JP2002284683A - Appetite suppressant - Google Patents
Appetite suppressantInfo
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- JP2002284683A JP2002284683A JP2001088087A JP2001088087A JP2002284683A JP 2002284683 A JP2002284683 A JP 2002284683A JP 2001088087 A JP2001088087 A JP 2001088087A JP 2001088087 A JP2001088087 A JP 2001088087A JP 2002284683 A JP2002284683 A JP 2002284683A
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- JP
- Japan
- Prior art keywords
- pipecolic acid
- appetite
- acid
- administration
- effect
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- Hydrogenated Pyridines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【0001】[0001]
【発明の属する技術分野】本発明は、食欲抑制作用また
は食欲減退作用を有する薬剤に関し、さらに詳しくはピ
ペコリン酸またはその酸付加塩を有効成分とする食欲抑
制剤に関する。TECHNICAL FIELD The present invention relates to a drug having an appetite-suppressing or appetite-reducing action, and more particularly to an appetite suppressant containing pipecolic acid or an acid addition salt thereof as an active ingredient.
【0002】[0002]
【従来の技術】近年、食料事情が良くなり、生活が向上
するにつれて、あるいは精神的なストレスが原因となっ
て肥満症が増加する傾向にある。肥満は、体構成に占め
る脂肪組織量が異常に増加した状態のことで、成人病の
誘因となり、糖尿病、高血圧、高脂血症、冠状動脈硬化
症(狭心症、心筋梗塞)、通風、胆石症、脂肪肝、不妊
症や変形性関節症などが合併しやすくなる。2. Description of the Related Art In recent years, obesity has tended to increase as food conditions have improved and living has improved, or due to mental stress. Obesity is a condition in which the amount of adipose tissue occupying the body is abnormally increased, and is a cause of adult illness. Gallstone disease, fatty liver, infertility, osteoarthritis, etc. are likely to be complicated.
【0003】肥満症には食欲の異常な亢進による調節性
肥満症と食べ方とは関係なく代謝に異常があって脂肪の
中で増殖が起こる代謝性肥満症の二つに分類される。肥
満治療の基本は食事療法と運動療法の併用であるが、こ
れには限界があり、特に高度肥満症に対しては薬物療法
が有効であると期待されている。[0003] Obesity is classified into two types: regulatory obesity due to abnormally high appetite and metabolic obesity in which there is an abnormality in metabolism irrespective of eating style and proliferation occurs in fat. The basis of obesity treatment is a combination of diet and exercise therapy, but this has limitations, and pharmacotherapy is expected to be particularly effective for severe obesity.
【0004】食欲抑制または食欲減退作用を有する薬物
としては、アンフェタミン系の薬物(覚醒剤)が最もそ
の作用の強いことで知られているが、これらは中枢興奮
剤に属すもので、覚醒作用と同時に興奮作用も発現する
ので使用に際しては慎重さを要する。同様に覚醒作用の
あるカフィロンや交感神経作用薬で中枢作用によって食
欲を抑制する薬物として、フェンフルラミン、マジンド
ール、フェンテルミン等が知られているが、いずれも効
果および副作用の点で十分とはいえない。[0004] Amphetamine-based drugs (stimulants) are known to have the strongest action as drugs having an appetite suppressing or reducing appetite, but they belong to central stimulants, Care must be taken when using it because it also produces an excitatory effect. Similarly, fenfluramine, mazindol, phentermine, and the like are known as cafilon and sympathomimetics that have awakening effects and suppress appetite by central action, but none of them are sufficient in terms of effect and side effects. I can't say.
【0005】[0005]
【発明が解決しようとする課題】本発明は、毒性が低
く、副作用の少ない新しいタイプの食欲抑制または食欲
減退作用を有する薬剤を提供することを目的としてい
る。SUMMARY OF THE INVENTION An object of the present invention is to provide a new type of a drug having an appetite suppressing or reducing appetite with low toxicity and few side effects.
【0006】[0006]
【課題を解決するための手段】本発明者は上記目的を達
成すべく鋭意研究を行った結果、アミノ酸の一種である
リジンのアナログで、下記構造式にて表されるピペコリ
ン酸のラセミ体、光学活性体及びその酸付加塩が優れた
食欲抑制作用または食欲減退作用を有することを見出し
て、本発明を完成するに至った。Means for Solving the Problems The present inventors have made intensive studies to achieve the above object, and as a result, a racemic form of pipecolic acid represented by the following structural formula, which is an analog of lysine which is a kind of amino acid, The present inventors have found that the optically active substance and its acid addition salt have an excellent appetite suppressing or appetite-reducing action, and have completed the present invention.
