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The Info List - Ubenimex





Ubenimex
Ubenimex
(INN), also known more commonly as bestatin, is a competitive, reversible protease inhibitor. It is an inhibitor of arginyl aminopeptidase (aminopeptidase B),[2] leukotriene A4 hydrolase (a zinc metalloprotease that displays both epoxide hydrolase and aminopeptidase activities),[3] alanyl aminopeptidase (aminopeptidase M/N),[4] leucyl/cystinyl aminopeptidase (oxytocinase/vasopressinase),[5][6] and membrane dipeptidase (leukotriene D4 hydrolase). It is being studied for use in the treatment of acute myelocytic leukemia[7] and lymphedema[8]. It is derived from Streptomyces olivoreticuli.[9] Ubenimex
Ubenimex
has been found to inhibit the enzymatic degradation of oxytocin, vasopressin, enkephalins, and various other peptides and compounds.[citation needed]

Crystal structure of ubenimex in the binding pocket of leukotriene A4 hydrolase. Rendered from PDB 1HS6.

See also[edit]

Amastatin Pepstatin

References[edit]

^ N-((2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl)-L-leucine at Sigma-Aldrich ^ Umezawa, H.; Aoyagi, T.; Suda, H.; Hamada, M.; Takeuchi, T. (1976). "Bestatin, an inhibitor of aminopeptidase B, produced by actinomycetes" (29): 97–99.  ^ Muskardin, D.T.; Voelkel, N.F.; Fitzpatrick, F.A. (1994). "Modulation of pulmonary leukotriene formation and perfusion pressure by Bestatin, an inhibitor of leukotriene A4 hydrolase" (48): 131–137.  ^ K Sekine; H Fujii; F Abe (1999). "Induction of apoptosis by Bestatin (ubenimex) in human leukemic cell lines". 13 (5): 729–734. doi:10.1038/sj.leu.2401388.  ^ Nakanishi Y, Nomura S, Okada M, Ito T, Katsumata Y, Kikkawa F, Hattori A, Tsujimoto M, Mizutani S (2000). "Immunoaffinity purification and characterization of native placental leucine aminopeptidase/oxytocinase from human placenta". Placenta. 21 (7): 628–34. doi:10.1053/plac.2000.0564. PMID 10985965.  ^ Naruki M, Mizutani S, Goto K, Tsujimoto M, Nakazato H, Itakura A, Mizuno K, Kurauchi O, Kikkawa F, Tomoda Y (1996). " Oxytocin
Oxytocin
is hydrolyzed by an enzyme in human placenta that is identical to the oxytocinase of pregnancy serum". Peptides. 17 (2): 257–61. doi:10.1016/0196-9781(95)02124-8. PMID 8801531.  ^ Hirayama, Y; Sakamaki, S; Takayanagi, N; Tsuji, Y; Sagawa, T; Chiba, H; Matsunaga, T; Niitsu, Y (2003). "Chemotherapy with ubenimex corresponding to patient age and organ disorder for 18 cases of acute myelogeneous leukemia in elderly patients--effects, complications and long-term survival". Gan to kagaku ryoho. Cancer & chemotherapy. 30 (8): 1113–8. PMID 12938265.  ^ Tian, W; Rockson, S; Jiang, X; Kim, J; Begaye, A; Shuffle, EM; Tu, AB; Cribb, M; Nepiyushchikh, Z; Feroze, AH; Zamanian, RT; Dhillon, RT; Voelkel, NF; Peters-Golden, M; Kitajewski, J; Dixon, JB; Nicolls, MR (2017). " Leukotriene
Leukotriene
B4 antagonism ameliorates experimental lymphedema". Science Translational Medicine. 9 (389): eaal3920. doi:10.1126/scitranslmed.aal3920. PMID 28490670.  ^ Bauvois, B; Dauzonne, D (January 2006). "Aminopeptidase-N/CD13 (EC 3.4.11.2) inhibitors: Chemistry, biological evaluations, and therapeutic prospects". Medicinal Research Reviews. 26 (1): 88–130. doi:10.1002/med.20044. PMID 16216010. 

