DE3424009A1 - Agent and therapeutic composition for the therapy of neuralgia, neuritis and rheumatic disorders, as well as of gout - Google Patents
Agent and therapeutic composition for the therapy of neuralgia, neuritis and rheumatic disorders, as well as of goutInfo
- Publication number
- DE3424009A1 DE3424009A1 DE19843424009 DE3424009A DE3424009A1 DE 3424009 A1 DE3424009 A1 DE 3424009A1 DE 19843424009 DE19843424009 DE 19843424009 DE 3424009 A DE3424009 A DE 3424009A DE 3424009 A1 DE3424009 A1 DE 3424009A1
- Authority
- DE
- Germany
- Prior art keywords
- active ingredient
- phe
- ingredient according
- arg
- msh
- 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.)
- Withdrawn
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
- C07K5/0823—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp and Pro-amino acid; Derivatives thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/665—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
- C07K14/68—Melanocyte-stimulating hormone [MSH]
- C07K14/685—Alpha-melanotropin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/665—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
- C07K14/695—Corticotropin [ACTH]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Toxicology (AREA)
- Endocrinology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
Wirkstoff und therapeutisches Mittel zur TherapieActive ingredient and therapeutic agent for therapy
von Neuralgien, Neuritiden und rheumatischen Erkrankungen sowie der Gicht Die vorliegende Erfindung betrifft einen Wirkstoff zur Therapie von Neuralgien, Neuritiden und rheumatischen Erkrankungen sowie der Gicht. Die Erfindung bezieht sich ferner auf ein therapeutisches Mittel, das einen derartigen Wirkstoff enthält.of neuralgia, neuritis and rheumatic diseases as well as the Gout The present invention relates to an active ingredient for the therapy of neuralgia, Neuritis and rheumatic diseases as well as gout. The invention relates also refer to a therapeutic agent containing such an active ingredient.
Es ist ein Mittel zur Behandlung von rheumatischen Krankheitsbildern bekannt, bei dem es sich um ein synthetisches ACTH-Präparat handelt. Das Präparat enthält ein offenkettiges Polypeptid, das der Sequenz der ersten 24 Aminosäuren des natürlichen ACTH-Moleküls (Corticotrophin) entspricht und alle pharmakologischen Eigenschaften des körpereigenen Corticotrophins besitzt. Es ist bekannt, daß ACTH das Wachstum der Nebenrinden und die Bildung und Freisetzung von Steroid-Hormonen durch die Nebennierenrinde stimuliert, insbesondere die Bildung von Cortisol und seiner Vorstufen in der Nebennierenrinde steigert. Die therapeutischen Wirkungen des vorstehend genannten synthetischen ACTH-Präparates werden im. wesentlichen auf diese Effekte zurückgeführt.It is a means of treating rheumatic diseases known, which is a synthetic ACTH preparation. The preparation contains an open-chain polypeptide that follows the sequence of the first 24 amino acids of the natural ACTH molecule (corticotrophin) and all pharmacological Has properties of the body's own corticotrophin. It is known that ACTH the growth of the side cortices and the formation and release of steroid hormones stimulated by the adrenal cortex, in particular the formation of cortisol and its precursors in the adrenal cortex increases. The therapeutic effects of the aforementioned synthetic ACTH preparation are in. essential on attributed these effects.
Erfindungsgemäß wird die Anwendung von i-Melanotropin ( o( -MSH), ß-Melanotropin ( p-MSH) und/oder »t-Melanotropin ( 8a-MSH) sowie Peptid-Teilstücken dieser Substanzen als Wirkstoff zur Therapie von Neuralgien, Neuritiden und rheumatischen Erkrankungen sowie der Gicht vorgeschlagen.According to the invention, the use of i-melanotropin (o (-MSH), ß-melanotropin (p-MSH) and / or »t-melanotropin (8a-MSH) as well as peptide fragments these substances as an active ingredient for the therapy of neuralgia, neuritides and rheumatic diseases Diseases as well as gout are suggested.