【0007】[0007]
【化1】 Embedded image
【0008】すなわち、本発明はピペコリン酸またはそ
の医薬的に許容しうる塩を有効成分とする食欲抑制剤で
ある。[0008] That is, the present invention is an appetite suppressant comprising pipecolic acid or a pharmaceutically acceptable salt thereof as an active ingredient.
【0009】[0009]
【発明の実施の形態】本発明に係るピペコリン酸のL−
体は植物に広く存在するが、光学活性体およびラセミ体
を問わず、いずれも公知方法、例えば[Fujii,M
iyoshi,Bull.Chem.Soc.Japa
n 48,1341(1975)]、[R.T.Shu
man et al.,J.Org.Chem.55,7
38(1990)]に記載の方法により製造することが
できる。BEST MODE FOR CARRYING OUT THE INVENTION L-Pipecolic acid according to the present invention
Although the body exists widely in plants, both optically active and racemic forms are known in the art, for example [Fujii, M.
iyoshi, Bull. Chem. Soc. Japan
n 48, 1341 (1975)], [R. T. Shu
man et al. , J. et al. Org. Chem. 55 , 7
38 (1990)].
【0010】本発明の有効成分であるピペコリン酸はラ
セミ体、L体、D体のいずれも使用可能であるが、特に
L体が好ましい。The active ingredient of the present invention, pipecolic acid, may be any of racemic, L-form and D-form, but L-form is particularly preferred.
【0011】ピペコリン酸の医薬的に許容される塩とし
ては、塩酸、硫酸、リン酸等の無機酸との塩、酢酸、乳
酸、リンゴ酸、酒石酸、フマール酸、マレイン酸、メタ
ンスルホン酸等の有機酸との塩が挙げられ、好ましくは
塩酸塩、乳酸塩、リンゴ酸塩、酒石酸塩である。The pharmaceutically acceptable salts of pipecolic acid include salts with inorganic acids such as hydrochloric acid, sulfuric acid and phosphoric acid, acetic acid, lactic acid, malic acid, tartaric acid, fumaric acid, maleic acid, methanesulfonic acid and the like. Examples include salts with organic acids, preferably hydrochloride, lactate, malate and tartrate.
【0012】ピペコリン酸またはその酸付加塩の薬理作
用については、抑制性の神経伝達物質であるGABAの
放出を高め、取り込みを抑えることが知られているが、
食欲抑制作用または食欲減退作用を有することは従来全
く知られておらず、本発明者によって初めて究明された
ものである。特筆すべきことは、後記試験例から明らか
なように、ピペコリン酸については、光学活性D−体も
L−体と同様の食欲抑制作用を有すること、そして前駆
体のリジンと比較した場合、投与量において有意な差が
認められることである。L−体のラットに対する急性毒
性は200mg/kgをc.p.(腹腔内投与)しても死
亡率が0%と低く、極めて安全な化合物と言える。With respect to the pharmacological action of pipecolic acid or an acid addition salt thereof, it is known that the release of GABA which is an inhibitory neurotransmitter is increased and the uptake is suppressed.
It has never been known to have an appetite-suppressing action or an appetite-reducing action, and was first found by the present inventors. It should be noted that, as apparent from the test examples described below, pipecolic acid has an appetite-suppressing effect similar to that of the L-form, and administration of pipecolic acid when compared with the precursor lysine. A significant difference in the amount is observed. The acute toxicity of L-isomer to rats is as low as 0% even at 200 mg / kg c.p. (intraperitoneal administration), indicating that it is a very safe compound.
【0013】ピペコリン酸またはその塩を食欲抑制止剤
として用いる場合、単独または薬剤として許容しうる固
体担体又は液体担体で希釈して投与される。好ましい製
剤形態や投与形態は、患者の年令、性別、体重、症状の
程度、処置時期等に応じて適宜決定される。When pipecolic acid or a salt thereof is used as an appetite suppressant, it is administered alone or diluted with a pharmaceutically acceptable solid or liquid carrier. The preferred preparation form and administration form are appropriately determined according to the age, sex, weight, degree of symptoms, treatment time, etc. of the patient.
