CN1500483A - Novel use of phencynonate hydrochloride - Google Patents
Novel use of phencynonate hydrochloride Download PDFInfo
- Publication number
- CN1500483A CN1500483A CNA021489335A CN02148933A CN1500483A CN 1500483 A CN1500483 A CN 1500483A CN A021489335 A CNA021489335 A CN A021489335A CN 02148933 A CN02148933 A CN 02148933A CN 1500483 A CN1500483 A CN 1500483A
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- CN
- China
- Prior art keywords
- benzene ring
- nonyl ester
- ring nonyl
- epilepsy
- mice
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
The present invention relates to the new use of phencynonate hydrochloride in medicine preparing field, and especially the effect of the compound in treating and remitting epilepsy.
Description
Invention field
The present invention relates to benzene ring nonyl ester is used for the treatment of or alleviates purposes in the antiepileptic in preparation.
Background technology
Benzene ring nonyl ester, system name 2-phenyl-2-cyclopenta-2-hydroxyacetic acid-3-methyl-3-azabicyclo (3,3, the 1) ninth of the ten Heavenly Stems-9 α-ester hydrochloride, structural formula is
Chinese patent application 97125424.9 and Chinese patent application 93119491.1 disclose its preparation method and as the purposes of anti-kinetosis (carsickness, ship, machine etc.) medicine.
Epilepsy is one of modal nervous system disease, it is characterized in that because different clinical and electroencephalogram performances is followed in the caused repeatability outbreak of the unexpected over-discharge of brain cell.The whole world has 5,000 ten thousand people to suffer from epilepsy approximately at present, wherein has at least 20-30% when epilepsy existing medicine to be had Drug resistance.Although existing a large amount of antiepileptics listing, often curative effect is relatively poor or bigger side effect is arranged in the face of various types of epilepsies, and therefore, the antiepileptic of exploitation new role type has broad application prospects and huge market value.
Goal of the invention
The medicine that the purpose of this invention is to provide treatment or alleviation epilepsy.
The invention summary
The inventor has now found that the effectively generation of Taking Control of Epilepsy of benzene ring nonyl ester.Therefore, the present invention relates to benzene ring nonyl ester is used for the treatment of or alleviates purposes in the epilepsy medicine in preparation.
The invention still further relates to the method for treatment or alleviation epilepsy, comprise that the benzene ring nonyl ester with effective dose gives required patient.
The invention still further relates to the pharmaceutical composition that is used for the treatment of or alleviates epilepsy, it comprises benzene ring nonyl ester and pharmaceutical carrier or excipient.
Detailed Description Of The Invention
The following examples are used for describing in detail the present invention, but are not limited to the present invention.
Embodiment 1. mice maximal electroshocks outbreaks model is the experimental model of the epilepsy grand mal of generally acknowledging.Concrete grammar is as follows:
Kunming mice, body weight 20 ± 2mg, ♂, ♀ half and half, random packet, every group of 10 animals.At first dentation is pressed from both sides electrode and soak normal saline, be sandwiched in mice two ears respectively, pass to varying strength electric current (mA) then, with mice produce THE and flexing then the twin person of battle array be MES, thereby the current intensity of determining 97% above mice generation MES is 8.02mA.
On the basis of above-mentioned experiment, 0.5h ip injection various dose (2,5,10,20,40) mgkg before experiment
-1Benzene ring nonyl ester.The result shows that the anti-MES effect of benzene ring nonyl ester is along with the increase of dosage obviously strengthens ED
50Value is 6.80.See normal saline group in contrast simultaneously, obvious MES all appears in 10 animals, illustrates that adopting 8.02mA is reliable as the current intensity of observing the anti-MES effect of medicine.
The antagonism of table 1. benzene ring nonyl ester on mice MES
Convulsions number of animals (only) percentage rate (%) ED does not take place in dosage number of animals (only)
50
40 10 10 100
20 10 7 70
10 10 6 60 6.80
5 10 4 40
2 10 2 20
As seen from Table 1, benzene ring nonyl ester can fine antagonism MES.
Embodiment 2. on the model (MET) of fainting from fear due to the mice pentetrazole, the antagonism of benzene ring nonyl ester.
Mice MET observes the experimental animal model that epilepsy petit mal curative effect of medication is generally acknowledged, concrete grammar is as follows:
Kunming mice, body weight 20 ± 2mg, ♂, ♀ half and half, random packet, every group of 10 animals.Sc injects pentylenetetrazole, the twin property convulsions of battle array occurs with animal in the 30min, and continuing was whole index more than 3 seconds, determines that it is 92.1mgkg that 97% above animal produces the pentetrazole dose value of fainting from fear
-1
On the basis of above-mentioned experiment, 0.5h ip injection various dose (4,8,10,16,20) mgkg before experiment
-1Benzene ring nonyl ester.The result shows that the anti-MET effect of benzene ring nonyl ester is along with the increase of dosage obviously strengthens ED
50Value is 9.07.See normal saline group in contrast simultaneously, obvious convulsions all appears in 10 animals, illustrates to adopt 92.1mgkg
-1Pentetrazole (sc injection) is reliable as the dosage of observing the anti-MET effect of medicine.
The antagonism of table 2. benzene ring nonyl ester on the MET model
Dosage number of animals number of animals percentage rate (%) ED that faints from fear
50
(mg/kg) (only) (only)
20 10 9 90
16 10 6 60
10 10 5 50 9.07
8 10 5 50
4 10 2 4
As seen from Table 2, benzene ring nonyl ester can fine antagonism MET.
Above-mentioned two animal models prove that benzene ring nonyl ester all has tangible anticonvulsant action on the experimental animal model of the epilepsy grand mal of generally acknowledging, petit mal, therefore show that the present invention has tangible antiepileptic action.
Claims (1)
1. the benzene ring nonyl ester shown in the following formula is in preparation treatment or alleviation epilepsy
Medicine in application.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB021489335A CN1189173C (en) | 2002-11-12 | 2002-11-12 | Novel use of phencynonate hydrochloride |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB021489335A CN1189173C (en) | 2002-11-12 | 2002-11-12 | Novel use of phencynonate hydrochloride |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1500483A true CN1500483A (en) | 2004-06-02 |
| CN1189173C CN1189173C (en) | 2005-02-16 |
Family
ID=34233403
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB021489335A Expired - Fee Related CN1189173C (en) | 2002-11-12 | 2002-11-12 | Novel use of phencynonate hydrochloride |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1189173C (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008086678A2 (en) * | 2006-12-30 | 2008-07-24 | Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China | The medical use of levo-phencynonate as neuroprotective agent |
| CN102836432A (en) * | 2011-06-22 | 2012-12-26 | 伍丽娟 | Nasal preparation for treating epilepsy |
-
2002
- 2002-11-12 CN CNB021489335A patent/CN1189173C/en not_active Expired - Fee Related
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008086678A2 (en) * | 2006-12-30 | 2008-07-24 | Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China | The medical use of levo-phencynonate as neuroprotective agent |
| WO2008086678A3 (en) * | 2006-12-30 | 2008-09-04 | Inst Pharm & Toxicology Amms | The medical use of levo-phencynonate as neuroprotective agent |
| CN102836432A (en) * | 2011-06-22 | 2012-12-26 | 伍丽娟 | Nasal preparation for treating epilepsy |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1189173C (en) | 2005-02-16 |
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| C14 | Grant of patent or utility model | ||
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| CF01 | Termination of patent right due to non-payment of annual fee |