External links[edit]

The MEROPS
MEROPS
online database for peptidases and their inhibitors: Bestatin

v t e

Leukotriene
Leukotriene
signaling modulators

Receptor (ligands)

BLT

BLT1

Agonists: 12-HETE 20-Hydroxy-LTB4 Leukotriene
Leukotriene
B4 LY-255283

Antagonists: 20-Carboxy-LTB4 Amelubant CGS-23131 (LY-223982) CGS-25019C CP-105696 CP-195543 Etalocib LY-293111 Moxilubant ONO-4057 RG-14893 RP-69698 SB-209247 SC-53228 Ticolubant U-75302 ZK-158252

BLT2

Agonists: 12-HETE 12-HHT 12-HpETE 15-HETE 15-HpETE 20-Hydroxy-LTB4 Leukotriene
Leukotriene
B4

Antagonists: CP-195543 LY-255283 ZK-158252

CysLT

CysLT1

Agonists: Leukotriene
Leukotriene
C4 Leukotriene
Leukotriene
D4 Leukotriene
Leukotriene
E4

Antagonists: Ablukast BAYu9773 BAYu9916 BAYx7195 Cinalukast FPL-55712 ICI-198615 Iralukast LY-170680 Masilukast MK-571 Montelukast ONO-1078 Pobilukast Pranlukast Ritolukast SKF-104353 SR-2640 Sulukast Tipelukast Tomelukast Verlukast Zafirlukast ZD-3523

CysLT2

Agonists: Leukotriene
Leukotriene
C4 Leukotriene
Leukotriene
D4 Leukotriene
Leukotriene
E4

Antagonists: BAYu9773 BAYu9916

CysLTE

Agonists: Leukotriene
Leukotriene
E4

Enzyme (inhibitors)

5-LOX

2-TEDC Baicalein BW-A4C BW-B70C Caffeic acid CDC CJ-13610 Curcumin Fenleuton Hyperforin Hypericum perforatum
Hypericum perforatum
(St. John's Wort) Meclofenamic acid
Meclofenamic acid
(meclofenamate) Minocycline N-Stearoyldopamine Timegadine Zileuton

FLAP inhibitors: AM-103 AM-679 BAYx1005 MK-591 MK-886

12-LOX

2-TEDC 3-Methoxytropolone Baicalein CDC

15-LOX

2-TEDC CDC Luteolin PD-146176

LTA4H

Acebilustat Captopril DG-051 Fosinoprilat JNJ-26993135 SA-6541 SC-57461A Ubenimex
Ubenimex
(bestatin)

LTB4H

17-Octadecynoic acid

LTC4S

Azelastine MK-886

LTC4H

Acivicin Serine-borate complex

LTD4

Cilastatin Ubenimex
Ubenimex
(bestatin)

Others

Precursors: Linoleic acid γ-Linolenic acid (gamolenic acid) Dihomo-γ-linolenic acid Diacylglycerol Arachidonic acid 5-HPETE (arachidonic acid 5-hydroperoxide) Leukotriene
Leukotriene
A4

See also Receptor/signaling modulators Prostanoid signaling modulators Nuclear receptor modulators

v t e

Signaling peptide/protein receptor modulators

Adiponectin

AdipoR1

Agonists: Peptide: Adiponectin ADP-355 ADP-399; Non-peptide: AdipoRon (–)-Arctigenin Arctiin Gramine Matairesinol

Antagonists: Peptide: ADP-400

AdipoR2

Agonists: Peptide: Adiponectin ADP-355 ADP-399; Non-peptide: AdipoRon Deoxyschizandrin Parthenolide Syringing Taxifoliol

Antagonists: Peptide: ADP-400

Angiotensin

See here instead.