【0014】治療量は一般に、非経口投与で5〜100
mg/kg・日、経口投与で100〜1000mg/k
g・日であって、1日1回〜3回投与可能である。経口
投与する場合は、錠剤、カプセル剤、粉剤、顆粒剤、液
剤、エリキシル剤等の形態で、また、非経口投与の場
合、液体の殺菌した状態の形態で用いられる。Therapeutic doses are generally between 5 and 100 for parenteral administration.
mg / kg-day, 100-1000 mg / k by oral administration
g.day, and can be administered once to three times a day. For oral administration, it is used in the form of tablets, capsules, powders, granules, liquids, elixirs and the like, and for parenteral administration, it is used in the form of a sterile liquid.
【0015】固体担体の例としては、通常ゼラチンタイ
プのカプセルが用いられる。賦形剤としては、ゼラチ
ン:乳糖、グルコース、マンニット、キシリトール、エ
リスリトール等の糖類:コーン、小麦、米、とうもろこ
し澱粉等の澱粉類:ステアリン酸等の脂肪酸:ステアリ
ン酸カルシウム、ステアリン酸マグネシウム等の脂肪酸
塩:炭酸ナトリウム:リン酸水素ナトリウム:タルク:
植物油:ステアリルアルコール等のアルコール:ガム:
ポリアルキレングリコール等が挙げられる。As an example of a solid carrier, a gelatin type capsule is usually used. As an excipient, gelatin: sugars such as lactose, glucose, mannitol, xylitol and erythritol: starches such as corn, wheat, rice and corn starch: fatty acids such as stearic acid: fatty acids such as calcium stearate and magnesium stearate Salt: sodium carbonate: sodium hydrogen phosphate: talc:
Vegetable oil: alcohol such as stearyl alcohol: gum:
And polyalkylene glycol.
【0016】これらのカプセル、錠剤、顆粒、粉末は、
一般的に10〜90重量%、好ましくは30〜70重量
%のピペコリン酸化合物を有効成分として含む。液状担
体としては、一般に水、生理食塩水、テキストロースま
たは類似の糖類溶液、エチレングリコール、プロピレン
グリコール、ポリエチレングリコール等のグリコール類
が好ましい。These capsules, tablets, granules and powders are
It generally contains 10 to 90% by weight, preferably 30 to 70% by weight, of a pipecolic acid compound as an active ingredient. As the liquid carrier, water, physiological saline, textrose or a similar saccharide solution, and glycols such as ethylene glycol, propylene glycol, and polyethylene glycol are generally preferred.
【0017】非経口的に筋肉内注射、静脈内注射、皮下
注射で投与する場合、食塩またはグルコース等の他の溶
質を添加した無菌溶液として使用される。注射用の適当
な溶剤としては、減菌水、塩酸リドカイン溶液(筋肉内
注射用)、生理食塩水、ブドウ糖、静脈内注射用液体、
電解質溶液(静脈内注射用)等が挙げられる。これらの
注射液の場合には、通常1〜50重量%、好ましくは1
〜25重量%の有効成分を含むようにすることがよい。When administered parenterally by intramuscular injection, intravenous injection, or subcutaneous injection, it is used as a sterile solution to which other solutes such as salt or glucose are added. Suitable solvents for injection include sterile water, lidocaine hydrochloride solution (for intramuscular injection), physiological saline, glucose, liquid for intravenous injection,
Electrolyte solution (for intravenous injection) and the like. In the case of these injections, usually 1 to 50% by weight, preferably 1% by weight.
It may be desirable to include 〜25% by weight of the active ingredient.
【0018】経口投与の液剤の場合、10〜90重量%
の有効成分を含む懸濁液またはシロップがよい。In the case of a liquid preparation for oral administration, 10 to 90% by weight
Suspension or syrup containing the active ingredient is preferred.
【0019】次いで、本発明の実施例を挙げて具体的に
説明するが、本発明は何らこれら実施例によって限定さ
れるものではない。Next, the present invention will be described specifically with reference to examples, but the present invention is not limited to these examples.
【0020】[0020]
【実施例】<製剤例1>エリスリトール54g、コーン
スターチ45gを十分に混合し、これに水20gに1g
のL−ピペコリン酸を溶かした水溶液を加え、造粒、乾
燥後、32号ふるいにかけて1%含有の散剤とした。EXAMPLES <Formulation Example 1> 54 g of erythritol and 45 g of corn starch were thoroughly mixed, and 1 g of this was added to 20 g of water.
