萘普生/奥美拉唑(Naproxen/Omeprazole) - 药物靶点：COX x Proton pump_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Omeprazole/naproxen

靶点

COX x Proton pump

作用机制

COX抑制剂(环氧化酶抑制剂)、质子泵抑制剂

治疗领域

免疫系统疾病感染消化系统疾病+ [2]

在研适应症-

非在研适应症

强直性脊柱炎骨关节炎类风湿关节炎+ [2]

原研机构

Old API Wind-down Ltd.

在研机构-

非在研机构

POZEN, Inc.

最高研发阶段无进展临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C17H19N3O3S

InChIKeySUBDBMMJDZJVOS-UHFFFAOYSA-N

CAS号73590-58-6

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关联

2

项与萘普生/奥美拉唑相关的临床试验

NCT00442208 / Completed临床1期

An Open-Label, Randomized, Comparative 3-Way Cross-Over Study to Evaluate the Effect of Food on the 24-Hour Intragastric pH at Day 5 After Twice Daily Oral Administration of PN 200 (Omeprazole/Naproxen) in Healthy Volunteers

Primary: To compare the pharmacodynamic efficacy of PN 200 in controlling intragastric pH (percent time pH> 4.0) following twice daily administration at different dosing times relative to food (30 or 60 minutes prior to food or taken togeterh with food) on Day 5.

开始日期2007-01-01

申办/合作机构

POZEN, Inc.

NCT00367211 / Completed临床3期

A 6-Month, Phase 3, Randomized, Double-Blind, Parallel-Group, Controlled, Multi-Center Study to Evaluate the Incidence of Gastric Ulcers Following Administration of Either PN 200 or Naproxen in Subjects Who Are at Risk for Developing NSAID-Associated Ulcers.

The purpose of this study is to evaluate the incidence of gastric ulcers following administration of either PN 200 or Naproxen in subjects who are at risk for developing NSAID-associated ulcers.

开始日期2006-09-01

申办/合作机构

POZEN, Inc.

100 项与萘普生/奥美拉唑相关的临床结果

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100 项与萘普生/奥美拉唑相关的转化医学

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100 项与萘普生/奥美拉唑相关的专利（医药）

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3

项与萘普生/奥美拉唑相关的文献（医药）

1991-01-01·Toxicology3区 · 医学

Effect of manganese (II) bis(glycinate)dichloride on Ca2+ channel function in cultured chick atrial cells

3区 · 医学

Article

作者: Gretchen M. Hehn ; Joey V. Barnett ; Jonas B. Galper ; Steven C. Quay ; Wen Tan

Manganese (II) bis(glycinate)dichloride (Mn(glycinate)2) is a coordination complex of manganese with application as a contrast enhancement agent for magnetic resonance imaging in the heart. To determine the cardioactivity of the manganese ion in this chelation cage, the effects of Mn(glycinate)2 on Ca channel function in the cultured chick atrial cell was studied. Mn(glycinate)2 decreased amplitude of contraction in chick atrial cells from embryos 14 days in ovo with complete inhibition of beating at 1 mM and half-maximal effect at 0.1 mM. Under control conditions, Bay K 8644, a Ca channel activator increased amplitude of contraction by 86% with a half maximal effect at 3.2 x 10(-7) M. In the presence of 0.025 mM Mn(glycinate)2, a concentration which had no effect on the amplitude of contraction, the maximum response to Bay K 8644 was decreased to 31%. Mn(glycinate)2 had no effect on the EC50 for the response to Bay K 8644, 1.7 +/- 0.1 x 10(-9) M (S.E.M., n = 4) in control cells compared to 2.2 +/- 0.4 x 10(-9) M (S.E.M., n = 4) in cells incubated with Mn(glycinate)2. 45Ca2+ uptake over 5 min in cultured chick atrial cells decreased from 2.0 nmol/mg protein in control cells to 1.5 nmol/mg protein in the presence of 10(-5) M PN200-110, a Ca2+ channel blocker, a decrease of 28%. 45Ca2+ uptake decreased to 0.94 nmol/mg protein (53%) in the presence of 1 nmol Mn(glycinate)2. Effects of Mn(glycinate)2 and PN200 were not additive. These data demonstrate that Mn(glycinate)2 exerts its negative inotropic effect, at least partially, by interfering with the function of the L-type Ca channels at high concentrations.