Bradykinin

Agonists: Bradykinin Kallidin

Antagonists: FR-173657 Icatibant LF22-0542

CGRP

Agonists: Amylin CGRP Pramlintide

Antagonists: Atogepant BI 44370 TA CGRP (8-37) MK-3207 Olcegepant Rimegepant SB-268262 Telcagepant Ubrogepant

Antibodies: Eptinezumab Erenumab Fremanezumab Galcanezumab

Cholecystokinin

CCKA

Agonists: Cholecystokinin

Antagonists: Amiglumide Asperlicin Devazepide Dexloxiglumide Lintitript Lorglumide Loxiglumide Pranazepide Proglumide Tarazepide Tomoglumide

CCKB

Agonists: Cholecystokinin CCK-4 Gastrin Pentagastrin
Pentagastrin
(CCK-5)

Antagonists: Ceclazepide CI-988
CI-988
(PD-134308) Itriglumide L-365,360 Netazepide Proglumide Spiroglumide

Unsorted

Antagonists: Nastorazepide

CRH

CRF1

Agonists: Cortagine Corticorelin Corticotropin releasing hormone Sauvagine Stressin I Urocortin

Antagonists: Antalarmin Astressin-B CP-154,526 Emicerfont Hypericin LWH-234 NBI-27914 Pexacerfont R-121919 TS-041 Verucerfont

CRF2

Agonists: Corticorelin Corticotropin releasing hormone Sauvagine Urocortin

Antagonists: Astressin-B

Cytokine

See here instead.

Endothelin

Agonists: Endothelin 1 Endothelin 2 Endothelin 3 IRL-1620

Antagonists: A-192621 ACT-132577 Ambrisentan Aprocitentan Atrasentan Avosentan Bosentan BQ-123 BQ-788 Clazosentan Darusentan Edonentan Enrasentan Fandosentan Feloprentan Macitentan Nebentan Sitaxentan Sparsentan Tezosentan Zibotentan

Galanin

GAL1

Agonists: Galanin Galanin
Galanin
(1-15) Galanin-like peptide Galmic Galnon NAX 810-2

Antagonists: C7 Dithiepine-1,1,4,4-tetroxide Galantide (M15) M32 M35 M40 SCH-202596

GAL2

Agonists: Galanin Galanin
Galanin
(1-15) Galanin
Galanin
(2-11) Galanin-like peptide Galmic Galnon J18 NAX 810-2

Antagonists: C7 Galantide (M15) M32 M35 M40 M871

GAL3

Agonists: Galanin Galanin
Galanin
(1-15) Galmic Galnon

Antagonists: C7 Galantide (M15) GalR3ant HT-2157 M32 M35 M40 SNAP-37889 SNAP-398299

Ghrelin/GHS

See here instead.

GH

See here instead.

GHRH

See here instead.

GLP

GLP-1

Agonists: Albiglutide Beinaglutide Dulaglutide Efpeglenatide Exenatide GLP-1 Langlenatide Liraglutide Lixisenatide Oxyntomodulin Semaglutide Taspoglutide

GLP-2

Agonists: Apraglutide Elsiglutide Glepaglutide GLP-2 Teduglutide

Others

Propeptides: Preproglucagon Proglucagon

Glucagon

Agonists: Dasiglucagon Glucagon Oxyntomodulin

Antagonists: Adomeglivant L-168,049 LGD-6972

Propeptides: Preproglucagon Proglucagon

GnRH

See here instead.

Gonadotropin

See here instead.

Growth factor

See here instead.

Insulin

Agonists: Chaetochromin
Chaetochromin
(4548-G05) Insulin-like growth factor 1 Insulin-like growth factor 2 Insulin Insulin
Insulin
aspart Insulin
Insulin
degludec Insulin
Insulin
detemir Insulin
Insulin
glargine Insulin
Insulin
glulisine Insulin
Insulin
lispro Mecasermin Mecasermin
Mecasermin
rinfabate

Antagonists: BMS-754807 S661 S961

Kinase inhibitors: Linsitinib

Antibodies: Xentuzumab (against IGF-1 and IGF-2)

Kisspeptin

Agonists: Kisspeptin Kisspeptin-10

Antagonists: Kisspeptin-234

Leptin

Agonists: Leptin Metreleptin

MCH

MCH1

Agonists: Melanin concentrating hormone

Antagonists: ATC-0065 ATC-0175 GW-803430 NGD-4715 SNAP-7941 SNAP-94847

MCH2

Agonists: Melanin concentrating hormone

Melanocortin

See here instead.