Of L-pipecolic acid was added, granulated and dried, and then passed through a No. 32 sieve to obtain a powder containing 1%.
【0021】<製剤例2>グルコース51g、コーンス
ターチ34g、タルク10gおよびリン酸水素ナトリウ
ム3gを十分に混合し、次いで水20gに1gのL−ピ
ペコリン酸を溶かした水溶液を加え、造粒、乾燥後整粒
した。これに滑沢剤ステアリン酸マグネシウム1gを加
えて混合後、常法により1錠100mgの錠剤とした。<Preparation Example 2> 51 g of glucose, 34 g of corn starch, 10 g of talc and 3 g of sodium hydrogen phosphate are sufficiently mixed, and then an aqueous solution obtained by dissolving 1 g of L-pipecolic acid in 20 g of water is added, followed by granulation and drying. It was sized. 1 g of a magnesium stearate lubricant was added to the mixture, mixed, and then made into a tablet of 100 mg per tablet by a conventional method.
【0022】[食欲抑制試験] 実験例1〜4における供試動物と供試飼料:Cobb系
統のプロイラー雄ヒナ2日齢を別個に飼育した。実験に
供試した羽数nは、図1〜4中に記した。[Appetite Suppression Test] Test animals and test feed in Experimental Examples 1 to 4: Cobb strain broiler male chicks, 2 days old, were separately raised. The number n of wings used in the experiment is shown in FIGS.
【0023】給与した飼料は市販の飼料(豊橋飼料「H
i−ヘルス餌AX SAFETY」商品名)を用いた。The feed fed was a commercial feed (Toyohashi Feed “H
i-Health Bait AX SAFETY (trade name) was used.
【0024】溶液の投与方法:ヒナの脳室への投与は、
アクリル製の脳定位固定装置とハミルトンのマイクロシ
リンジを用いて行った(Davis,J.L.,Mas
uoka,D.T.,Gerbrandt,J.F.,
Cherkin,A.,1979.Autoradio
graphic distribution of L−
prolinein chicks after int
racerebral injection.Phys
iol.Behav.22,693〜695)。経口投
与は、1mlシリンジ(テルモ株式会社製)の先にビニ
ールホースを装着し、咽頭を介してそ嚢内にその先端を
挿入して行った。Method of administration of the solution: Administration of the chick to the ventricle
This was performed using an acrylic stereotaxic apparatus and a Hamilton microsyringe (Davis, JL, Mas).
Uoka, D .; T. , Gerbrandt, J .; F. ,
Cherkin, A .; 1979. Autoradio
graphic distribution of L-
prolinein chickens after int
raceebral injection. Phys
iol. Behav. 22, 693-695). Oral administration was performed by attaching a vinyl hose to the tip of a 1 ml syringe (manufactured by Terumo Corporation) and inserting the tip into the capsule through the pharynx.
【0025】試験例1:L−ピペコリン酸の脳室投与が
ヒナの飼料摂取量に及ぼす影響 ヒナを3時間絶食させ、その間水だけを自由に与えた。
L−ピペコリン酸を0.1%のエバンスブルーを含む
0.85%生理食塩水に0.5mgと1.0mgの2水
準で溶解させ、ヒナの脳室に投与し、その後30,60
および120分の飼料摂食量を調査した。コントロール
には0.1%のエバンスブルーを含む0.85%生理食
塩水を用い、1羽当たり10μl投与した。実験終了
後、ヒナを屠殺し、脳室内に色素が確認できない個体は
計算から除外した。Test Example 1: Effect of intraventricular administration of L-pipecolic acid on feed intake of chicks The chicks were fasted for 3 hours, during which time only water was given freely.
L-Pipecolic acid was dissolved in 0.85% saline containing 0.1% Evans blue at two levels of 0.5 mg and 1.0 mg, and administered to the chick ventricle.
And 120 minutes of food intake. As a control, 0.85% physiological saline containing 0.1% Evans blue was used, and 10 μl was administered per bird. At the end of the experiment, the chicks were sacrificed and individuals for which no pigment was found in the ventricle were excluded from the calculations.
