更新于：2024-11-01

HP-228

更新于：2024-11-01

概要

研发状态

概要

基本信息

药物类型

小分子化药

别名

靶点-

作用机制-

治疗领域

神经系统疾病内分泌与代谢疾病其他疾病+ [2]

在研适应症-

非在研适应症

哮喘化疗引起的损伤2型糖尿病+ [3]

原研机构

Sygnis Bioscience GmbH & Co KG

在研机构-

非在研机构

Sygnis Bioscience GmbH & Co KG

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C47H66ClN15O9

InChIKeyGIVHMWDXPMQVKJ-XDOYWBIESA-N

CAS号232601-62-6

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序列信息

Sequence Code 440955

关联

100 项与 HP-228 相关的临床结果

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100 项与 HP-228 相关的转化医学

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100 项与 HP-228 相关的专利（医药）

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项与 HP-228 相关的文献（医药）

2007-06-01·Current Topics in Medicinal Chemistry4区 · 医学

Melanocortins in the Treatment of Male and Female Sexual Dysfunction

4区 · 医学

Review

作者: Shubh D. Sharma ; Annette M. Shadiack ; Carl Spana ; Dennis C. Earle ; Trevor J. Hallam

Melanocortinergic agents are currently being investigated for a possible therapeutic role in male and female sexual dysfunction. These investigations were sparked by findings that systemic administration of a synthetic analog of alpha-MSH, MT-II, causes penile erections in a variety of species, including humans. Several other melanocortinergic agents including HP-228, THIQ, and bremelanotide (PT-141) have since been shown to have erectogenic properties thought to be due to binding to melanocortin receptors in the central nervous system, particularly the hypothalamus. Bremelanotide, a nasally administered synthetic peptide, is the only melanocortinergic agent that has been clinically studied in both males and females. Data from Phase II clinical trials of bremelanotide support the use of melanocortin-based therapy for erectile dysfunction. Studies using animal models have demonstrated that pre-copulatory behaviors in female rats analogous to sexual arousal are evoked, and preliminary clinical data also suggest a role in promoting sexual desire and arousal in women. Based on bremelanotide clinical experience, administration of a melanocortin agonist is well tolerated and not associated the hypotension observed with phosphodiesterase-5 inhibitors currently used to treat erectile dysfunction. This review discusses investigations of melanocortin agonists for the treatment of sexual dysfunction with emphasis on proposed sites and mechanisms of action in the central nervous system that appear to be involved in melanocortinergic modulation of sexual function. Current research validates use of melanocortinergic agents for the treatment of both male and female sexual dysfunction.

2006-02-01·European Journal of Pharmacology3区 · 医学

The melanocortin peptide HP228 displays protective effects in acute models of inflammation and organ damage

3区 · 医学

Article

作者: Michele D'Amico ; Clara Di Filippo ; Mauro Perretti ; Stephen J. Getting

The clinically efficacious melanocortin peptide HP228 has here been investigated for its anti-inflammatory efficacy. In this study we have investigated the efficacy of HP228 in murine acute models of inflammation and myocardial ischaemia. Systemic treatment of mice with HP228 inhibited neutrophil accumulation in zymosan; urate crystal and carrageenan induced inflammatory models. In the urate model this was due to inhibition of pro-inflammatory chemokines and cytokines, whilst different mechanisms exist for zymosan peritonitis and carrageenan-induced air-pouch inflammation. HP228 was next evaluated in a model of myocardial ischaemia, another condition where cytokines and neutrophils are thought to play a causal role. HP228 caused a 50% reduction in myocardial damage following reperfusion. HP228 therefore inhibits the most important facet of the host inflammatory response namely leukocyte migration. These data show for the first time that the clinically efficacious peptide HP228 displays protective effects in models of inflammation and organ damage.

2006-02-01·Peptides3区 · 医学

Cardiovascular responses to melanocortin 4-receptor stimulation in conscious unrestrained normotensive rats

3区 · 医学

Article

作者: Janet R. Nicholson ; Ulrich Nordheim ; Karl G. Hofbauer ; Patrick Dunant ; Karol Dokladny

In the present studies, we used a non-selective melanocortin MC3/4 receptor agonist (HP228) and a novel selective melanocortin MC4 receptor (MC4-R) agonist (MK-cpd1) to study the cardiovascular, temperature, locomotor and feeding responses to melanocortin receptor stimulation in comparison to sibutramine in rats instrumented with a telemetry transmitter. Moreover, norepinephrine turnover rates in heart and brown adipose tissue were determined. HP228 (1, 3 and 10mg/kg, i.p.) reduced 24h food intake dose-dependently and increased heart rate and mean arterial pressure (maximal differences: +60+/-8beats/min and +8+/-1mmHg, means+/-S.E.M., p<0.001 and p<0.01, respectively). After 10mg/kg HP228 showed a three-fold increase in norepinephrine turnover in the heart. The selective MC4-R agonist MK-cpd1 tended to decrease 24h food intake only at the highest dose tested (10mg/kg, i.p., p=0.06) and increased both heart rate (+17+/-4 and +22+/-5beats/min at 3 and 10mg/kg, p<0.01) and mean arterial pressure (+4+/-1mmHg at 10mg/kg, p<0.05). Sibutramine reduced food intake at all doses tested (1, 3 and 10mg/kg, i.p.). It did not change mean arterial pressure significantly, and increased heart rate only at the highest dose tested (+36+/-6beats/min, p<0.05). If also observed in humans, the pharmacological profile of MC4-R agonists would not offer a significant therapeutic advantage over currently used appetite suppressants such as sibutramine.

100 项与 HP-228 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
哮喘	临床2期	美国	-	-
化疗引起的损伤	临床2期	美国	-	-
2型糖尿病	临床2期	-	Sygnis Bioscience GmbH & Co KG	-
2型糖尿病	临床2期	美国	-	-
炎症	临床2期	-	Sygnis Bioscience GmbH & Co KG	-
炎症	临床2期	美国	-	-
肥胖	临床2期	美国	-	-
肥胖	临床2期	-	Sygnis Bioscience GmbH & Co KG	-
术后疼痛	临床2期	-	Sygnis Bioscience GmbH & Co KG	-
术后疼痛	临床2期	美国	-	-