ライフサイエンスコーパス: H3 receptor

1 ndistinguishable from that for the histamine H3 receptor.

2 and subnanomolar affinities at human and rat H3 receptors.

3 hanism that does not utilize brain H1, H2 or H3 receptors.

4 H1 or H2 receptors, but had weak activity on H3 receptors.

5 ptors, adenosine A1-receptors, and histamine H3-receptors.

6 These ligands have high H3 receptor affinity, thereby illustrating how the model

7 The H3-receptor agonist imetit (0.1 micromol/L) decreased ca

8 The H3-receptor agonist imetit attenuated the inotropic resp

9 bination therapy of sigma1R antagonists with H3 receptor agonists could serve to reduce some effects

10 lcium mobilization response to histamine and H3 receptor agonists including imetit and immepip.

11 or antagonist cimetidine (20 microM) nor the H3 receptor antagonist thioperamide (20 microM) prevente

12 A new structural series of histamine H3 receptor antagonist was developed.

13 reasing histamine release in the CNS with an H3 receptor antagonist-increased hypophagia.

14 This effect was blocked by the H3-receptor antagonist thioperamide (0.3 micromol/L), in

15 The effects of imetit were blocked by the H3-receptor antagonist thioperamide.

16 d the relative efficacy of a novel selective H3-receptor antagonist, JNJ-39220675, in preventing nasa

17 New, potent, and selective histamine H3 receptor antagonists have been synthesized by employi

18 ole (32) is one of the most potent histamine H3 receptor antagonists reported to date.

19 This series represents a new scaffold of H3 receptor antagonists that demonstrates in vivo exposu

20 A new series of H3 receptor antagonists was discovered with nanomolar an

21 ualitative pharmacophore model for histamine H3 receptor antagonists.

22 H3 receptor antagonists/inverse agonists also may be use

23 in several disease models, its binding to a H3 receptor as well as a hERG channel prevented it from

24 Histamine, acting via H3 receptors, augments acid secretion by eliminating the

25 0.13 nM) demonstrated a stereopreference in H3 receptor binding affinity for the (1R,2R) enantiomer

26 ioligand for determination of human cerebral H3 receptor binding and allows highly reproducible in vi

27 ptor antagonist, but not by selective H1 and H3 receptor blockers, and were mimicked by an H2 recepto

28 The availability of the human H3 receptor cDNA should greatly aid in the development o

29 and occurs upon cocaine binding to sigma1-D1-H3 receptor complexes.

30 directly via H2 receptors and indirectly via H3 receptors coupled to inhibition of somatostatin secre

31 eviously showed that prejunctional histamine H3-receptors downregulate norepinephrine exocytosis, whi

32 mplies that endogenous histamine, acting via H3 receptors, exerts an inhibitory paracrine influence o

33 caudate nucleus) previously associated with H3 receptor function.

34 A new histamine H3 receptor (H3R) antagonist chemotype 1 was designed by

35 Since H3 receptor (H3R) antagonists/inverse agonists can impro

36 Ciproxifan is a well-investigated histamine H3 receptor (H3R) inverse agonist/antagonist, showing an

37 rs of the biologic effects of histamine, the H3 receptor (H3R) is distinguished for its almost exclus

38 oamine oxidases A/B as well as the histamine H3 receptor (H3R) were obtained by optimization of the n

39 Receptors for histamine, especially the H3 receptor (H3R), are highly expressed in the striatum,

40 wild-type animals, mice with a disrupted HA H3 receptor (H3RKO), the expression of which is normally

41 The human histamine H3 receptor (hH3R) is subject to extensive gene splicing

42 , S) have been synthesized and evaluated for H3-receptor histamine antagonism in vitro (Ki for [3H]hi

43 cription-PCR analysis revealed expression of H3 receptors in a population of GABAergic neurons, while

44 ine (6), was discovered to bind to histamine H3 receptors in a radioligand-based high-throughput scre

45 was designed to characterize the location of H3 receptors in the fundus of the stomach and the mechan

46 The role of histamine H3 receptors in the regulation of gastric acid secretion

47 134, 2 potential IA drugs targeting cerebral H3 receptors, in 6 healthy male subjects (age, 19-40 y).

48 Because prejunctional histamine H3-receptors inhibit transmitter release from autonomic

49 H3 receptor inverse agonists (IAs) may be efficacious in

50 The histamine 3 (H3) receptor is a presynaptic autoreceptor in the centra

51 tor by an antagonist restores the protective H3 receptor-mediated brake on D1 receptor signaling and

52 ition binding as well as functional tests of H3 receptor-mediated calcium mobilization and GTPgammaS

53 m may be cocaine's blockade of the histamine H3 receptor-mediated inhibition of D1 receptor function.

54 onomic nerves, we tested the hypothesis that H3-receptors modulate CGRP release in the heart.

55 n the present study, we investigated whether H3-receptors modulate nonexocytotic norepinephrine relea

56 r biodistribution, quantification, and brain H3 receptor occupancy (RO) of MK-0249 and MK-3134, 2 pot

57 in turn inhibits CGRP releases by activating H3-receptors on C-fiber terminals.

58 rain-penetrant antagonist/inverse agonist of H3 receptors, on AHN (proliferation, maturation and surv

59 isplayed high affinity at both rat and human H3 receptors (pKi = 7.61 and 8.27) and generally high se

60 acid secretion induced by the activation of H3 receptors reflected changes in somatostatin secretion

61 ions of preoptic neurons that express H1 and H3 receptor subtypes, respectively.

62 antinociception is mediated by an action on H3 receptors, the effects of the H3 agonist R-alpha-meth

63 or was found to closely resemble that of the H3 receptor; the major difference was that (R)-alpha-met

64 The existence of the histamine H3 receptor was demonstrated pharmacologically 15 years