【0026】結果は図1に示すようにL−ピペコリン酸
の1mg投与区で、飼料給与後30分においてコントロ
ール区に比して有意な飼料摂取量の抑制が観察された。
この効果は、60分後においても継続した。120分に
至るとその抑制が解除され始めるが、依然としてコント
ロール区に比して飼料摂取量は有意に低かった。しかし
ながら、L−ピペコリン酸の0.5mg投与区では、各
時間においてコントロール区との間に有意な差は認めら
れなかった。脳内においてL−リジンから産生されるL
−ピペコリン酸には、摂食行動を抑制する機能があるこ
とが判明した。As shown in FIG. 1, a significant suppression of feed intake was observed in the group administered with 1 mg of L-pipecolic acid 30 minutes after feeding the feed compared to the control group as shown in FIG.
This effect continued even after 60 minutes. At 120 minutes, the suppression began to be released, but the feed intake was still significantly lower than in the control group. However, in the 0.5 mg L-pipecolic acid administration group, no significant difference was observed at each time from the control group. L produced from L-lysine in the brain
-Pipecolic acid was found to have a function of suppressing feeding behavior.
【0027】試験例2:D−ピペコリン酸の脳室投与が
ヒナの飼料摂取量に及ぼす影響 栄養素として摂取したL−ピペコリン酸は消化管内微生
物によりD−ピペコリン酸にも代謝されることが知られ
ているので、試験例1においてL−ピペコリン酸の代り
にD−ピペコリン酸を投与した以外は同様の実験を行っ
た。すなわち、ヒナを3時間絶食させ、その間水だけを
自由に与えた。D−ピペコリン酸を0.1%のエバンス
ブルーを含む0.85%生理食塩水に0.5mgと1.
0mgの2水準で溶解させ、ヒナの脳室に投与し、その
後30,60および120分の飼料摂食量を調査した。
コントロールには0.1%のエバンスブルーを含む0.
85%生理食塩水を用い、1羽当たり10μl投与し
た。実験終了後、ヒナを屠殺し、脳室内に色素が確認で
きない個体は計算から除外した。結果を図2示すよう
に、L型と同様の効果がD型にもあることが判明した。Test Example 2: Effect of ventricular administration of D-pipecolic acid on feed intake of chicks It is known that L-pipecolic acid taken as a nutrient is also metabolized to D-pipecolic acid by microorganisms in the digestive tract. Therefore, the same experiment was performed except that D-pipecolic acid was administered instead of L-pipecolic acid in Test Example 1. That is, the chicks were fasted for 3 hours, during which time they were given only water. 0.5 mg of D-pipecolic acid in 0.85% saline containing 0.1% of Evans blue was added.
0 mg was dissolved at two levels and administered to the chick ventricle, after which the food intake for 30, 60 and 120 minutes was investigated.
Controls contain 0.1% Evans blue.
Using 85% physiological saline, 10 μl was administered per bird. At the end of the experiment, the chicks were sacrificed and individuals without pigment in the ventricle were excluded from the calculation. As shown in FIG. 2, it was found that the same effect as in the L type was also obtained in the D type.
【0028】試験例3(参考例):L−リジンモノ塩酸
塩の脳室投与がヒナの飼料摂取量に及ぼす影響 L−ピペコリン酸の前駆体であるL−リジンにおける効
果を確認するために同様の実験を行った。Test Example 3 (Reference Example): Influence of intraventricular administration of L-lysine monohydrochloride on feed intake of chicks To confirm the effect on L-lysine, a precursor of L-pipecolic acid, An experiment was performed.
【0029】すなわち、ヒナを3時間絶食させ、その間
水だけを自由に与えた。L−リジンモノ塩酸塩を0.1
%のエバンスブルーを含む0.85%生理食塩水に1m
g、2mgおよび4mgの3水準で溶解させ、ヒナの脳
室に投与し、その後30,60および120分の飼料摂
食量を調査した。コントロールには0.1%のエバンス
ブルーを含む0.85%生理食塩水を用い、1羽当たり
10μl投与した。実験終了後、ヒナを屠殺し、脳室内
に色素が確認できない個体は計算から除外した。That is, chicks were fasted for 3 hours, during which time they were given water only. 0.1 L-lysine monohydrochloride
1m in 0.85% saline containing 0.1% Evans Blue
g, 2 mg and 4 mg were dissolved and administered to the chick ventricle, after which the food intake at 30, 60 and 120 minutes was investigated. As a control, 0.85% physiological saline containing 0.1% Evans blue was used, and 10 μl was administered per bird. At the end of the experiment, the chicks were sacrificed and individuals for which no pigment was found in the ventricle were excluded from the calculations.
