エンケファリナーゼ、エンケファリン分解酵素
- 関
- neprilysin、neutral endopeptidase
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/04/02 02:17:49」(JST)
[Wiki en表示]
Enkephalinases are enzymes that degrade endogenous enkephalin opioid peptides. They include:
- Aminopeptidase N (APN)[1]
- Neutral endopeptidase (NEP)[1]
- Dipeptidyl peptidase 3 (DPP3)[1]
- Carboxypeptidase A6 (CPA6)[2]
- Angiotensin-converting enzyme (ACE)[3]
See also[edit]
- Enkephalinase inhibitor
- Enkephalin
References[edit]
- ^ a b c Thanawala V, Kadam VJ, Ghosh R (October 2008). "Enkephalinase inhibitors: potential agents for the management of pain". Current Drug Targets 9 (10): 887–94. doi:10.2174/138945008785909356. PMID 18855623.
- ^ Lyons PJ, Callaway MB, Fricker LD (March 2008). "Characterization of carboxypeptidase A6, an extracellular matrix peptidase". The Journal of Biological Chemistry 283 (11): 7054–63. doi:10.1074/jbc.M707680200. PMID 18178555.
- ^ Benuck M, Berg MJ, Marks N (1982). "Separate metabolic pathways for Leu-enkephalin and Met-enkephalin-Arg(6)-Phe(7) degradation by rat striatal synaptosomal membranes". Neurochemistry International 4 (5): 389–96. doi:10.1016/0197-0186(82)90081-X. PMID 20487892.
Hydrolase: proteases (EC 3.4)
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3.4.11-19: Exopeptidase |
3.4.11 |
- Aminopeptidase
- Alanine
- Arginyl
- Aspartyl
- Cystinyl
- Leucyl
- Glutamyl
- Methionyl
- O
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3.4.13 |
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3.4.14 |
- Dipeptidyl peptidase
- Cathepsin C
- Dipeptidyl peptidase-4
- Tripeptidyl peptidase
- Tripeptidyl peptidase I
- Tripeptidyl peptidase II
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3.4.15 |
- Angiotensin-converting enzyme
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3.4.16 |
- Serine type carboxypeptidases: Cathepsin A
- DD-transpeptidase
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3.4.17 |
- Metallocarboxypeptidases: Carboxypeptidase
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Other/ungrouped |
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3.4.21-24: Endopeptidase |
- Serine proteases
- Cysteine protease
- Aspartic acid protease
- Metalloendopeptidases
- Other/ungrouped: Amyloid precursor protein secretase
- Alpha secretase
- Beta-secretase 1
- Beta-secretase 2
- Gamma secretase
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3.4.99: Unknown |
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- B
- enzm
- 1.1
- 2
- 3
- 4
- 5
- 6
- 7
- 8
- 10
- 11
- 13
- 14
- 15-18
- 2.1
- 3.1
- 4.1
- 5.1
- 6.1-3
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Opioids
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Opium and
poppy straw
derivatives |
Crude opiate
extracts /
whole opium
products |
- B&O Supprettes
- Diascordium
- Dover's powder
- Kendal Black Drop
- Laudanum
- Mithridate
- Opium
- Paregoric
- Polish heroin (compote/kompot)
- Poppy straw
- Poppy tea
- Smoking opium
- Theriac
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Natural opiates |
Opium
alkaloids |
- Codeine
- Morphine
- Oripavine
- Pseudomorphine
- Thebaine
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Alkaloid
salts mixtures |
- Pantopon
- Papaveretum (Omnopon)
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Semisynthetics
including
Bentley
compounds |
Morphine
family |
- 2,4-Dinitrophenylmorphine
- 6-MDDM
- Azidomorphine
- Chlornaltrexamine
- Desocodeine
- Desomorphine
- Dihydromorphine
- Hydromorphinol
- Methyldesorphine
- N-Phenethylnormorphine
- RAM-378
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3,6-diesters
of morphine |
- Acetylpropionylmorphine
- Diacetyldihydromorphine
- Dibenzoylmorphine
- Dipropanoylmorphine
- Heroin
- Nicomorphine
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Codeine-dionine
family |
- 6-Monoacetylcodeine
- Benzylmorphine
- Codeine methylbromide
- Ethylmorphine
- Heterocodeine
- Isocodeine
- Myrophine
- Pholcodine
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Morphinones
and morphols |
- 14-Cinnamoyloxycodeinone
- 14-Ethoxymetopon
- 14-Methoxymetopon
- 14-Phenylpropoxymetopon
