SER-100(SER-100) - 药物靶点：OOR_专利_临床

概要

基本信息

药物类型

合成多肽

别名

AC-RYYRWKKKKKKK-NH2、Acetyl-Arg-Tyr-Tyr-Arg-Trp-Lys-Lys-Lys-Lys-Lys-Lys-Lys-NH2

+ [7]

靶点

OOR

作用机制

OOR激动剂(孤啡肽受体激动剂)

治疗领域

心血管疾病呼吸系统疾病

在研适应症-

非在研适应症

急性失代偿性心力衰竭高血压肺性高血压

原研机构

Zealand Pharma A/S

在研机构-

非在研机构

Serodus ASAZealand Pharma US, Inc.

最高研发阶段终止临床2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C85H141N27O15

InChIKeyGJLXVWOMRRWCIB-MERZOTPQSA-N

CAS号383123-18-0

序列信息

Sequence Code 1319966

关联

3

项与 SER-100 相关的临床试验

NCT01987284 / Completed临床2期

A Randomized, Double-blind, Placebo-controlled, Cross-over, Multi-center Study Assessing the Safety, Tolerability and Efficacy of SER100 10 mg s.c. Twice Daily for 2 Days in Patients With Isolated Systolic Hypertension Insufficiently Treated With One or More Anti-hypertensives.

Isolated Systolic Hypertension (ISH)is the dominating hypertensive disease in elderly people. Much attention has recently been drawn to the strong relationship between the systolic blood pressure and cardiovascular morbidity.
In previous clinical studies carried out in individuals with normal blood pressure at baseline SER100 decreased primarily the systolic blood pressure. It is hypothesized that the effect on systolic blood pressure in hypertensive patients will be larger or equal to the fall seen in normotensive patients.

开始日期2013-10-01

申办/合作机构

Noregs forskingsråd

[+1]

NCT00283361 / Terminated临床2期

A Phase II,Randomized, Double-Blind, Flexible Dose Study of ZP120 I.V. Infusion as Add-On Therapy in Patients With Acute or Sub-Acute Decompensated Chronic Heart Failure NYHA Class III-IV Treated With Furosemide

The main purpose of this study is to see if the experimental drug ZP120, when given with the approved drug furosemide to patients with acute or sub-acute heart failure, can reduce the amount of fluid in the patients' lungs and make breathing easier.

开始日期2006-01-01

申办/合作机构

Zealand Pharma US, Inc.

[+1]

EUCTR2004-004801-11-DK / Unknown status临床2期

A Phase II, Multicenter, Double-Blind, Efficacy, Safety, and Tolerability Study of ZP120 Administered as Short Term I.V. Infusion as Add-On Therapy in Patients with Subacute Decompensated Chronic Heart Failure NYHA Class III-IV Treated with Furosemide - NA

开始日期2005-02-14

申办/合作机构

Zealand Pharma A/S

100 项与 SER-100 相关的临床结果

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100 项与 SER-100 相关的转化医学

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100 项与 SER-100 相关的专利（医药）

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153

项与 SER-100 相关的文献（医药）

2024-01-11·Journal of Medicinal Chemistry1区 · 医学

Structure–Activity Relationships of a Novel Cyclic Hexapeptide That Exhibits Multifunctional Opioid Agonism and Produces Potent Antinociceptive Activity

1区 · 医学

Article

作者: Wu, Shuyuan ; Zhang, Shichao ; Xu, Biao ; Zhang, Xiaodi ; Yang, Zhenyun ; Zhang, Qinqin ; Fang, Quan ; Chen, Dan ; Hu, Xuanran ; Yu, Bowen ; Zhang, Mengna

The cyclic peptide c[d-Lys², Asp⁵]-DN-9 has recently been identified as a multifunctional opioid/neuropeptide FF receptor agonist, displaying potent analgesic activity with reduced side effects. This study utilized Tyr-c[d-Lys-Gly-Phe-Asp]-d-Pro-NH₂ (0), a cyclic hexapeptide derived from the opioid pharmacophore of c[d-Lys², Asp⁵]-DN-9, as a chemical template. We designed, synthesized, and characterized 22 analogs of 0 with a single amino acid substitution to investigate its structure-activity relationship. Most of these cyclic hexapeptide analogs exhibited multifunctional activity at μ and δ opioid receptors (MOR and DOR, respectively) and produced antinociceptive effects following subcutaneous administration. The lead compound analog 15 showed potent agonistic activities at the MOR, κ opioid receptor (KOR), and DOR in vitro and produced a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test. Further biological evaluation identified that analog 15 did not cause significant side effects such as tolerance, withdrawal, or reward liability.