Neuropeptide FF

Agonists: Neuropeptide AF Neuropeptide FF Neuropeptide SF (RFRP-1) Neuropeptide VF (RFRP-3)

Antagonists: BIBP-3226 RF9

Neuropeptide S

Agonists: Neuropeptide S

Antagonists: ML-154 SHA-68

Neuropeptide Y

Y1

Agonists: Neuropeptide Y Peptide
Peptide
YY

Antagonists: BIBO-3304 BIBP-3226 BVD-10 GR-231118 PD-160170

Y2

Agonists: 2-Thiouridine 5'-triphosphate Neuropeptide Y Neuropeptide Y
Neuropeptide Y
(13-36) Peptide
Peptide
YY Peptide
Peptide
YY (3-36)

Antagonists: BIIE-0246 JNJ-5207787 SF-11

Y4

Agonists: GR-231118 Neuropeptide Y Pancreatic polypeptide Peptide
Peptide
YY

Antagonists: UR-AK49

Y5

Agonists: BWX-46 Neuropeptide Y Peptide
Peptide
YY

Antagonists: CGP-71683 FMS-586 L-152,804 Lu AA-33810 MK-0557 NTNCB Velneperit
Velneperit
(S-2367)

Neurotensin

NTS1

Agonists: Neurotensin Neuromedin N

Antagonists: Meclinertant SR-142948

NTS2

Agonists: Neurotensin

Antagonists: Levocabastine SR-142948

Opioid

See here instead.

Orexin

OX1

Agonists: Orexin
Orexin
(A, B)

Antagonists: ACT-335827 ACT-462206 Almorexant Filorexant Lemborexant SB-334867 SB-408124 SB-649868 Suvorexant TCS-1102

OX2

Agonists: Orexin
Orexin
(A, B) SB-668875

Antagonists: ACT-335827 ACT-462206 Almorexant EMPA Filorexant JNJ-10397049 Lemborexant MK-1064 SB-649868 Seltorexant Suvorexant TCS-1102 TCS-OX2-29

Oxytocin

See here instead.

Prolactin

Agonists: Growth hormone Human placental lactogen Placental growth hormone
Placental growth hormone
(growth hormone variant) Prolactin S179D-hPRL Somatotropin

Antagonists: Δ1–9-G129R-hPRL Δ1–14-G129R-hPRL G120K-hGH G129R-hPRL

Prolactin
Prolactin
modulators: Prolactin
Prolactin
inhibitors: D2 receptor
D2 receptor
agonists (e.g., bromocriptine, cabergoline); Prolactin
Prolactin
releasers: D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) Estrogens (e.g., estradiol) Progestogens (e.g., progesterone)

PTH

Agonists: Abaloparatide Parathyroid hormone Parathyroid hormone-related protein
Parathyroid hormone-related protein
(PTHrP) Semparatide Teriparatide

Relaxin

Agonists: Insulin-like factor 3 Relaxin
Relaxin
(1, 2, 3) Serelaxin

Somatostatin

See here instead.

Tachykinin

See here instead.

TRH

Agonists: Azetirelin Fertirelin Montirelin Orotirelin Posatirelin Protirelin Rovatirelin Taltirelin TRH (TRF)

TSH

Agonists: Thyrotropin alfa TSH (thyrotropin)

Vasopressin

See here instead.