- 3-Acetyloxymorphone
- 3,14-Diacetyloxymorphone
- 6-MDDM
- 7-Spiroindanyloxymorphone
- Acetylmorphone
- Codeinone
- Codoxime
- Conorfone
- Hydrocodone
- Hydromorphone
- IBNtxA
- Methyldihydromorphine
- Metopon
- Morphinone
- N-Phenethyl-14-ethoxymetopon
- Nalmexone
- Oxycodone
- Oxymorphol
- Oxymorphone
- Pentamorphone
- Semorphone
- Thebacon
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Morphides |
- α-Chlorocodide
- Chloromorphide
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Dihydrocodeine
series |
- 14-Hydroxydihydrocodeine
- Acetyldihydrocodeine
- Dihydrocodeine
- Nicocodeine
- Nicodicodeine
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Nitrogen
morphine
derivatives |
- Codeine-N-oxide
- Morphine-N-oxide
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Hydrazones |
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Halogenated
morphine
derivatives |
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Active opiate
metabolites |
- 6-Monoacetylmorphine
- Morphine-6-glucuronide
- Norcodeine
- Normorphine
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Morphinans |
- 3-Hydroxymorphinan
- Butorphanol
- Cyclorphan
- Cyprodime
- Dextrallorphan
- Drotebanol
- Ketorfanol
- Levallorphan
- Levomethorphan
- Levophenacylmorphan
- Levorphanol
- Nalbuphine
- Norlevorphanol
- Oxilorphan
- Phenomorphan
- Proxorphan
- Racemethorphan/Methorphan
- Racemorphanol/Morphanol
- Ro4-1539
- Sinomenine/Cocculine
- Xorphanol
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Benzomorphans |
- 8-CAC
- Alazocine
- Anazocine
- Bremazocine
- Butinazocine
- Carbazocine
- Cogazocine
- Dezocine
- Eptazocine
- Etazocine
- Ethylketazocine
- Fluorophen
- Ibazocine
- Ketazocine
- Metazocine
- Moxazocine
- Pentazocine
- Phenazocine
- Tonazocine
- Volazocine
- Zenazocine
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4-Phenylpiperidines |
Pethidines
(Meperidines) |
- 4-Fluoropethidine
- Allylnorpethidine
- Anileridine
- Benzethidine
- Carperidine
- Difenoxin
- Diphenoxylate
- Etoxeridine (Carbetidine)
- Furethidine
- Hydroxypethidine (Bemidone)
- Morpheridine
- Oxpheneridine (Carbamethidine)
- Pethidine (Meperidine)
- Pethidine intermediate A
- Pethidine intermediate B (Norpethidine)
- Pethidine intermediate C (Pethidinic Acid)
- Pheneridine
- Phenoperidine
- Piminodine
- Properidine (Ipropethidine)
- Sameridine
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Prodines |
- Allylprodine
- Meprodine (α-meprodine / β-meprodine)
- MPPP (Desmethylprodine)
- PEPAP
- Prodine (α-prodine / β-prodine)
- Prosidol
- Trimeperidine (Promedol)
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Ketobemidones |
- Acetoxyketobemidone
- Droxypropine
- Ketobemidone
- Methylketobemidone
- Propylketobemidone
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Others |
- Alvimopan
- Loperamide
- Picenadol
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Open chain
opioids |
Amidones |
- Dipipanone
- Isomethadone
- Levomethadone
- Methadone
- Normethadone
- Norpipanone
- Phenadoxone (Heptazone)
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Methadols |
- Acetylmethadol
- Alphacetylmethadol
- Alphamethadol
- Betacetylmethadol
- Betamethadol
- Dimepheptanol (methadol)
- Isomethadol
- Levacetylmethadol
- Noracymethadol
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Moramides |
- Desmethylmoramide
- Dextromoramide
- Levomoramide
- Moramide/Racemoramide
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Thiambutenes |
- Diethylthiambutene
- Dimethylthiambutene
- Ethylmethylthiambutene
- Piperidylthiambutene
- Pyrrolidinylthiambutene
- Tipepidine
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Phenalkoxams |
- Dextropropoxyphene
- Dimenoxadol
- Dioxaphetyl butyrate
- Levopropoxyphene
- Norpropoxyphene
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Ampromides |
- Diampromide
- Phenampromide
- Propiram
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Others |
- Alimadol
- IC-26
- Isoaminile
- Lefetamine
- R-4066
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Anilidopiperidines |
- 3-Allylfentanyl
- 3-Methylfentanyl
- 3-Methylthiofentanyl