2023-12-01·Prostaglandins & Other Lipid Mediators

Tartary buckwheat protein-derived peptide AFYRW alleviates H2O2-induced vascular injury via the PI3K/AKT/NF-κB pathway

Article

作者: Xu, Qingzhong ; Zhang, Lilin ; Xiao, Yi ; Deng, Yan ; Yang, Jiajun ; Li, Hongmei

Tartary buckwheat protein-derived peptide (Ala-Phe-Tyr-Arg-Trp, AFYRW) is a natural active peptide that hampers the atherosclerosis process, but the underlying role of AFYRW in angiogenesis remains unknown. Here, we present a system-based study to evaluate the effects of AFYRW on H₂O₂-induced vascular injury in human umbilical vein endothelial cells (HUVECs). HUVECs were co-incubated with H₂O₂ for 2 h in the vascular injury model, and AFYRW was added 24 h in advance to investigate the protective mechanism of vascular injury. We identified that AFYRW inhibits oxidative stress, cell migration, cell invasion, and angiogenesis in H₂O₂-treated HUVECs. In addition, we found H₂O₂-induced upregulation of phosphoinositide 3-kinase (PI3K), protein kinase B (AKT), phosphorylation of nuclear factor-κB (NF-κB) p65 and nuclear translocation of NF-κB decreased by AFYRW. Taken together, AFYRW attenuated H₂O₂-induced vascular injury through the PI3K/AKT/NF-κB pathway. Thereby, AFYRW may serve as a therapeutic option for vascular injuries.

2023-09-01·Neuropsychopharmacology

Blocking μ-opioid receptors attenuates reinstatement of responding to an alcohol-predictive conditioned stimulus through actions in the ventral hippocampus

Article

作者: LeCocq, Mandy Rita ; Chander, Priya ; Chaudhri, Nadia

The µ-opioid system is involved in the reinstatement of responding that is immediately evoked by alcohol-predictive cues. The extent of its involvement in reinstatement observed in a new model that evaluates the delayed effects of re-exposure to alcohol, however, is unclear. The current study investigated the role of µ-opioid receptors (MORs) in the delayed reinstatement of an extinguished, Pavlovian conditioned response that was evoked 24 h after alcohol re-exposure. Female and male Long-Evans rats received Pavlovian conditioning in which a conditioned stimulus (CS) was paired with the delivery of an appetitive unconditioned stimulus (US; Experiments 1, 2, 4: 15% v/v alcohol; Experiment 3: 10% w/v sucrose) that was delivered into a fluid port for oral intake. During subsequent extinction sessions, the CS was presented as before but without the US. Next, the US was delivered but without the CS. A reinstatement test was conducted 24 h later, during which the CS was presented in the absence of the US. Silencing MORs via systemic naltrexone (0.3 or 1.0 mg/kg) attenuated reinstatement of port entries elicited by an alcohol-CS, but not those elicited by a sucrose-CS. Finally, blocking MORs in the ventral hippocampus via bilateral microinfusion of D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2 (CTAP; 2.5 or 5.0 µg/hemisphere) prevented reinstatement of port alcohol-CS port entries. These data show that MORs are involved in the delayed reinstatement of a Pavlovian conditioned response in an alcohol-specific manner. Importantly, these data illustrate, for the first time, that MORs in the ventral hippocampus are necessary for responding to an alcohol-predictive cue.

100 项与 SER-100 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB16013

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
高血压	临床2期	芬兰	Serodus ASA	2013-10-06
急性失代偿性心力衰竭	临床2期	美国	Zealand Pharma US, Inc.	2006-01-01
肺性高血压	临床2期	挪威	Serodus ASA	-