endorphin

Endorphin

Endorphine

Recent studies suggest that physical activity, as well as electric nerve stimulation and acupuncture, sends specific afferent nerve signals to the central nervous system resulting afterwards in increased pain threshold, and lower activity in the central sympathetic nervous system, resulting in lower heart rate and blood pressure. These effects seem to be mediated via endorphin release in the central nervous system because they can be mimicked by local administration of these substances and inhibited by naloxone. It seems an interesting possibility that physical training lowers blood pressure and other expressions of increased sympathetic nervous system activity via such a mechanism. Further studies along this line may be rewarding from different aspects.

Neuere Studien legen nahe, dass körperliche Aktivität sowie elektrische Nervenstimulation und Akupunktur, bestimmte afferente Signale an das zentrale Nervensystem sich danach in erhöhte Schmerzgrenze, und geringere Aktivität in der zentralen sympathischen Nervensystems sendet, was zu niedrigeren Herzfrequenz und Blutdruck Druck. Diese Wirkungen scheinen über Endorphinen im zentralen Nervensystem vermittelt werden, da sie durch lokale Verabreichung dieser Substanzen nachgeahmt werden können und inhibiert durch Naloxon. Es scheint eine interessante Möglichkeit, dass körperliches Training den Blutdruck und andere Ausdrücke der erhöhten Aktivität des sympathischen Nervensystems über einen solchen Mechanismus senkt. Weitere Studien entlang dieser Linie kann lohnend sein unter verschiedenen Aspekten.

Endorphin Deficiency Syndrome

Endorphin-Mangel-Syndrom

Bc, Vit. C, biotin; chemotherapeutic agents/antibiotics (sulfonamide/combinations, ?-lactams, tetracycline, macrolide, aminoglycoside), e.g. sulfacarbamide, sulfafurazol, sulfisomidine, sulfadiazine/(tetroxoprim), sulfamethoxazol/(trimethoprim), sulfamethoxypyridazine, sulfamethoxydiazine, sulfaperin, sulfadimethoxin, sulfamethoxypyrazine, sulfaguanol, e.g. nalidixic acid, oxalinic acid, quinoxalinic acid, pipemidic acid, norfloxacin, ofloxacin, ciprofloxacin, benzylpenicillin, phenoxymethylpenicillin, propicillin, oxacillin, dicloxacillin, flucloxacillin, ampicillin, amoxicillin, epicillin, azlocillin, methacillin, piperacillin, apalcillin, carbenicillin, ticarcillin, temocillin, bacampicillin, cephalothin, cefaloridine, cefazoline, cefazedone, cefamandole, cefuroxime, cefotiam, cefoxitin, cefotetan, cefotaxime, ceftizoxime, cefmenoxime, ceftriaxone, ceftazidime, cefoperazone, cefsulodin, cephalexin, cefaclor, cefradine, cefadroxil, latamoxef, aztreonam, imipenem, cilastatin, tetracycline, oxytetracycline, demeclocycline, doxycycline, minocycline, rolitetracycline, erythromycin, streptomycin, clindamycin, neomycin, kanamycin A; antifungal agents, e.g. griseofulvin, amphotericin, ketoconazol, miconazol; chemotherapeutic agents (antimetabolities, antibiotics, hormone antagonists, sex hormones), e.g. methotrexate, mercaptopurine, fluorouracil, cytarabine, aclarubicin, daunorubicin, doxorubicin, dactinomycin, epirubicin, bleomycin; high molecular weight active materials, e.g. erythropoetin, LH-RH-analogs, nafarelin, triptorelin, leuprorelin, buserelin, goserelin, antide, ciclosporin (A), interferon, somatotropin, somatostatin and analogs, octreotide, lanreotide, vapreotide, calcitonin, CGRP (calcitonin gene related peptide), ANP (atrial natriuretic peptide), BNP (brain natriuretic peptide), EGF (epidermal growth factor), GLP (glucagon like peptide), heparin, hirudin, hirugen, superoxide dismutase, angiotensinase, medullipin II, HBGF1 (KHK); endorphins/enkephalins, e.g. a,?,y-endorphin, dynorphin, met-enkephalin, leu-enkephalin, and vaccines, e.g. tetanus-toxoid-vaccine, diphteria-toxoid vaccine, influenza, hepatitis, poliomyelitis, measles, mumps, German measles, pertussis, FSME, cholera, typhus/paratyphus, and rabies.