- 4-Phenylfentanyl
- α-Methylacetylfentanyl
- α-Methylfentanyl
- α-methylthiofentanyl
- β-hydroxyfentanyl
- β-hydroxythiofentanyl
- β-methylfentanyl
- Alfentanil
- Brifentanil
- Carfentanil
- Fentanyl
- Lofentanil
- Mirfentanil
- Ocfentanil
- Ohmefentanyl
- Parafluorofentanyl
- Phenaridine
- Remifentanil
- Sufentanil
- Thiofentanyl
- Trefentanil
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Oripavine
derivatives |
- 7-PET
- Acetorphine
- Alletorphine
- BU-48
- Buprenorphine
- Cyprenorphine
- Dihydroetorphine
- Etorphine
- Homprenorphine
- Norbuprenorphine
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Phenazepanes |
- Ethoheptazine
- Meptazinol
- Metethoheptazine
- Metheptazine
- Proheptazine
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Pirinitramides |
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Benzimidazoles |
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Indoles |
- 18-MC
- 7-Hydroxymitragynine
- Akuammine
- Eseroline
- Hodgkinsine
- Ibogaine
- Mitragynine
- Noribogaine
- Pericine
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Diphenylmethyl-
piperazines |
- BW373U86
- DPI-221
- DPI-287
- DPI-3290
- SNC-80
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Opioid peptides |
- Adrenorphin
- Amidorphin
- Biphalin
- Casokefamide
- Casomorphin
- Cytochrophin
- DADLE
- DAMGO
- Deltorphin
- Dermorphin
- Dynorphin
- Endomorphin
- Endorphins
- Enkephalin
- Frakefamide
- Gliadorphin
- Hemorphin
- Leumorphin
- Metkefamide
- Morphiceptin
- Neoendorphin
- Nociceptin
- Octreotide
- Opiorphin
- Rubiscolin
- Spinorphin
- TRIMU 5
- Tynorphin
- Valorphin
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Others |
- AD-1211
- AH-7921
- Azaprocin
- BRL-52537
- Bromadol
- Bromadoline
- C-8813
- Ciprefadol
- Ciramadol
- Doxpicomine
- Enadoline
- Faxeladol
- GR-89696
- Herkinorin
- ICI-199,441
- ICI-204,448
- J-113,397
- JTC-801
- LPK-26
- MCOPPB
- Metofoline
- MT-45
- N-Desmethylclozapine
- NNC 63-0532
- Nortilidine
- O-Desmethyltramadol
- Phenadone
- Phencyclidine
- Prodilidine
- Profadol
- Ro64-6198
- Salvinorin A
- SB-612,111
- SC-17599
- RWJ-394,674
- TAN-67
- Tapentadol
- Tifluadom
- Tilidine
- Tramadol
- Trimebutine
- U-50,488
- U-69,593
- Viminol
- W-18
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Opioid
antagonists &
inverse agonists |
- 5'-Guanidinonaltrindole
- Alvimopan
- Chlornaltrexamine
- Chloroxymorphamine
- Conorfone
- Cyclazocine
- Cyprodime
- Diacetylnalorphine
- Difenamizole
- Diprenorphine (M5050)
- Gemazocine
- JDTic
- Levallorphan
- LY-255,582
- Methylnaltrexone
- Nalbuphine
- Naldemedine
- Nalmefene
- Nalmexone
- Nalorphine
- Nalorphine dinicotinate
- Naloxazone
- Naloxegol
- Naloxonazine
- Naloxone
- Naltrexol-d4
- Naltrexone
- Naltriben
- Naltrindole
- Norbinaltorphimine
- Oxilorphan
- Quadazocine
- Samidorphan
- Tonazocine
- Zenazocine
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Biased ligands |
- TRV130
- Herkinorin
- 6'-GNTI
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Uncategorized
opioids |
- Anilopam
- Asimadoline
- Axomadol
- FE 200665
- Fedotozine
- Nalfurafine
- Nalorphine
- Nalorphine dinicotinate
- SoRI-9409
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UpToDate Contents
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English Journal
- LCZ696, Angiotensin II Receptor-Neprilysin Inhibitor, Ameliorates High-Salt-Induced Hypertension and Cardiovascular Injury More Than Valsartan Alone.
- Kusaka H1, Sueta D1, Koibuchi N1, Hasegawa Y1, Nakagawa T1, Lin B1, Ogawa H2, Kim-Mitsuyama S3.
- American journal of hypertension.Am J Hypertens.2015 Dec;28(12):1409-17. doi: 10.1093/ajh/hpv015. Epub 2015 Mar 10.
- BACKGROUND: LCZ696, an angiotensin receptor-neprilysin inhibitor, has recently been demonstrated to exert more beneficial effects on hypertensive or heart failure patients than conventional renin-angiotensin system blockers. However, the mechanism underlying the benefit of LCZ696 remains to be under
- PMID 25762811
- Influence of polar side chains modifications on the dual enkephalinase inhibitory activity and conformation of human opiorphin, a pain perception related peptide.