VIP/PACAP

VIPR1

Agonists: Peptide: Bay 55-9837 LBT-3393 PACAP VIP

VIPR2

Agonists: Peptide: LBT-3627 PACAP VIP

PAC1

Agonists: PACAP PACAP (1-27) PACAP (1-38)

Antagonists: PACAP (6-38)

Unsorted

PHI PHM PHV

Others

Endogenous: Adrenomedullin Apelin Asprosin Bombesin Calcitonin Carnosine CART CLIP DSIP Enteroglucagon Formyl peptide GALP GIP GRP Integrin
Integrin
ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) Kininogens Motilin Natriuretic peptides (ANP, BNP, CNP, urodilatin) Nesfatin-1 Neuromedin B Neuromedin N Neuromedin S Neuromedin U Obestatin Osteocalcin Resistin Secretin Thymopoietin Thymosins Thymulin Urotensin-II VGF

Exogenous: Lifitegrast
Lifitegrast
(LFA-1 antagonist)

See also Receptor/signaling modulators

v t e

Opioid receptor
Opioid receptor
modulators

MOR

Agonists (abridged; see here for a full list): 3-HO-PCP 7-Acetoxymitragynine 7-Hydroxymitragynine ψ-Akuammigine α-Chlornaltrexamine α-Narcotine Acetyldihydrocodeine Acetylfentanyl Acrylfentanyl Adrenorphin
Adrenorphin
(metorphamide) AH-7921 Akuammicine Akuammidine Alfentanil Anileridine Apparicine β-Endorphin BAM-12P BAM-18P BAM-22P Benzhydrocodone Benzylmorphine Bezitramide Biphalin BU08070 Buprenorphine Butorphan Butorphanol Butyrfentanyl BW-373U86 Carfentanil Casokefamide Cebranopadol Chloroxymorphamine Codeine DADLE DAMGO
DAMGO
(DAGO) Dermorphin Desmetramadol
Desmetramadol
(desmethyltramadol) Desomorphine Dextromoramide Dextropropoxyphene
Dextropropoxyphene
(propoxyphene) Dezocine Dimenoxadol Dimethylaminopivalophenone Eluxadoline Diamorphine (heroin) Dihydrocodeine Dihydroetorphine Dihydromorphine Diphenoxylate Dipipanone Dynorphin A Embutramide Endomorphin-1 Endomorphin-2 Eseroline Ethylmorphine Etorphine Fentanyl Fluorophen Frakefamide Furanylfentanyl Hemorphin-4 Herkinorin Hodgkinsine Hydrocodone Hydromorphinol Hydromorphone IBNtxA Ketamine Ketobemidone Kratom Laudanosine Lefetamine Leu-enkephalin Levacetylmethadol Levomethorphan Levorphanol Lexanopadol Loperamide Loxicodegol Matrine Meptazinol Met-enkephalin
Met-enkephalin
(metenkefalin) Methadone Metkefamide Metopon Mitragynine Mitragynine
Mitragynine
pseudoindoxyl Morphiceptin Morphine Nalbuphine Nalbuphine
Nalbuphine
sebacate NalBzOH Nalmexone Naltalimide Neopine NFEPP Nicocodeine Nicodicodeine Nicomorphine NKTR-181 Norketamine Octreotide Oliceridine OM-3-MNZ Oripavine Oxycodone Oxymorphazone Oxymorphonazine Oxymorphone Oxymorphone
Oxymorphone
phenylhydrazone OxyPNPH Papaver somniferum
Papaver somniferum
(opium) Pentazocine Pericine Pethidine
Pethidine
(meperidine) Phenazocine Phencyclidine Piminodine Piritramide PL-017 Prodine Propiram PZM21 Racemethorphan Racemorphan Remifentanil Salsolinol SC-17599 Sinomenine Sufentanil Tapentadol Tetrahydropapaveroline TH-030418 Thebaine Thienorphine Tianeptine Tilidine Tramadol Trimebutine TRIMU 5 TRV734 Tubotaiwine U-47700 Valorphin Viminol Xorphanol

