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疾病领域	数量

神经系统疾病	1

排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

δ opioid receptor x κ opioid receptor x μ opioid receptor	1

关联

13

项与 Enhance Biotech, Inc. 相关的药物

DPI-125

靶点

δ opioid receptor x κ opioid receptor x μ opioid receptor

作用机制

δ opioid receptor激动剂 [+2]

在研机构

DMK Pharmaceuticals Corp. [+2]

原研机构

Enhance Biotech, Inc.

在研适应症

阿片相关性障碍 [+1]

非在研适应症-

最高研发阶段临床1期

首次获批国家/地区-

首次获批日期-

LIF-316

靶点-

作用机制-

在研机构-

原研机构

Enhance Biotech, Inc.

在研适应症-

非在研适应症

不孕

最高研发阶段终止

首次获批国家/地区-

首次获批日期-

LI-316b

靶点-

作用机制-

在研机构-

原研机构

Enhance Biotech, Inc.

在研适应症-

非在研适应症

男性不育症

最高研发阶段终止

首次获批国家/地区-

首次获批日期-

100 项与 Enhance Biotech, Inc. 相关的临床结果

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0 项与 Enhance Biotech, Inc. 相关的专利（医药）

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6

项与 Enhance Biotech, Inc. 相关的文献（医药）

2006-01-01·Journal of Pharmacology and Experimental Therapeutics3区 · 医学

ARD-353 [4-((2R,5S)-4-(R)-(4-Diethylcarbamoylphenyl)(3-hydroxyphenyl)methyl)-2,5-dimethylpiperazin-1-ylmethyl)benzoic Acid], A Novel Nonpeptide δ Receptor Agonist, Reduces Myocardial Infarct Size without Central Effects

3区 · 医学

Article

作者: Chang, Kwen-Jen ; Wei, Ke ; O'Neill, Scott J. ; Watson, Michael J. ; Holt, Jonathon D. S. ; Gengo, Peter J. ; Gross, Garrett J. ; Pendergast, William

A novel delta-receptor selective compound, ARD-353 [4-((2R,5S)-4-(R)-(4-diethylcarbamoylphenyl)(3-hydroxyphenyl)methyl)-2, 5-dimethylpiperazin-1-ylmethyl)benzoic acid], was evaluated for activity on infarct size in a rat model of acute myocardial infarction. ARD-353 was characterized as having delta receptor selectivity using radioligand binding and had no apparent selectivity between delta receptor subtypes as determined by [(3)H] cyclic [D-Pen(2),D-Pen(5)]enkephalin (delta(1)) and [(3)H]Deltorphin II (delta(2)) competition binding. ARD-353 also showed selective delta receptor agonist activity in mouse-isolated vas deferens. There was no evidence of any seizure-like convulsions when ARD-353 was administered to mice either i.v. or p.o., implying minimal penetration of the blood-brain barrier. ARD-353 decreased infarct size in a left anterior descending coronary artery (LAD) occlusion model of myocardial infarction. In animals pretreated with ARD-353 (i.v.) and then subjected to 30 min of LAD occlusion followed by 90 min of reperfusion, infarct size was reduced in a dose-dependent manner compared with vehicle-treated controls. The effects of ARD-353 on infarct size were blocked by the delta(1)-opioid selective antagonist 7-benzylidenenaltrexone, indicating a significant role for the delta(1)-opioid receptor in the cardioprotective mechanism of ARD-353. ARD-353 (0.3 mg/kg i.v.) produced significant protection when administered 5 min and 12 and 48 h before ischemic insult or when given immediately after the ischemic insult (at the start of reperfusion). Given the lack of central nervous system effects and beneficial efficacy in the rat model of myocardial ischemia, it is felt that ARD-353 is the first nonpeptide delta-receptor agonist with true potential for clinical use before surgically induced ischemia or in an emergency setting.

2005-11-01·Journal of Pharmacology and Experimental Therapeutics3区 · 医学

DPI-221 [4-((α-S)-α-((2S,5R)-2,5-Dimethyl-4-(3-fluorobenzyl)-1-piperazinyl)benzyl)-N,N-diethylbenzamide]: A Novel Nonpeptide δ Receptor Agonist Producing Increased Micturition Interval in Normal Rats

3区 · 医学

Article

作者: Chang, Kwen-Jen ; Holt, Jonathon D. S. ; Pendergast, William ; O'Neill, Scott J. ; Wei, Ke ; Gengo, Peter J. ; Chang, Jane P. ; Watson, Michael J.