1989-11-01·Journal of Neurochemistry2区 · 医学

(+)‐PN200‐l 10 and Ouabain Binding Sites in Purified Bovine Adrenomedullary Plasma Membranes and Chromaffin Cells

2区 · 医学

Article

作者: Carlos J. F. Castillo ; Kurt Rosenheck ; Rosalba I. Fonteríz ; Manuela G. López ; Antonio G. García

Abstract: Bovine adrenal medulla plasma membranes were purified by a differential centrifugation procedure using sucrose and Urografin discontinuous density gradients; the membranes were enriched 10‐ 12‐fold in acetylcholinesterase activity and [3H]ouabain binding sites. Specific (+)‐[3H]PN200‐1 10 binding to these membranes amounted to 90% of total binding and was saturabie and of high affinity (KD= 41 pM; Bmax= 119 fmol/mg of protein) with a Hill coefficient close to I, a result suggesting the presence of a single, homogeneous population of dihydropyridine receptors. The association and dissociation rate constants were, respectively, 7.5 × 10′ M‐′ rnin‐l and 0.023 min‐I. Unlabeled (+)‐PN200‐110 displaced (+)‐[3H]PN200‐ 1 10 binding with a potency 100‐fold higher than (‐)‐PN200‐1 10 (ICsO, 0.5 and 45 nM, respectively). Although the two enantiomers of BAY K 8644 completely displaced (+)‐[3H]PN200‐1 10 binding, they exhibited no stereoselectivity (ICsO, 69 and 83 nM, respectively). Whereas (i‐)‐nitrendipine very potently displaced (+)‐[3H]PN200‐l 10 binding (ICsO = 1.3 nM), verapamil and cinnarizine displaced the binding by only 30 and 40% at 1 FM, and diltiazem increased it by 20% at 10 pM. [3H]Ouabain bound to plasma membranes with a KD of 34 nM and a Bmax of 9.75 pmol/mg of protein, a figure 80‐fold higher than the Bmax for (+)‐PN200‐ 1 10. t3H]Ouabain also bound to intact chromaffin cells with a Bmax of 244 fmol/106 cells. This figure, together with the plasma membrane ouabain/(+)‐PNZOO‐ I I0 ratio of 80, allows the calculation of 1,884 (+)‐PN200‐110 binding sites/cell. Assuming a 1: 1 stoichiometry, this means that intact chromaffin cells contain ‐ 1.5 L‐type, dihydropyridine‐associated, voltage‐dependent Ca2+ channels/pm2 of surface area.

1987-10-01·Journal of Neurochemistry2区 · 医学

Insulin Enhances Development of Functional Voltage‐Dependent Ca²⁺ Channels in Aneurally Cultured Human Muscle

2区 · 医学

Article

作者: W. King Engel ; Valerie Askanas ; Claude Desnuelle

Abstract: Voltage‐dependent Ca2+ channels were studied by the binding of the potent Ca2+ channel antagonist PN200‐MO and by the K+‐induced 45Ca2+ uptake in human muscle cultured aneurally in the presence of insulin, fibroblast growth factor, and epidermal growth factor, added in combination or individually. Compared to the muscle grown in medium without growth factors, 14–15 days of treatment with insulin (10 μg/rnI) alone or in combination with two other growth factors caused a 3.4‐and 3.8‐fold increase per culture dish in the number of PN200–110 binding sites, respectively. There was no change in the affinity of the ligand‐receptor complex. Under the same conditions, there was also a fourfold increase of the K+‐in‐duced 45Ca2+ uptake in cultured human muscle. Neither fibroblast growth factor nor epidermal growth facto alone influenced PN200–110 binding sites. Our study demonstrates that insulin enhances the development of functional voltage‐dependent Ca2+ channels in cultured human muscle.

100 项与萘普生/奥美拉唑相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
强直性脊柱炎	临床3期	美国	POZEN, Inc.	2006-09-01
骨关节炎	临床3期	美国	POZEN, Inc.	2006-09-01
类风湿关节炎	临床3期	美国	POZEN, Inc.	2006-09-01
胃溃疡	临床3期	美国	POZEN, Inc.	2006-09-01
溃疡	临床3期	美国	POZEN, Inc.	2006-09-01