PAMs: BMS-986121 BMS-986122

Antagonists: (3S,4S)-Picenadol 2-(S)-N,N-(R)-Viminol 3CS-nalmefene 4-Caffeoyl-1,5-quinide 4′-Hydroxyflavanone 4',7-Dihydroxyflavone 6β-Naltrexol 6β-Naltrexol-d4 18-MC α-Gliadin β-Chlornaltrexamine β-Funaltrexamine Akuammine Alvimopan AM-251 Apigenin AT-076 Axelopran Bevenopran Catechin Catechin
Catechin
gallate Clocinnamox CTAP CTOP Cyclofoxy Cyprodime Diacetylnalorphine Diprenorphine ECG EGC Epicatechin Eptazocine Gemazocine Ginsenoside R Hyperoside Ibogaine Levallorphan Lobeline LY-255582 LY-2196044 Methocinnamox Methylnaltrexone Methylsamidorphan chloride Naldemedine Nalmefene Nalodeine
Nalodeine
(N-allylnorcodeine) Nalorphine Nalorphine
Nalorphine
dinicotinate Naloxazone Naloxegol Naloxol Naloxonazine Naloxone Naltrexazone Naltrexonazine Naltrexone Naltrindole Naringenin Noribogaine Oxilorphan Pawhuskin A Rimonabant Quadazocine Samidorphan Taxifolin

Unknown/unsorted: Cannabidiol Coronaridine Cyproterone acetate Dihydroakuuamine Tabernanthine Tetrahydrocannabinol

DOR

Agonists: 3CS-nalmefene 6'-GNTI 7-SIOM ADL-5747 (PF-04856881) ADL-5859 Alazocine
Alazocine
(SKF-10047) Amoxapine AR-M100390 (ARM390) AZD2327 β-Endorphin BAM-18P Biphalin BU-48 Butorphan Butorphanol BW-373U86 Casokefamide Cebranopadol Codeine Cyclazocine DADLE Deltorphin
Deltorphin
A Deltorphin
Deltorphin
I Deltorphin
Deltorphin
II Desmethylclozapine Desmetramadol
Desmetramadol
(desmethyltramadol) Dezocine Diamorphine (heroin) Dihydroetorphine Dihydromorphine DPDPE DPI-221 DPI-3290 DSLET Ethylketazocine Etorphine Fentanyl FIT Fluorophen Hemorphin-4 Hydrocodone Hydromorphone Ibogaine Isomethadone JNJ-20788560 KNT-127 Kratom Laudanosine Leu-enkephalin Levomethorphan Levorphanol Lexanopadol Lofentanil Met-enkephalin
Met-enkephalin
(metenkefalin) Metazocine Metkefamide Mitragynine Mitragynine
Mitragynine
pseudoindoxyl Morphine N-Phenethyl-14-ethoxymetopon Norbuprenorphine NalBzOH Oripavine Oxycodone Oxymorphone Pethidine
Pethidine
(meperidine) Proglumide Racemethorphan Racemorphan RWJ-394674 Samidorphan SB-235863 SNC-80 SNC-162 TAN-67
TAN-67
(SB-205,607) TH-030418 Thebaine Thiobromadol
Thiobromadol
(C-8813) Tonazocine Tramadol TRV250 Xorphanol Zenazocine

Antagonists: 4',7-Dihydroxyflavone 5'-NTII 6β-Naltrexol 6β-Naltrexol-d4 α-Santolol β-Chlornaltrexamine Apigenin AT-076 Axelopran Bevenopran BNTX Catechin Catechin
Catechin
gallate Clocinnamox Diacetylnalorphine Diprenorphine ECG EGC Eluxadoline Epicatechin ICI-154129 ICI-174864 LY-255582 LY-2196044 Methylnaltrexone Methylnaltrindole N-Benzylnaltrindole Nalmefene Nalorphine Naltrexone Naltriben Naltrindole Naloxone Naringenin Noribogaine Pawhuskin A Quadazocine SDM25N SoRI-9409 Taxifolin Thienorphine

Unknown/unsorted: 18-MC Cannabidiol Coronaridine Cyproterone acetate Tabernanthine Tetrahydrocannabinol