There is a wealth of information from animal models and clinical opioid-analgesic use that indicates a significant role for opioid receptors in the modulation of bladder activity. The novel benzhydrylpiperazine compound DPI-221 [4-((alpha-S)-alpha-((2S,5R)-2,5-dimethyl-4-(3-fluorobenzyl)-1-piperazinyl)benzyl)-N,N-diethylbenzamide] was characterized as having delta receptor selectivity using radioligand binding (K(i) = 2.0 +/- 0.7 nM, delta receptor; 1800 +/- 360 nM, mu receptor; and 2300 +/- 680 nM, kappa receptor), and agonist activity was demonstrated in the mouse isolated vas deferens where DPI-221 inhibited electrically induced contractions with an IC(50) value of 88 +/- 7.5 nM. In the guinea pig isolated ileum, DPI-221 had no effect on electrically induced contractions at concentrations as high as 1 microM. Sterile saline was infused (7 ml/h) into the bladder of Sprague-Dawley rats, via a transmural catheter; DPI-221 (1.0 to 20 mg/kg p.o.) significantly increased the interval between micturition events, whereas peak void pressure was not significantly decreased by any dose of DPI-221. The micturition effects of 10 mg/kg p.o. DPI-221 were blocked by naltrindole, indicating a delta receptor mechanism of action. In isolated rat bladder strips, DPI-221 was ineffective at relaxing detrusor muscle precontracted with carbachol. The most crucial safety aspect of delta agonist administration is the incidence of seizure-like convulsions in rodents. DPI-221 produced no convulsions at doses up to 100 mg/kg p.o. in mice, although rapid bolus i.v. injection of 5 mg/kg produced convulsions in 3% of mice tested. These findings indicate a good safety profile for DPI-221 administered orally, with potent efficacy in modifying bladder activity.

2003-12-01·Journal of Pharmacology and Experimental Therapeutics3区 · 医学

DPI-3290 [(+)-3-((α-R)-α-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-(3-fluorophenyl)-N-methylbenzamide]. II. A Mixed Opioid Agonist with Potent Antinociceptive Activity and Limited Effects on Respiratory Function

3区 · 医学

Article

作者: O'Neill, Scott J. ; McNutt, Robert ; Su, Ying Fu ; Pettit, Hugh O. ; Chang, Kwen-jen ; Gengo, Peter J.

Allyl-2,5-dimethyl-1-piperazines have been of interest as analgesic agents for the management of moderate-to-severe pain. In this study, we compared the antinociceptive properties and respiratory depressant activity of one such agent, (+)-3-((alpha-R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-(3-fluorophenyl)-N-methylbenzamide (DPI-3290), with those of established narcotic analgesics, morphine and fentanyl. Intravenous administration of DPI-3290 in conscious laboratory rats increased antinociception in a dose-dependent manner with a corresponding ED(50) value of 0.05 +/- 0.0072 mg/kg. Simultaneous measurement of arterial blood gas in animals treated with DPI-3290 demonstrated dose-dependent increases in pCO2 with an ED(50) value of 0.91 +/- 0.22 mg/kg. In comparison, morphine and fentanyl increased antinociception in rats with ED(50) values of 2.01 +/- 0.0005 and 0.0034 +/- 0.00024 mg/kg, respectively, and the ED(50) value for morphine-induced changes in pCO2 was 4.23 +/- 0.72 mg/kg, whereas the ED(50) value for fentanyl-induced changes in pCO2 was 0.0127 +/- 0.0035 mg/kg. A separate series of experiments were designed to examine the effects of DPI-3290 on mu-opioid receptor induced antinociception and hypercapnia. Intravenous bolus doses of DPI-3290 that ranged from 0.2 to 1.0 mg/kg had no effect on antinociception mediated by alfentanil (2 microg/kg/min i.v.) but reduced hypercapnia by approximately 50%. Results from these studies demonstrate the equivalent antinociceptive efficacy of DPI-3290, morphine, and fentanyl but dramatic differences in the hypercapnia that antinociceptive doses of these drugs produce. When measured simultaneously, DPI-3290 had an 18.2-fold difference in the ratio comparing the ED(50) value for antinociception with the ED(50) value for changes in pCO2; this ratio was 2.1 for morphine and 3.7 for fentanyl. Furthermore, DPI-3290 reduced the alfentanil-mediated hypercapnia without any effect on antinociception. Together, the balanced opioid agonist activity of DPI-3290 may provide a means of powerful analgesia while mitigating the mu-opioid receptor-mediated hypercapnia.

100 项与 Enhance Biotech, Inc. 相关的药物交易

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100 项与 Enhance Biotech, Inc. 相关的转化医学

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临床1期

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当前项目

药物(靶点)	适应症	全球最高研发状态

DPI-125 ( δ opioid receptor x κ opioid receptor x μ opioid receptor )	疼痛更多	临床1期
BIO-236	鼻唇沟皱纹更多	终止
LI-313	银屑病更多	终止
Org-41793 ( δ opioid receptor x μ opioid receptor )	术后疼痛更多	终止
LIF-316	不孕更多	终止