GS-1590(GS-1590) - 药物靶点：BDNF x NGF_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

BDNF x NGF

作用机制

BDNF激动剂(脑源性神经营养因子激动剂)、NGF刺激剂(神经生长因子刺激剂)、神经元刺激剂

治疗领域

神经系统疾病

在研适应症-

非在研适应症

神经系统疾病

原研机构

Cephalon, Inc.

在研机构-

非在研机构

LEO Pharma A/S

最高研发阶段终止临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C30H44O3

InChIKeyPSFKUDRQUWPZMR-JBINGYQBSA-N

CAS号163005-56-9

关联

100 项与 GS-1590 相关的临床结果

登录后查看更多信息

100 项与 GS-1590 相关的转化医学

登录后查看更多信息

100 项与 GS-1590 相关的专利（医药）

登录后查看更多信息

1

项与 GS-1590 相关的文献（医药）

2004-03-01·The Journal of Steroid Biochemistry and Molecular Biology2区 · 生物学

Vitamin D3 polyunsaturated side-chain analogues (EB1089, GS1590) and the 20-epi-vitamin D3 analogue CB1393 suppress parathyroid hormone secretion and mRNA level in bovine parathyroid cells

2区 · 生物学

Article

作者: Lise Binderup ; Pernille Kaae Holm ; Göran Åkerström ; Ulrika Segersten ; Per Hellman ; Gunnar Westin

Several vitamin D analogues, with reduced hypercalcemic and hyperphosphatemic toxicity at therapeutic dosages, are in clinical use for prevention and treatment of secondary hyperparathyroidism (HPT) in chronic renal failure. We have performed a first in vitro evaluation of five vitamin D analogues displaying less calcemic activity in normal rats, considerably more antiproliferative ability and higher transcription activation potential than 1,25-dihydroxyvitamin D(3) (1,25(OH)(2)D(3)), with the future prospects in mind to identify even more effective and less calcemic vitamin D analogues for treatment of HPT. The vitamin D analogues EB1089 and GS1590 have polyunsaturated side-chains, whereas HEP187, MC1598 and CB1393 display altered stereochemistry at carbon 20. In primary cultures of bovine parathyroid cells EB1089, GS1590, CB1393 and MC1598 as well as the comparative controls 1,25(OH)(2)D(3), 22-oxacalcitriol (OCT, maxacalcitol), 19-nor-1,25(OH)(2)D(2) (paricalcitol) and 1alpha(OH)D(2) (doxercalciferol) significantly suppressed PTH secretion or reduced PTH mRNA level at 10(-8), 10(-10), and 10(-11)M for all compounds except for MC1598 at the lowest concentration. The analogue HEP187 displayed no PTH suppressive activity. We conclude that the vitamin D analogues EB1089, GS1590 and CB1393 may be suitable for treatment of hyperparathyroidism secondary to uremia and that further evaluation in vivo should be considered.

100 项与 GS-1590 相关的药物交易

登录后查看更多信息