Die Dispergierung erfolgte unter Eiskühlung in einem Ultraschallprozessor (Vibracell, VC375, Sonics and Materials, Danbury, CT) mit einer Energie von 260 W während 2 x 30 s. Die Dispersion wird in einem Laborsprühtrockner (Mini Spray Dryer, Büchi 190, Büchi Laboratorien, CH-Flawil) unter folgenden Bedingungen versprüht: Eingangstemperatur: 55 °C, Sprühflow: 400 Skalenteile, Aspirator: 15 Skalenteile, Sprühgeschwindigkeit: 2,4 ml/min. Die Mikrokapseln fallen als weisses, freifliessendes Pulver an.

A compound according to any one of Claims 37, 45, 50 and 55, wherein [D] is GABA, glycine, glutamic acid, aspartic acid, dopamine, norephinephrine, epinephrine, serotonin, tryptamine, neurotensin, LHRH, somatostatin, an enkephalin, an endorphin, oxytocin M, vasopressin, hydrocortisone, betamethasone, dexamethasone, cortisone, flumethasone, fluprednisolone, meprednisone, methyl prednisolone, prednisolone, prednisone, triamcinolone, cortodoxone, fludrocortisone, fluandrenolone acetonide, paramethasone, testosterone, methyl testosterone, ethinyl estradiol, norgestrel, mestranol, norethindrone, ethisterone, estradiol, estriol, estrone, dimethisterone, allylestrenol, cingestol, ethynerone, lynestrenol, norgesterone, norvininsterone, ethynodiol, oxogestone, tigestol, quinestrol, Ara-AC, pentostatin, Ara-C, 3-deazaguanine, dihydro-5-azacytidine, tiazofurin, sangivamycin, Ara-A, 6-MMPR, PCNU, spiromustine, bisbenzimidazole, L-alanosine, DON, L-ICRF, trimethyl TMM, 5-methyl tetrahydrohomofolic acid, glyoxylic acid sulfonylhydrazone, DACH, SR-2555, SR-2508, desmethylmisonidazole, mitoxantrone, menogarol, aclacinomycin A, phyllanthoside, bactobolin, aphidocolin, homoharringtonine, levonantradol, acivicin, streptozotocin, hydroxyurea, chlorambucil, cyclophosphamide, uracil mustard, melphalan, 5-FUDR, cytosine arabinoside, 6-mercaptopurine, thioguanine, 