ライフサイエンスコーパス: tetrabenazine

1 sicular monoamine transport (VMAT) inhibitor tetrabenazine.

2 but was restored by treating the slices with tetrabenazine.

3 with d-methamphetamine, methylphenidate, and tetrabenazine.

4 nt with methamphetamine, methylphenidate, or tetrabenazine.

5 blocked by 1 microM reserpine and 10 microM tetrabenazine.

6 e neurotransmitters as well as the inhibitor tetrabenazine.

7 rotonin and histamine and the sensitivity to tetrabenazine.

8 R was blocked by 100 nM reserpine, 10 microM tetrabenazine, 1 mM serotonin, and 10 mM (-)-norepinephr

9 [125I]2-N-[(3'-iodo-4'-azidophenyl)propionyl]tetrabenazine ([125I]TBZ-AIPP).

10 2 vesicular monoamine transporter) inhibitor tetrabenazine (9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6

11 Tetrabenazine, a monoamine depleter and dopamine recepto

12 In addition to tetrabenazine, a monoamine-depleting drug, new formulati

13 All 19 patients continued to take tetrabenazine after the study.

14 inically relevant dopamine pathway inhibitor tetrabenazine alleviated the motor deficits and reduced

15 The pharmacologic inhibitors carbidopa and tetrabenazine also revealed differential effects between

16 ater (10:1) gave direct cyclization to (+/-)-tetrabenazine and occurred more rapidly.

17 Drug therapy with benzhexol, tetrabenazine and pimozide or haloperidol may be benefic

18 Furthermore, transient exposure to tetrabenazine and reserpine, but not methyl reserpate an

19 s, we demonstrated that the VMAT2 inhibitors tetrabenazine and Ro 4-1284 inhibit P-GP and that the P-

20 tion K446Q reduced the affinity of VMAT2 for tetrabenazine and serotonin but not histamine, whereas F

21 enuated by inhibitors of VMAT (reserpine and tetrabenazine) and DAT (GBR12909 and rimcazole).

22 lowing 15-min incubations with reserpine and tetrabenazine, as evidenced by a decrease in exocytotic

23 cellular studies revealed that reserpine and tetrabenazine at concentrations near their K(i) values n

24 , demonstrating involvement of TM 10-12 in a tetrabenazine binding domain.

25 ffinity than the endo,endo analogue 3 at the tetrabenazine binding site on VMAT2, indicating that the

26 demonstrating that Cys(439) is either at the tetrabenazine binding site, or conformationally linked t

27 binding site, or conformationally linked to tetrabenazine binding.

28 binds the cytoplasm-facing conformation, and tetrabenazine binds the lumen-facing conformation.

29 rt than of VMAT1-mediated transport, whereas tetrabenazine binds to and inhibits only VMAT2.

30 and histamine as well as the sensitivity to tetrabenazine but only in the context of more C-terminal

31 A behaviorally active dose of tetrabenazine decreased extracellular DA in nucleus accu

32 e rated after a mean of 20.3 weeks at a mean tetrabenazine dose of 57.9 mg/day.

33 Citing the use of tetrabenazine for chorea in Huntington disease, adrenoco

34 The authors studied the use of tetrabenazine for tardive dyskinesia.

35 ol/g tissue) with a pharmacological profile (tetrabenazine > or = iodovinyltetrabenazine > ketanserin

36 erpine and one iodophenylazide derivative of tetrabenazine have been synthesized and characterized as

37 ognition of the ring nitrogen that occurs in tetrabenazine, histamine, and serotonin but not dopamine

38 nd Asp-461 with Asn reduced the affinity for tetrabenazine, histamine, and serotonin.

39 he higher affinity interaction of VMAT2 with tetrabenazine, histamine, and serotonin.

40 nic amine uptake, and in vivo by reversal of tetrabenazine-induced ptosis.

41 Tetrabenazine is a high-affinity inhibitor of the vesicu

42 Tetrabenazine is efficacious for chorea control; however

43 The effects of tetrabenazine on effort-related choice were reversed by

44 (one); discontinuation of lithium (one) and tetrabenazine (one); and the introduction of clonazepam

45 that antagonists of dopamine pathway such as tetrabenazine or dopamine receptor blockers may have a t

46 One patient did not tolerate tetrabenazine owing to sedation.

47 Drug therapy used included benzhexol, tetrabenazine, pimozide, baclofen, chlorpromazine, halop

48 tension, and by the noncompetitive inhibitor tetrabenazine, presently in use for symptomatic treatmen

49 Additions of organometallic reagents to tetrabenazine produced 2-methyl, 2-ethyl, 2-n-propyl, 2-

50 Tetrabenazine produces depressive symptoms in humans and

51 Supporting a direct effect, the position of tetrabenazine-protectable Cys 439 is consistent with pre

52 esicles expressing VMAT2 show reserpine- and tetrabenazine-protectable photolabeling by [125I]IAmF.

53 the active metabolites of the prior, stable tetrabenazine regimen.

54 we now show that the sensitivity of VMAT2 to tetrabenazine requires Ala-315, and this interaction occ

55 uces serotonin but not histamine affinity or tetrabenazine sensitivity in the context of more N-termi

56 tonin affinity but not histamine affinity or tetrabenazine sensitivity, and whereas the region from T

57 ty and perhaps histamine recognition but not tetrabenazine sensitivity, providing more evidence for s

58 a partial increase in substrate affinity and tetrabenazine sensitivity.

59 Tetrabenazine shifted response choice in rats, producing

60 The enantioselective synthesis of (+)-tetrabenazine (TBZ) and (+)-dihydrotetrabenazine (DTBZ),

61 Tetrabenazine (TBZ) is a non-competitive inhibitor of VM

62 Our results show that ketanserin and tetrabenazine (TBZ) strikingly abolished the aggressive

63 cular monoamine transport (VMAT-2) inhibitor tetrabenazine (TBZ) were investigated.

64 urified rVMAT2 were protectable by 10 microM tetrabenazine (TBZ), 10 microM 7-aminoketanserin, and 1

65 oved drug for the treatment of chorea in HD, tetrabenazine (TBZ).

66 and 2-N-[(3'-iodo-4'-azidophenyl)-propionyl]tetrabenazine (TBZ-AIPP).

67 ll as a greater sensitivity to the inhibitor tetrabenazine than the nonneuronal VMAT1.

68 on and the recognition of both histamine and tetrabenazine that may account for the observed differen

69 nd Australia who were taking stable doses of tetrabenazine that provided a therapeutic benefit were s

70 interactions with serotonin, histamine, and tetrabenazine, the region of VMAT2 from TMD3 through TMD

71 ng the VMAT2-specific ligands ketanserin and tetrabenazine, this study describes the synthesis and ch

72 and explore the efficacy of conversion from tetrabenazine to deutetrabenazine in patients with chore

73 ncreased stereotypies that were decreased by tetrabenazine treatment.

74 3.7 months) were videotaped before and after tetrabenazine treatment.

75 (+/-)-Tetrabenazine was synthesized in six steps from commerci

76 Tetrabenazine was well tolerated and resulted in signifi

77 ich blocks VMAT1 and VMAT2, but resistant to tetrabenazine, which is a selective inhibitor of VMAT2.

78 These experiments demonstrate that tetrabenazine, which is used in animal models to produce