- Rosa M1, Marcelo F2, Calle LP3, Rougeot C4, Jiménez-Barbero J5, Arsequell G1, Valencia G1.
- Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2015 Nov 15;25(22):5190-3. doi: 10.1016/j.bmcl.2015.09.071. Epub 2015 Oct 14.
- The dual inhibitory action of the pain related peptide opiorphin (H-Gln-Arg-Phe-Ser-Arg-OH) against neutral endopeptidase (NEP) and aminopeptidase N (AP-N) was further investigated by a SAR study involving minor modifications on the polar side chains of Arg residues and glycosylation with monosaccha
- PMID 26463133
- Comparing LCZ696 With Enalapril According to Baseline Risk Using the MAGGIC and EMPHASIS-HF Risk Scores: An Analysis of Mortality and Morbidity in PARADIGM-HF.
- Simpson J1, Jhund PS1, Silva Cardoso J2, Martinez F3, Mosterd A4, Ramires F5, Rizkala AR6, Senni M7, Squire I8, Gong J6, Lefkowitz MP6, Shi VC6, Desai AS9, Rouleau JL10, Swedberg K11, Zile MR12, McMurray JJ13, Packer M14, Solomon SD9; PARADIGM-HF Investigators and Committees.
- Journal of the American College of Cardiology.J Am Coll Cardiol.2015 Nov 10;66(19):2059-71. doi: 10.1016/j.jacc.2015.08.878.
- BACKGROUND: Although most patients in the PARADIGM-HF (Prospective Comparison of ARNI With ACEI to Determine Impact on Global Mortality and Morbidity in Heart Failure) trial had mild symptoms, there is a poor correlation between reported functional limitation and prognosis in heart failure.OBJECTIVE
- PMID 26541915
Japanese Journal
- Behavioral Effects of δ-Opioid Receptor Agonists: Potential Antidepressants?
- Broom Daniel C.,Jutkiewicz Emily M.,Rice Kenner C. [他],TRAYNOR John R.,WOODS James H.
- The Japanese journal of pharmacology 90(1), 1-6, 2002-09-01
- … Also, enkephalinase inhibitors, which prevent the degradation of endogenous enkephalins, produced antidepressant-like effects mediated through the δ-opioid receptor in animal models of depression. …
- NAID 130000078441
- Dynorphin A Processing Enzyme: Tissue Distribution, Isolation, and Characterization.
- Berman Yemiliya,Ageyeva Lyudmila,Veksler Boris,Wood David,Devi Lakshmi A.
- The Journal of Biochemistry 125(3), 641-647, 1999
- … Specific inhibitors of other metallopeptidases such as enkephalinase [EC 3. …
- NAID 130003417905
- Antinociceptive and Antidepressant-Like Profiles of BL-2401, a Novel Enkephalinase Inhibitor, in Mice and Rats
- Kita Atsuko,Imano Kiyomi,Seto Yasuhiro [他],YAKUO Ikuhisa,DEGUCHI Takashi,NAKAMURA Hideo
- The Japanese journal of pharmacology 75(4), 337-346, 1997-12-01
- … To clarify the properties of BL-2401 ((±)-3-[2-benzyl-3-(propionylthio) propionyl]amino-5methylbenzoic acid), a novel enkephalinase inhibitor, we examined its antinociceptive and antidepressantlike activities after oral administration, along with their association with endogenous opioid systems. … As for the mechanism of the action, the active metabolite of BL-2401, BL-2240 ((±)-3-(2-benzyl-3-mercaptopropionyl) amino-5-methylbenzoic acid), selectively inhibited enkephalinase in vitro (IC<SUB>50</SUB>: 5.2 nM). …
- NAID 10008190367
Related Links
- enkephalinase (en-kef'a-lin-āz), Membrane metalloendopeptidase, enzyme that breaks down circulating enkephalins and other peptides. ... Indianapolis, IN) included amino acid precursors such as L-phenylalanine, l-tyrosine, L ...
- Inhibitors of enkephalin-degrading enzymes are exciting prospects for the future ... Antinociceptive and antidepressant-like profiles of BL-2401, a novel enkephalinase inhibitor, in mice and rats by Kita A, Imano K, Seto Y, Yakuo I ...
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★リンクテーブル★
[★]
- 英
- enkephalinase
- 関
- エンケファリン分解酵素、ネプリライシン、中性エンドペプチダーゼ
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ネプリライシン
- 関
- enkephalinase、neutral endopeptidase
- 同
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[★]
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- enkephalinase、neprilysin
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[★]
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