5-azacytidine, methotrexate, doxorubicin, daunomycin, aminopterin, dactinomycin, mitomycin C, a podophyllotoxin derivative, ribavirin, acyclovir, amantadine, 5-amidino-2-(5-amidino-2-benzofuranyl)indole, 4',6-diimidazolino-2-phenylbenzo(b)thiophene, 2-guanidino-4,5-di-n-propyloxazole, 2-guanidino-4,5-diphenyloxazole, 6[[(hydroxyimino)phenyl]methyl]-1-[(1-methylethyl)sulfonyl]-1 -benzimidazol-2-amine, 5,7-dimethyl-2-?- -ribofuranosyl-s-triazole(1,5-a)pyrimidine, 2-deoxy- -glucose, glucosamine, 2-deoxy-2-fluoro- -mannose, 6-amino-6-deoxy- -glucose, phenyl-6-chloro-6-deoxy-?- -glucopyranoside, (S)-9-(2,3-dihydroxypropyl)adenine, 6-azauridine, 5,6-dichloro-1-?- -ribofuranosylbenzimidazole, diazepam, oxazepam, lorazepam, chlordiazepoxide, flurazepam, bromazepam, clorazepate, nitrazepam, temazepam, phenytoin, ethotoin, mephenytoin, acetophenazine, carphenazine, fluphenazine, perphenazine, piperacetazine, clonidine, methyldopa, bethanidine, debrisoquin, hydralazine, guanethidine, haloperidol, hydroxyzine, clopenthixol, ?-vinyl GABA, ?-acetylenic GABA, phenobarbital, amobarbital, butalbital, glutethimide, aminoglutethimide, methyprylon, valproic acid, 5-hydroxy-2-n-propylpentanoic acid, 4-hydroxy-2-n-propylpentanoic acid, 3-hydroxy-2-n-propylpentanoic acid, methamphetamine, phentermine, phenmetrazine, dextroamphetamine, levamphetamine, amphetamine, phenylethylamine, methylphenidate, tranylcypromine, protriptyline, opipramol, desipramine, nortriptyline, bemegride, amiphenazole, anileridine, hydromorphone, oxymorphone, apomorphine, levorphanol, morphine, pentazocine, codeine, oxycodone, naloxone, nalorphine, tryptophan, tryamine, levodopa, ampicillin, amoxicillin, oxacillin, carbenicillin, dicloxacillin, chlortetracycline, tetracycline, methacycline, nalidixic acid, cephalexin, cephalothin, cefoxitin, clindamycin, lincomycin, oxolinic acid, phenazopyridine, sulfadiazine, thiopental, benzestrol or diethylstilbestrol.

