that the binding conformation for the kappa receptor may have structural requirements that are

144 nce in activation of native, not recombinant kappa receptors may be explained by different mouse/huma

145 maximum Ih and significantly attenuated the kappa-receptor-mediated enhancement of Ih.

146 in vitro, and suggest that the activation of kappa-receptors mobilizes [Ca2+]i and inhibits cell prol

147 ted striatum, which contain higher levels of kappa receptor mRNA and binding.

148 -treated females; however, increased mu- and kappa-receptor mRNA expression as well as decreased POMC

149 rphine exposed females had increased mu- and kappa-receptor mRNA expression as well as decreased POMC

150 During lactation, mu- and kappa-receptor mRNA expression in the MBH decreased whil

151 e relative contributions of both presynaptic kappa receptors on dopamine terminals and postsynaptic k

152 ptors on dopamine terminals and postsynaptic kappa receptors on striatal neurons by analyzing opioid

153 ist pentazocine, which acts predominantly at kappa-receptors, produced significantly better postopera

154 The most prominently labeled kappa-receptor regions are the ventral and dorsal nuclei

155 All three compounds were selective for the kappa receptor relative to the micro and delta receptors

156 a receptor and were highly selective for the kappa receptor relative to the mu and delta opioid recep

157 and an 18-fold increase in affinity for the kappa receptor relative to the mu-selective ligand, (+)-

158 i) values of 0.95 and 0.62 nM for the mu and kappa receptors, respectively.

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

160 he putative second extracellular loop of the kappa receptor selectively recognizes residues 6-11 of d

161 led to a potent ligand (IC(50) 4.9 nM) with kappa receptor selectivity.

162 e guinea pig cerebellum and greatly enhanced kappa-receptor selectivity (Ki ratio (kappa/mu) > 200) c

163 ults were attributable to the attenuation of kappa-receptor signaling mechanisms and to dependence.

164 tes appear to exist predominantly within the kappa receptor since the selectivity arises from a 530-f

165 ibuted to activation of peripherally located kappa receptors, since 14b did not affect centrally medi

166 Schwyzer to adopt a helical conformation at kappa receptor sites.

167 The delta and kappa receptor-specific agonists cyclic[D-Pen2, D-Pen5]e

168 behavioural evidence that activation of the kappa-receptor specifically antagonizes mu-receptor-medi

169 This provides a physiological function for kappa-receptor-stimulated calcium release and may sugges

170 Kappa receptor stimulation produced analgesia and increa

171 say have often been ascribed to differential kappa receptor subtypes prevailing in central vs periphe

172 ry cells stably transfected with human mu or kappa receptor subtypes.

173 3, or 9 were found to be more potent for the kappa receptor than analogues with an L-Asp at the same

174 r affinity but similar selectivities for the kappa receptor than analogues with charged residues at t

175 approximately 2-fold more selective for the kappa receptor than for the mu receptor.

176 s been reported that KDN21 bridges delta and kappa receptors that are organized as heterodimers.

177 rms the co-existence of surrogate lambda and kappa receptors that are proposed to work in concert to

178 s indicate only subtle changes in delta- and kappa-receptors throughout the brains of animals deficie

179 Exposure of the human kappa receptor to the agonists U50,488H, U69,593, ethylk

180 ever, beta2 receptors, when coexpressed with kappa receptors, undergo neither opioid- nor isoproteren

181 ver, the proportion of astrocytes expressing kappa-receptors was greatest during a period of rapid ce

182 The binding characteristics of kappa receptors were assessed in the frontal cortex (CX)

183 affinities of these compounds for the mu and kappa receptors were in the micromolar or greater range

184 affinities of these compounds for the mu and kappa receptors were negligible, indicating excellent de

185 ORL1, mu-, delta- and kappa-receptors were labelled with [(3)H] leucyl-nocicep

186 The second extracellular loop of the kappa receptor, which contains several acidic residues,

187 U50,488H or etorphine stimulation of the rat kappa receptor, which did not undergo internalization, a

188 cted as partial or full agonists of delta or kappa receptors while retaining an antagonist profile at

189 e interaction of the pharmacophore at mu and kappa receptors, while not affecting delta receptors.

190 yed high affinities at opioid delta, mu, and kappa receptors with K(i) values of 0.78, 1.5, and 8.8 n

191 e delta-selective NTI could bind both mu and kappa receptors with significantly enhanced affinity whe

192 In mouse intestine, naturally expressing kappa receptors within its nervous system, both compound