Als Melanotropin bezeichnet man im Hypophysenzwischenlappen gebildete Peptidhormone, deren Sekretion durch den Hyphothalamus-Faktor gehemmt wird. Bei -Melanotropin ( o( -MSH) handelt es sich um ein lineares Polypeptid mit dreizehn Aminosäuren, während es sich bei p -MSH (Mensch) um ein Polypeptid mit achtzehn Aminosäuren handelt. Als t -Melanotropin ( P -MSH) wird ein Polypeptid mit zwölf Aminosäuren bezeichnet. Die vorstehend genannten Substanzen sind bereits isoliert bzw. synthetisch hergestellt worden und bekannt. Derartige Hormone werden auch als Farbwechselhormone des Hyphophysenzwischenlappens bezeichnet. Es ist bekannt, daß diese Hormone eine Erweiterung der dunklen (und roten) Pigmentzellen bei kaltblütigen Wirbeltieren bewirken. Melanotropin is one that is formed in the pituitary lobe Peptide hormones whose secretion is inhibited by the hyphothalamus factor. at -Melanotropin (o (-MSH) is a linear polypeptide of thirteen Amino acids, while p -MSH (human) is a polypeptide of eighteen Amino acids. As t -melanotropin (P -MSH) is a polypeptide with twelve Called amino acids. The substances mentioned above have already been isolated or synthetically produced and known. Such hormones are also called Color-changing hormones of the pituitary lobe called. It is known that these hormones are an enlargement of the dark (and red) pigment cells in cold blooded ones Effect vertebrates.
Es wurde nunmehr gefunden, daß sich diese Substanzen in ausgezeichneter Weise als Wirkstoff zur Therapie der vorstehend geschilderten Krankheitsbilder eignen. It has now been found that these substances are excellent Way suitable as an active ingredient for the therapy of the diseases described above.
Es sei darauf hingewiesen, daß beim synthetisch zugänglichen oC -MSH die Folge der dreizehn aufbauenden Aminosäuren der des Hormons ACTH entspricht. Die Fachwelt war zwar bisher aufgrund von Untersuchungen mit Polypeptidfragmenten und synthetischen Polypeptiden der Auffassung, daß für die biologische Aktivilät des ACTH nicht das gesamte Molekül benötigt wird; hierbei wurde jedoch synthetischen Polypeptiden, die aus neunzehn oder dreiundzwanzig Aminosäuren bestehen, die vollständige biologische Aktivität zugesprochen. Den hier in Rede stehenden Polypeptiden wurde keine therapeutische Wirkung beigemessen. It should be noted that the synthetically accessible oC -MSH the sequence of the thirteen constituent amino acids corresponds to that of the hormone ACTH. The professional world has been based on investigations with polypeptide fragments and synthetic polypeptides believed to be essential for biological activity ACTH does not require the entire molecule; however, this was synthetic Polypeptides composed of nineteen or twenty-three amino acids, the complete biological activity awarded. The polypeptides in question here was no therapeutic effect attached.
Als Beispiele für die Anwendung des MSH-Wirkstoffes seien entzündliche rheumatische Erkrankungen, wie beispielsweise chronische Polyarthritis, Spondylarthritis ankylopoetica degenerative rheumatische Erkrankungen, wie beispielsweise Arthrosen, Spondylosen, extraartikuläre rheumatische Erkrankungen, wie beispielsweise Muskelrheumatismus, und pararheumatische Erkrankungen, insbesondere Kollagenosen genannt. Der Wirkstoff ist ferner zur Therapie der Gicht (Hyperurikämie) geeignet. Er ist des weiteren zur Behandlung von Neuralgien (anfallsweise auftretenden Schmerzen in der Bahn eines sensiblen oder gemischten Nerven) oder Neuritiden (Nervenentzündungen) der verschiedenen Erscheinungsformen geeignet.Examples of the use of the MSH active ingredient are inflammatory ones rheumatic diseases such as rheumatoid arthritis, spondylarthritis ankylopoetica degenerative rheumatic diseases such as Arthrosis, spondylosis, extra-articular rheumatic diseases such as Muscular rheumatism and pararheumatic diseases, especially collagenoses called. The active ingredient is also suitable for the therapy of gout (hyperuricemia). It is also used to treat neuralgia (attacks of pain in the pathway of a sensitive or mixed nerve) or neuritis (inflammation of the nerves) suitable for the various manifestations.
Die Wirkstoffe können sowohl in reiner Form als auch als therapeutische Mittel in Verbindung mit üblichen Träger (Inert)- und Hilfsstoffen appliziert werden, wobei grundsätzlich sämtliche möglichen Applikationsformen geeignet sind. Da die Wirkstoffe ausserordentlich empfindlich sind und sehr rasch ihre Wirksamkeit verlieren, sollten sie vorzugsweise zusammen mit einer Depotsubstanz appliziert werden. Der Wirkstoff kann dabei beispielsweise an einen anorganischen Zinkkomplex adsorbiert werden.The active ingredients can be used both in pure form and as therapeutic Agents are applied in conjunction with common carriers (inert) and auxiliaries, in principle, all possible forms of application are suitable. Since the Active ingredients are extremely sensitive and lose their effectiveness very quickly, they should preferably be applied together with a depot substance. Of the Active ingredient can be adsorbed on an inorganic zinc complex, for example will.