Verbindung nach einem der Ansprüche 37, 45, 50 und 55, worin [D] ist: GABA, Glycin, Glutaminsäure, Asparaginsäure, Dopamin, Norepinephrin, Epinephrin, Serotonin, Tryptamin, Neurotensin, LHRH, Somatostatin, ein Enkephalin, ein Endorphin, Oxytocin M, Vasopressin, Hydrocortison, Betamethason, Dexamethason, Cortison, Flumethason, Fluprednisolon, Meprednison, Methylprednisolon, Prednisolon, Prednison, Triamcinolon, Cortodoxon, Fludrocortison, Fluandrenolonacetonid, Paramethason, Testosteron, Methyltestosteron, Ethinylöstradiol, Norgestrel, Mestranol, Norethindron, Ethisteron, Östradiol, Östriol, Östron, Dimethisteron, Allylöstrenol, Cingestol, Ethyneron, Lynöstrenol, Norgesteron, Norvininsteron, Ethynodiol, Oxogeston, Tigestol, Chinestrol, Ara-AC, Pentostatin, Ara-C, 3-Deazaguanin, Dihydro-5-azacytidin, Tiazofurin, Sangivamycin, Ara-A, 6-MMPR, PCNU, Spiromustin, Bisbenzimidazol, L-Alanosin, DON, L-ICRF, Trimethyl-TMM, 5-Methyltetrahydrohomofolsäure, Glyoxalsäuresulfonylhydrazon, DACH, SR-2555, SR-2508, Desmethylmisonidazol, Mitoxantron, Menogarol, Aclacinomycin A, Phyllanthosid, Bactobolin, Aphidocolin, Homoharringtonin, Levonantradol, Acivicin, Streptozotocin, Hydroxyharnstoff, Chlorambucil, Cyclophosphamid, Uracilsenf, Melphalan, 5-FUDR, Cytosinarabinosid, 6-Mercaptopurin, Thioguanin, 5-Azacytidin, Methotrexat, Doxorubicin, Daunomycin, Aminopterin, Dactinomycin, Mitomycin C, ein Podophyllotoxinderivat, Ribavirin, Acyclovir, Amantadin, 5-Amidino-2-(5-amidino-2-benzofuranyl)indol, 4',6-Diimidazolino-2-phenylbenzo(b)thiophen 2-Guanidino-4,5-di-n-propyloxazol, 2-Guanidino-4,5-diphenyloxazol, 6-[[(Hydroxyimino)phenyl]methyl]-1-[(1-methylethyl)sulfonyl]-1 -benzimidazol-2-amin, 5,7-Dimethyl-?- -ribofuranosyl-s-triazol(1,5-a)pyrimidin, 2-Deoxy- -glucose, Glucosamin, 2-Deoxy-2-fluor- -mannose, 6-Amino-6-deoxy- -glucose, Phenyl-6-chlor-6-deoxy-?- -glucopyranosid, (S)-9-(2,3-Dihydroxypropyl)adenin, 6-Azauridin, 5,6-Dichlor-1-?- -ribofuranosylbenzimidazol, Diazepam, Oxazepam, Lorazepam, Chlordiazepoxid, Flurazepam, Bromazepam, Clorazepat, Nitrazepam, Temazepam, Phenytoin, Ethotoin, Mephenytoin, Acetophenazin, Carphenazin, Fluphenazin, Perphenazin, Piperacetazin, Clonidin, Methyldopa, Bethanidin, Debrisoquin, Hydralazin, Guanethidin, Haloperidol, Hydroxyzin, Clopenthixol, ?-Vinyl-GABA, ?-acetylenisches GABA, Phenobarbital, Amobarbital, Butalbital, Glutethimid, Aminoglutethimid, Methyprylon, Valpronsäure, 5-Hydroxy-2-n-propylpentansäure, 4-Hydroxy-2-n-propylpentansäure, 3-Hydroxy-2-n-propylpentansäure, Methamphetamin, Phentermin, Phenmetrazin, Dextroamphetamin, Levamphetamin, Amphetamin, Phenylethylamin, Methylphenidat, Tranylcypromin, Protriptylin, Opipramol, Desipramin, Nortriptylin, Bemegrid, Amiphenazol, Anileridin, Hydromorphon, Oxymorphon, Apomorphin, Levorphanol, Morphin, Pentazocin, Codein, Oxycodon, Naloxon, Nalorphin, Tryptophan, Tyramin, Levodopa, Ampicillin, Amoxycillin, Oxacillin, Carbenicillin, Dicloxacillin, Chlortetracyclin, Tetracyclin, Methacyclin, Nalidixinsäure, Cephalexin, Cephalothin, Cefoxitin, Clindamycin, Lincomycin, Oxolinsäure, Phenazopyridin, Sulfadiazin, Thiopental, Benzöstrol oder Diethylstilböstrol.