【0030】結果は図3に示すように、L−リジンでは
L−ピペコリン酸で効果が認められた1mgの投与で
は、摂食抑制は起こらず、抑制効果が発現するためには
さらに多くの量を必要とすることが分かる。As shown in FIG. 3, as shown in FIG. 3, administration of 1 mg at which L-lysine had an effect on L-lysine did not suppress food intake, but required a larger amount to achieve the effect. It turns out that it is necessary.
【0031】試験例4:L−ピペコリン酸とL−リジン
の経口投与がヒナの飼料摂取量に及ぼす影響 試験例1〜3の結果から、L−リジンはL−ピペコリン
酸に代謝されることで、脳内において摂食抑制作用を示
すことが明らかとなった。そこで、この効果が経口で摂
取した場合にも発現するか否かを明らかにするために本
実験を行った。本実験では、L−リジンとL−ピペコリ
ン酸の吸収を考慮し、経口投与の30分後から飼料の投
与を開始した。Test Example 4: Effect of oral administration of L-pipecolic acid and L-lysine on feed intake of chicks From the results of Test Examples 1 to 3, L-lysine is metabolized to L-pipecolic acid. In addition, it was revealed that the substance had an antifeeding effect in the brain. Therefore, the present experiment was performed to clarify whether or not this effect is exhibited even when taken orally. In this experiment, the administration of the feed was started 30 minutes after oral administration in consideration of the absorption of L-lysine and L-pipecolic acid.
【0032】すなわち、ヒナを3時間絶食させ、その間
水だけを自由に与えた。その後、ヒナを7群に分け、1
群には経口で生理的食塩水1mlを対照として投与し
た。他の6群は、L−ピペコリン酸またはL−リジンを
それぞれ生理的食塩水1mlに0.1,0.2および
0.4ミリモル溶解し投与した。その30分後から飼料
給与を開始し、30,60および120分後の飼料摂取
量を調査した。That is, the chicks were fasted for 3 hours, and only water was freely given during that time. After that, the chicks were divided into 7 groups,
The group was orally administered 1 ml of physiological saline as a control. The other six groups were administered with L-pipecolic acid or L-lysine dissolved in 1 ml of physiological saline in 0.1, 0.2 and 0.4 mmol, respectively. Feeding was started 30 minutes after that, and the feed intake at 30, 60 and 120 minutes was investigated.
【0033】結果は図4に示すように、飼料投与後30
分と60分の試料摂取量に有意な差は検出されなかった
が、120分における摂食量は、L−ピペコリン酸0.
4ミリモルの区で他の投与区に比して有意に低下した。
これに対し、等量のL−リジンには効果は認められなか
ったことから、L−ピペコリン酸の摂食抑制効果は、経
口投与でも有効であることが判明した。The results are shown in FIG.
No significant difference was detected between the sample intakes of the L-pipecolic acid and L-pipecolic acid at 120 minutes.
The value was significantly reduced in the 4 mmol group as compared with the other administration groups.
On the other hand, since no effect was observed with an equivalent amount of L-lysine, it was found that the effect of L-pipecolic acid on food intake was also effective by oral administration.
【0034】試験例5:マウスの飼料摂取量に対するL
−およびD−ピペコリン酸の経口投与の効果: 8週齢のマウスを17時間絶食し、L−ピペコリン酸と
D−ピペコリン酸溶液を経口投与し、30分後から3時
間自由摂取させた。投与したピペコリン酸は、液量0.
2ml中に200μmolとした。対照区には生理食塩
水を投与した。使用頭数は、コントロール(6匹)、L
−ピペコリン酸(L−PA)(6匹)、D−ピペコリン
酸(D−PA)(6匹)、飼料摂取量の単位はgであ
る。Test Example 5: L to mouse food intake
Effect of oral administration of-and D-pipecolic acid: 8-week-old mice were fasted for 17 hours, and L-pipecolic acid and D-pipecolic acid solution were orally administered, and allowed to freely ingest for 3 hours after 30 minutes. The pipecolic acid dosed was 0.
It was 200 μmol in 2 ml. Saline was administered to the control. The number of animals used was control (6), L
-Pipecolic acid (L-PA) (6 animals), D-Pipecolic acid (D-PA) (6 animals), unit of feed intake is g.
