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 safety of pitolisant, a selective histamine H3 receptor antagonist with wake-promoting effects, for

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

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

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

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

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

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

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

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

22 ualitative pharmacophore model for histamine H3 receptor antagonists.

23 H3 receptor antagonists/inverse agonists also may be use

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

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

26 0.13 nM) demonstrated a stereopreference in H3 receptor binding affinity for the (1R,2R) enantiomer

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

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

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

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

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

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

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

34 caudate nucleus) previously associated with H3 receptor function.

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

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

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

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

39 The histamine H3 receptor (H3R) is highly enriched in the spiny projec

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

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

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

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

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

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

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

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

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

49 134, 2 potential IA drugs targeting cerebral H3 receptors, in 6 healthy male subjects (age, 19-40 y).

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

51 a(2+) channels blockade, cholinesterase, and H3 receptor inhibition were obtained by multicomponent s

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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