A process according to Claim 25 or 30, wherein [D] is GABA, glycine, glutamic acid, aspartic acid, dopamine, norephinephrine, epinephrine, serotonin, tryptamine, neurotensin, LHRH, somatostatin, an enkephalin, an endorphin, oxytocin M, vasopressin, hydrocortisone, betamethasone, dexamethasone, cortisone, flumethasone, fluprednisolone, meprednisone, methyl prednisolone, prednisolone, prednisone, triamcinolone, cortodoxone, fludrocortisone, fluandrenolone acetonide, paramethasone, testosterone, methyl testosterone, ethinyl estradiol, norgestrel, mestranol, norethindrone, ethisterone, estradiol, estriol, estrone, dimethisterone, allylestrenol, cingestol, ethynerone, lynestrenol, norgesterone, norvininsterone, ethynodiol, oxogestone, tigestol, quinestrol, Ara-AC, pentostatin, Ara-C, 3-deazaguanine, dihydro-5-azacytidine, tiazofurin, sangivamycin, Ara-A, 6-MMPR, PCNU, spiromustine, bisbenzimidazole, L-alanosine, DON, L-ICRF, trimethyl TMM, 5-methyl tetrahydrohomofolic acid, glyoxylic acid sulfonylhydrazone, DACH, SR-2555, SR-2508, desmethylmisonidazole, mitoxantrone, menogarol, aclacinomycin A, phyllanthoside, bactobolin, aphidocolin, homoharringtonine, levonantradol, acivicin, streptozotocin, hydroxyurea, chlorambucil, cyclophosphamide, uracil mustard, melphalan, 5-FUDR, cytosine arabinoside, 6-mercaptopurine, thioguanine, 5-azacytidine, methotrexate, doxorubicin, daunomycin, aminopterin, dactinomycin, mitomycin C, a podophyllotoxin derivative, ribavirin, acyclovir, amantadine, 5-amidino-2-(5-amidino-2-benzofuranyl)indole, 4',6-diimidazolino-2-phenylbenzo(b)thiophene, 2-guanidino-4,5-di-n-propyloxazole, 2-guanidino-4,5-diphenyloxazole, 6[[(hydroxyimino)phenyl]methyl]-1-[(1-methylethyl)sulfonyl]-1 -benzimidazol-2-amine, 5,7-dimethyl-2-?- -ribofuranosyl-s-triazole(1,5-a)pyrimidine, 2-deoxy- -glucose, glucosamine, 2-deoxy-2-fluoro- -mannose, 6-amino-6-deoxy- -glucose, phenyl-6-chloro-6-deoxy-?- -glucopyranoside, (S)-9-(2,3-dihydroxypropyl)adenine, 6-azauridine, 5,6-dichloro-1-?- -ribofuranosylbenzimidazole, diazepam, oxazepam, lorazepam, chlordiazepoxide, flurazepam, bromazepam, clorazepate, nitrazepam, temazepam, phenytoin, ethotoin, mephenytoin, acetophenazine, carphenazine, fluphenazine, perphenazine, piperacetazine, clonidine, methyldopa, bethanidine, debrisoquin, hydralazine, guanethidine, haloperidol, hydroxyzine, clopenthixol, ?-vinyl GABA, ?-acetylenic GABA, phenobarbital, amobarbital, butalbital, glutethimide, aminoglutethimide, methyprylon, valproic acid, 5-hydroxy-2-n-propylpentanoic acid, 4-hydroxy-2-n-propylpentanoic acid, 3-hydroxy-2-n-propylpentanoic acid, methamphetamine, phentermine, phenmetrazine, dextroamphetamine, levamphetamine, amphetamine, phenylethylamine, methylphenidate, tranylcypromine, protriptyline, opipramol, desipramine, nortriptyline, bemegride, amiphenazole, anileridine, hydromorphone, oxymorphone, apomorphine, levorphanol, morphine, pentazocine, codeine, oxycodone, naloxone, nalorphine, tryptophan, tryamine, levodopa, ampicillin, amoxicillin, oxacillin, carbenicillin, dicloxacillin, chlortetracycline, tetracycline, methacycline, nalidixic acid, cephalexin, cephalothin, cefoxitin, clindamycin, lincomycin, oxolinic acid, phenazopyridine, sulfadiazine, thiopental, benzestrol or diethylstilbestrol.

