JPH0249289B2 - - Google Patents
Info
- Publication number
- JPH0249289B2 JPH0249289B2 JP56151901A JP15190181A JPH0249289B2 JP H0249289 B2 JPH0249289 B2 JP H0249289B2 JP 56151901 A JP56151901 A JP 56151901A JP 15190181 A JP15190181 A JP 15190181A JP H0249289 B2 JPH0249289 B2 JP H0249289B2
- Authority
- JP
- Japan
- Prior art keywords
- psychodepressant
- ceruletide
- polypeptide
- body weight
- pyr
- 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.)
- Expired - Lifetime
Links
- 229920001184 polypeptide Polymers 0.000 claims description 22
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 22
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 22
- 108010010737 Ceruletide Proteins 0.000 claims description 17
- YRALAIOMGQZKOW-UHFFFAOYSA-N sulfated caerulein Natural products C=1C=CC=CC=1CC(C(N)=O)NC(=O)C(CC(O)=O)NC(=O)C(CCSC)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)CNC(=O)C(C(C)O)NC(=O)C(NC(=O)C(CC(O)=O)NC(=O)C(CCC(N)=O)NC(=O)C1NC(=O)CC1)CC1=CC=C(OS(O)(=O)=O)C=C1 YRALAIOMGQZKOW-UHFFFAOYSA-N 0.000 claims description 17
- 229960001706 ceruletide Drugs 0.000 claims description 15
- YRALAIOMGQZKOW-HYAOXDFASA-N ceruletide Chemical group C([C@@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(N)=O)[C@@H](C)O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(OS(O)(=O)=O)C=C1 YRALAIOMGQZKOW-HYAOXDFASA-N 0.000 claims description 14
- 229940079593 drug Drugs 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 9
- 230000037396 body weight Effects 0.000 claims description 7
- 150000003839 salts Chemical class 0.000 claims description 5
- 241001465754 Metazoa Species 0.000 claims description 4
- 238000010255 intramuscular injection Methods 0.000 claims description 4
- 239000007927 intramuscular injection Substances 0.000 claims description 4
- -1 t-butyloxy-carbonyl Chemical group 0.000 claims description 4
- 238000010253 intravenous injection Methods 0.000 claims description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 2
- 239000007864 aqueous solution Substances 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 229910052739 hydrogen Inorganic materials 0.000 claims description 2
- 239000001257 hydrogen Substances 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 239000008101 lactose Substances 0.000 claims description 2
- 239000000969 carrier Substances 0.000 claims 2
- 238000007911 parenteral administration Methods 0.000 claims 2
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 230000003078 antioxidant effect Effects 0.000 claims 1
- 125000001664 diethylamino group Chemical class [H]C([H])([H])C([H])([H])N(*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- VZFDRQUWHOVFCA-UHFFFAOYSA-L disodium;2-sulfanylbutanedioate Chemical compound [Na+].[Na+].[O-]C(=O)CC(S)C([O-])=O VZFDRQUWHOVFCA-UHFFFAOYSA-L 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- LNEPOXFFQSENCJ-UHFFFAOYSA-N haloperidol Chemical compound C1CC(O)(C=2C=CC(Cl)=CC=2)CCN1CCCC(=O)C1=CC=C(F)C=C1 LNEPOXFFQSENCJ-UHFFFAOYSA-N 0.000 description 18
- 230000000694 effects Effects 0.000 description 12
- IZTQOLKUZKXIRV-YRVFCXMDSA-N sincalide Chemical compound C([C@@H](C(=O)N[C@@H](CCSC)C(=O)NCC(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(N)=O)NC(=O)[C@@H](N)CC(O)=O)C1=CC=C(OS(O)(=O)=O)C=C1 IZTQOLKUZKXIRV-YRVFCXMDSA-N 0.000 description 11
- 108010087230 Sincalide Proteins 0.000 description 10
- 238000010609 cell counting kit-8 assay Methods 0.000 description 10
- 206010010904 Convulsion Diseases 0.000 description 9
- 229960003878 haloperidol Drugs 0.000 description 9
- 238000007920 subcutaneous administration Methods 0.000 description 8
- 230000001773 anti-convulsant effect Effects 0.000 description 7
- 241000699670 Mus sp. Species 0.000 description 6
- 208000009132 Catalepsy Diseases 0.000 description 5
- LHNKBXRFNPMIBR-UHFFFAOYSA-N Picrotoxin Natural products CC(C)(O)C1(O)C2OC(=O)C1C3(O)C4OC4C5C(=O)OC2C35C LHNKBXRFNPMIBR-UHFFFAOYSA-N 0.000 description 5
- 206010047853 Waxy flexibility Diseases 0.000 description 5
- 150000001875 compounds Chemical class 0.000 description 5
- 230000036461 convulsion Effects 0.000 description 5
- 229960003529 diazepam Drugs 0.000 description 5
- AAOVKJBEBIDNHE-UHFFFAOYSA-N diazepam Chemical compound N=1CC(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 AAOVKJBEBIDNHE-UHFFFAOYSA-N 0.000 description 5
- VJKUPQSHOVKBCO-AHMKVGDJSA-N picrotoxin Chemical compound O=C([C@@]12O[C@@H]1C[C@]1(O)[C@@]32C)O[C@@H]3[C@H]2[C@@H](C(=C)C)[C@@H]1C(=O)O2.O=C([C@@]12O[C@@H]1C[C@]1(O)[C@@]32C)O[C@@H]3[C@H]2[C@@H](C(C)(O)C)[C@@H]1C(=O)O2 VJKUPQSHOVKBCO-AHMKVGDJSA-N 0.000 description 5
- 230000004006 stereotypic behavior Effects 0.000 description 5