Der Wirkstoff wirkt als oC -MSH praktisch in gleicher Weise wie als p -MSH, was darauf zurückzuführen ist, daß beide Stoffe eine identische Sequenz von sieben Aminosäuren haben, nämlich Met-Glu-His-Phe-Arg-Trp-Gly. Erfindungsgemäß kann daher auch das Polypeptid der entsprechenden Aminosäurensequenz selbst eingesetzt werden.The active ingredient acts as oC -MSH in practically the same way as as p -MSH, which is due to the fact that both substances have an identical sequence of seven amino acids, namely Met-Glu-His-Phe-Arg-Trp-Gly. According to the invention can therefore also use the polypeptide of the corresponding amino acid sequence itself will.
Die besten Ergebnisse wurd en mit dem Tetrapeptid His-Phe-Arg-Trp erzielt, das im o(-, p - und t -MSH vorkommt.The best results were achieved with the tetrapeptide His-Phe-Arg-Trp achieved, which occurs in the o (-, p - and t -MSH.
Dieses Tetrapeptid His-Phe-Arg-Trp wird als eigentlich biologisch aktiver Teil des MSH angesehen.This tetrapeptide His-Phe-Arg-Trp is actually considered biological active part of the MSH.
Auch weitere Polypeptide mit der Aminosäurensequenz His-Phe-Arg-Trp, wie beispielsweise t -MSH (3-8), haben zu guten Ergebnissen geführt.Also other polypeptides with the amino acid sequence His-Phe-Arg-Trp, such as t -MSH (3-8) have given good results.
Claims (17)
Priority Applications (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19843424009 DE3424009A1 (en) | 1984-06-29 | 1984-06-29 | Agent and therapeutic composition for the therapy of neuralgia, neuritis and rheumatic disorders, as well as of gout |
EP84115260A EP0146113A3 (en) | 1983-12-15 | 1984-12-12 | Active agent and therapeutical composition for the treatment of deincephalon failures of nervous deseases and skin diseases |
AU36680/84A AU3668084A (en) | 1983-12-15 | 1984-12-14 | Melanotropin or fragments thereof for treating nerve and skin disease |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19843424009 DE3424009A1 (en) | 1984-06-29 | 1984-06-29 | Agent and therapeutic composition for the therapy of neuralgia, neuritis and rheumatic disorders, as well as of gout |
Publications (1)
Publication Number | Publication Date |
---|---|
DE3424009A1 true DE3424009A1 (en) | 1986-01-02 |
Family
ID=6239469
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DE19843424009 Withdrawn DE3424009A1 (en) | 1983-12-15 | 1984-06-29 | Agent and therapeutic composition for the therapy of neuralgia, neuritis and rheumatic disorders, as well as of gout |
Country Status (1)
Country | Link |
---|---|
DE (1) | DE3424009A1 (en) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3623019A1 (en) * | 1986-07-09 | 1988-01-21 | Dieter Prof Dr Dr Aderhold | Melanotropin as therapeutic agent |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3345358A1 (en) * | 1983-12-15 | 1985-06-27 | Dieter Prof. Dr. Dr. 5883 Kierspe Aderhold | Therapeutic composition for the treatment of dysfunctions of the human diencephalon and/or of the pituitary, especially of multiple sclerosis |
-
1984
- 1984-06-29 DE DE19843424009 patent/DE3424009A1/en not_active Withdrawn
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3345358A1 (en) * | 1983-12-15 | 1985-06-27 | Dieter Prof. Dr. Dr. 5883 Kierspe Aderhold | Therapeutic composition for the treatment of dysfunctions of the human diencephalon and/or of the pituitary, especially of multiple sclerosis |
Non-Patent Citations (4)
Title |
---|
Chem. Abstr. 89, 1978, 140824 * |
J. Biol. Chem. 255, 1980, S.401-407, CAS Registry Handbook, Reg. Nr. 25 615-38-7 * |
JAHNTKE H.-D., JESCHHEITH.: Aminosäuren, Peptide, Proteine, 1982, s.273, 278, 279, 323 * |
VOELTER W., SCHMID-SIEGMANN E.: Dipeptides and Amino Acids, Vol.2, 1983, S.221 Ziffer 983 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3623019A1 (en) * | 1986-07-09 | 1988-01-21 | Dieter Prof Dr Dr Aderhold | Melanotropin as therapeutic agent |
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Legal Events
Date | Code | Title | Description |
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8110 | Request for examination paragraph 44 | ||
8139 | Disposal/non-payment of the annual fee |