Verfahren nach Anspruch 25 oder 30, wobei [D] ist: GABA, Glycin, Glutaminsäure, Asparaginsäure, Dopamin, Norepinephrin, Epinephrin, Serotonin, Tryptamin, Neurotensin, LHRH, Somatostatin, ein Enkephalin, ein Endorphin, Oxytocin M, Vasopressin, Hydrocortison, Betamethason, Dexamethason, Cortison, Flumethason, Fluprednisolon, Meprednison, Methylprednisolon, Prednisolon, Prednison, Triamcinolon, Cortodoxon, Fludrocortison, Fluandrenolonacetonid, Paramethason, Testosteron, Methyltestosteron, Ethinylöstradiol, Norgestrel, Mestranol, Norethindron, Ethisteron, Östradiol, Östriol, Östron, Dimethisteron, Allylöstrenol, Cingestol, Ethyneron, Lynöstrenol, Norgesteron, Norvininsteron, Ethynodiol, Oxogeston, Tigestol, Chinestrol, Ara-AC, Pentostatin, Ara-C, 3-Deazaguanin, Dihydro-5-azacytidin, Tiazofurin, Sangivamycin, Ara-A, 6-MMPR, PCNU, Spiromustin, Bisbenzimidazol, L-Alanosin, DON, L-ICRF, Trimethyl-TMM, 5-Methyltetrahydrohomofolsäure, Glyoxalsäuresulfonylhydrazon, DACH, SR-2555, SR-2508, Desmethylmisonidazol, Mitoxantron, Menogarol, Aclacinomycin A, Phyllanthosid, Bactobolin, Aphidocolin, Homoharringtonin, Levonantradol, Acivicin, Streptozotocin, Hydroxyharnstoff, Chlorambucil, Cyclophosphamid, Uracilsenf, Melphalan, 5-FUDR, Cytosinarabinosid, 6-Mercaptopurin, Thioguanin, 5-Azacytidin, Methotrexat, Doxorubicin, Daunomycin, Aminopterin, Dactinomycin, Mitomycin C, ein Podophyllotoxinderivat, Ribavirin, Acyclovir, Amantadin, 5-Amidino-2-(5-amidino-2-benzofuranyl)indol, 4',6-Diimidazolino-2-phenylbenzo(b)thiophen, 2-Guanidino-4,5-di-n-propyloxazol, 2-Guanidino-4,5-diphenyloxazol, 6-[[(Hydroxyimino)phenyl]methyl]-1-[(1-methylethyl)sulfonyl]-1 -benzimidazol-2-amin, 5,7-Dimethyl-?- -ribofuranosyl-s-triazol(1,5-a)pyrimidin, 2-Deoxy- -glucose, Glucosamin, 2-Deoxy-2-fluor- -mannose, 6-Amino-6-deoxy- -glucose, Phenyl-6-chlor-6-deoxy-?- -glucopyranosid, (S)-9-(2,3-Dihydroxypropyl)adenin, 6-Azauridin, 5,6-Dichlor-1-?- -ribofuranosylbenzimidazol, Diazepam, Oxazepam, Lorazepam, Chlordiazepoxid, Flurazepam, Bromazepam, Clorazepat, Nitrazepam, Temazepam, Phenytoin, Ethotoin, Mephenytoin, Acetophenazin, Carphenazin, Fluphenazin, Perphenazin, Piperacetazin, Clonidin, Methyldopa, Bethanidin, Debrisoquin, Hydralazin, Guanethidin, Haloperidol, Hydroxyzin, Clopenthixol, ?-Vinyl-GABA, ?-acetylenisches GABA, Phenobarbital, Amobarbital, Butalbital, Glutethimid, Aminoglutethimid, Methyprylon, Valpronsäure, 5-Hydroxy-2-n-propylpentansäure, 4-Hydroxy-2-n-propylpentansäure, 3-Hydroxy-2-n-propylpentansäure, Methamphetamin, Phentermin, Phenmetrazin, Dextroamphetamin, Levamphetamin, Amphetamin, Phenylethylamin, Methylphenidat, Tranylcypromin, Protriptylin, Opipramol, Desipramin, Nortriptylin, Bemegrid, Amiphenazol, Anileridin, Hydromorphon, Oxymorphon, Apomorphin, Levorphanol, Morphin, Pentazocin, Codein, Oxycodon, Naloxon, Nalorphin, Tryptophan, Tyramin, Levodopa, Ampicillin, Amoxycillin, Oxacillin, Carbenicillin, Dicloxacillin, Chlortetracyclin, Tetracyclin, Methacyclin, Nalidixinsäure, Cephalexin, Cephalothin, Cefoxitin, Clindamycin, Lincomycin, Oxolinsäure, Phenazopyridin, Sulfadiazin, Thiopental, Benzöstrol oder Diethylstilböstrol.

Endorphin, Beta (bEP) (8)

Endorphin, Beta (bEP) (8)

Endorphin, Beta (bEP) (8)

Faktor Xa (2)