- CWRVKFFCRWGWCS-UHFFFAOYSA-N Pentrazole Chemical compound C1CCCCC2=NN=NN21 CWRVKFFCRWGWCS-UHFFFAOYSA-N 0.000 description 4
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 description 4
- DUGOZIWVEXMGBE-UHFFFAOYSA-N Methylphenidate Chemical compound C=1C=CC=CC=1C(C(=O)OC)C1CCCCN1 DUGOZIWVEXMGBE-UHFFFAOYSA-N 0.000 description 3
- 101710082071 Phyllocaerulein Proteins 0.000 description 3
- 238000010586 diagram Methods 0.000 description 3
- 229960001344 methylphenidate Drugs 0.000 description 3
- 230000000144 pharmacologic effect Effects 0.000 description 3
- 230000003389 potentiating effect Effects 0.000 description 3
- 230000002936 tranquilizing effect Effects 0.000 description 3
- 206010015995 Eyelid ptosis Diseases 0.000 description 2
- 208000036754 Schizophrenia, catatonic type Diseases 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 230000003042 antagnostic effect Effects 0.000 description 2
- 239000001961 anticonvulsive agent Substances 0.000 description 2
- 229960003965 antiepileptics Drugs 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 231100000673 dose–response relationship Toxicity 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- 230000001939 inductive effect Effects 0.000 description 2
- 230000010534 mechanism of action Effects 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 229960005181 morphine Drugs 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 201000003004 ptosis Diseases 0.000 description 2
- 201000000980 schizophrenia Diseases 0.000 description 2
- 229940125725 tranquilizer Drugs 0.000 description 2
- 239000003204 tranquilizing agent Substances 0.000 description 2
- 208000009810 Catatonic Schizophrenia Diseases 0.000 description 1
- 101800001982 Cholecystokinin Proteins 0.000 description 1
- 102100025841 Cholecystokinin Human genes 0.000 description 1
- 108010016626 Dipeptides Proteins 0.000 description 1
- 102100038796 E3 ubiquitin-protein ligase TRIM13 Human genes 0.000 description 1
- 101000664589 Homo sapiens E3 ubiquitin-protein ligase TRIM13 Proteins 0.000 description 1
- 241000269431 Phyllomedusa sauvagii Species 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 229940035676 analgesics Drugs 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 230000000561 anti-psychotic effect Effects 0.000 description 1
- 239000008135 aqueous vehicle Substances 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 229930190815 caerulein Natural products 0.000 description 1
- 229940107137 cholecystokinin Drugs 0.000 description 1
- 239000012050 conventional carrier Substances 0.000 description 1
- 239000003179 convulsant agent Substances 0.000 description 1
- 230000002920 convulsive effect Effects 0.000 description 1
- 150000005332 diethylamines Chemical class 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000008451 emotion Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- UYXAWHWODHRRMR-UHFFFAOYSA-N hexobarbital Chemical compound O=C1N(C)C(=O)NC(=O)C1(C)C1=CCCCC1 UYXAWHWODHRRMR-UHFFFAOYSA-N 0.000 description 1
- 229960002456 hexobarbital Drugs 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 230000008450 motivation Effects 0.000 description 1
- 229960005152 pentetrazol Drugs 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 230000000630 rising effect Effects 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 230000004622 sleep time Effects 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
Landscapes
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP56151901A JPS5865222A (ja) | 1981-09-25 | 1981-09-25 | 精神抑制薬 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP56151901A JPS5865222A (ja) | 1981-09-25 | 1981-09-25 | 精神抑制薬 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5865222A JPS5865222A (ja) | 1983-04-18 |
| JPH0249289B2 true JPH0249289B2 (fr) | 1990-10-29 |
Family
ID=15528661
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP56151901A Granted JPS5865222A (ja) | 1981-09-25 | 1981-09-25 | 精神抑制薬 |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS5865222A (fr) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK489683A (da) * | 1982-10-27 | 1984-04-28 | Amano Pharma Co Ltd | Fremgangsmaade til fremstilling af peptider |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5750922A (en) * | 1980-09-16 | 1982-03-25 | Erba Carlo Spa | Polypeptide-containing analgesic |
-
1981
- 1981-09-25 JP JP56151901A patent/JPS5865222A/ja active Granted
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5750922A (en) * | 1980-09-16 | 1982-03-25 | Erba Carlo Spa | Polypeptide-containing analgesic |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS5865222A (ja) | 1983-04-18 |
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