【0035】結果は表1に示すように、投与後60分〜
120分、120分〜180分にかけてL−PA投与区
での顕著な摂取抑制が認められた。As shown in Table 1, the results were from 60 minutes after administration.
Remarkable suppression of intake in the L-PA administration group was observed over 120 minutes and 120 minutes to 180 minutes.
【0036】[0036]
【表1】 [Table 1]
【0037】[0037]
【発明の効果】以上説明したように、本発明の食欲抑制
剤は優れた食欲抑制作用または食欲減退作用を有するこ
とから、肥満症の治療薬として有用である。As described above, since the appetite suppressant of the present invention has an excellent appetite suppressing or appetite-reducing action, it is useful as a therapeutic agent for obesity.
【図1】 プロイラー雄ヒナの飼料摂取量に対する脳室
内L−ピペコリン酸投与の効果を示す図面。FIG. 1 is a drawing showing the effect of intraventricular L-pipecolic acid administration on feed intake of male broiler chicks.
【図2】 プロイラー雄ヒナの飼料摂取量に対する脳室
内D−ピペコリン酸投与の効果を示す図面。FIG. 2 is a graph showing the effect of intraventricular D-pipecolic acid administration on feed intake of male broiler chicks.
【図3】 プロイラー雄ヒナの飼料摂取量に対する脳室
内L−リジンモノ塩酸塩投与の効果を示す図面。FIG. 3 is a graph showing the effect of intraventricular L-lysine monohydrochloride administration on feed intake of male broiler chicks.
【図4】 プロイラー雄ヒナの飼料摂取量に対するL−
ピペコリン酸とL−リジンの経口投与の効果を示す図
面。FIG. 4. L- to feed intake of male broiler chicks
Drawing which shows the effect of the oral administration of pipecolic acid and L-lysine.
───────────────────────────────────────────────────── フロントページの続き Fターム(参考) 4C054 AA02 CC01 DD32 EE01 FF01 4C086 AA01 AA02 BC21 MA01 MA04 MA52 MA66 NA14 ZA70 ──────────────────────────────────────────────────続 き Continued on the front page F term (reference) 4C054 AA02 CC01 DD32 EE01 FF01 4C086 AA01 AA02 BC21 MA01 MA04 MA52 MA66 NA14 ZA70
Claims (2)
うる塩を有効成分とする食欲抑制剤。An appetite suppressant comprising pipecolic acid or a pharmaceutically acceptable salt thereof as an active ingredient.
の食欲抑制剤。2. The appetite suppressant according to claim 1, wherein the pipecolic acid is in an L form.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2001088087A JP2002284683A (en) | 2001-03-26 | 2001-03-26 | Appetite suppressant |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2001088087A JP2002284683A (en) | 2001-03-26 | 2001-03-26 | Appetite suppressant |
Publications (1)
Publication Number | Publication Date |
---|---|
JP2002284683A true JP2002284683A (en) | 2002-10-03 |
Family
ID=18943229
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2001088087A Pending JP2002284683A (en) | 2001-03-26 | 2001-03-26 | Appetite suppressant |
Country Status (1)
Country | Link |
---|---|
JP (1) | JP2002284683A (en) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1839661A3 (en) * | 2006-03-29 | 2008-04-30 | Ajinomoto Co., Inc. | Pipecolic acid-containing antidiabetic compositions |
JP2009209095A (en) * | 2008-03-04 | 2009-09-17 | Maruha Nichiro Foods Inc | Food intake regulator |
US9107941B2 (en) * | 2006-11-09 | 2015-08-18 | Sartec Corporation | Methods and compositions for reducing L-pipecolic acid effects in animals |
-
2001
- 2001-03-26 JP JP2001088087A patent/JP2002284683A/en active Pending
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1839661A3 (en) * | 2006-03-29 | 2008-04-30 | Ajinomoto Co., Inc. | Pipecolic acid-containing antidiabetic compositions |
US9107941B2 (en) * | 2006-11-09 | 2015-08-18 | Sartec Corporation | Methods and compositions for reducing L-pipecolic acid effects in animals |
JP2009209095A (en) * | 2008-03-04 | 2009-09-17 | Maruha Nichiro Foods Inc | Food intake regulator |
JP4691571B2 (en) * | 2008-03-04 | 2011-06-01 | 株式会社マルハニチロ食品 | Feeding regulator |
US8124131B2 (en) | 2008-03-04 | 2012-02-28 | Maruha Nichiro Foods, Inc. | Food intake regulator |
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