KOR

Agonists: 3CS-nalmefene 6'-GNTI 8-CAC 18-MC 14-Methoxymetopon β-Chlornaltrexamine β-Funaltrexamine Adrenorphin
Adrenorphin
(metorphamide) Akuuamicine Alazocine
Alazocine
(SKF-10047) Allomatrine Apadoline Asimadoline BAM-12P BAM-18P BAM-22P Big dynorphin Bremazocine BRL-52537 Butorphan Butorphanol BW-373U86 Cebranopadol Ciprefadol CR665 Cyclazocine Cyclorphan Cyprenorphine Desmetramadol
Desmetramadol
(desmethyltramadol) Diamorphine (heroin) Diacetylnalorphine Difelikefalin Dihydroetorphine Dihydromorphine Diprenorphine Dynorphin A Dynorphin B
Dynorphin B
(rimorphin) Eluxadoline Enadoline Eptazocine Erinacine E Ethylketazocine Etorphine Fedotozine Fentanyl Gemazocine GR-89696 GR-103545 Hemorphin-4 Herkinorin HS665 Hydromorphone HZ-2 Ibogaine ICI-199,441 ICI-204,448 Ketamine Ketazocine Laudanosine Leumorphin (dynorphin B-29) Levallorphan Levomethorphan Levorphanol Lexanopadol Lofentanil LPK-26 Lufuradom Matrine MB-1C-OH Menthol Metazocine Metkefamide Mianserin Mirtazapine Morphine Moxazocine MR-2034 N-MPPP Nalbuphine Nalbuphine
Nalbuphine
sebacate NalBzOH Nalfurafine Nalmefene Nalodeine
Nalodeine
(N-allylnorcodeine) Nalorphine Naltriben Niravoline Norbuprenorphine Norbuprenorphine-3-glucuronide Noribogaine Norketamine Oripavine Oxilorphan Oxycodone Pentazocine Pethidine
Pethidine
(meperidine) Phenazocine Proxorphan Racemethorphan Racemorphan RB-64 Salvinorin A
Salvinorin A
(salvia) Salvinorin B ethoxymethyl ether Salvinorin B methoxymethyl ether Samidorphan Spiradoline
Spiradoline
(U-62,066) TH-030418 Thienorphine Tifluadom Tricyclic antidepressants (e.g., amitriptyline, desipramine, imipramine, nortriptyline) U-50,488 U-54,494A U-69,593 Xorphanol

Antagonists: 4′-Hydroxyflavanone 4',7-Dihydroxyflavone 5'-GNTI 6'-GNTI 6β-Naltrexol 6β-Naltrexol-d4 β-Chlornaltrexamine Buprenorphine/samidorphan Amentoflavone ANTI Apigenin Arodyne AT-076 Axelopran AZ-MTAB Binaltorphimine BU09059 Buprenorphine Catechin Catechin
Catechin
gallate CERC-501
CERC-501
(LY-2456302) Clocinnamox Cyclofoxy Dezocine DIPPA EGC ECG Epicatechin Hyperoside JDTic LY-255582 LY-2196044 LY-2444296 LY-2459989 LY-2795050 MeJDTic Methylnaltrexone ML190 ML350 MR-2266 N-Fluoropropyl-JDTic Naloxone Naltrexone Naltrindole Naringenin Norbinaltorphimine Noribogaine Pawhuskin A PF-4455242 RB-64 Quadazocine Taxifolin UPHIT Zyklophin

Unknown/unsorted: Akuammicine Akuammine Coronaridine Cyproterone acetate Dihydroakuuamine Ibogamine Tabernanthine

NOP

Agonists: (Arg14,Lys15)Nociceptin ((pF)Phe4)Nociceptin(1-13)NH2 (Phe1Ψ(CH2-NH)Gly2)Nociceptin(1-13)NH2 Ac-RYYRWK-NH2 Ac-RYYRIK-NH2 BU08070 Buprenorphine Cebranopadol Dihydroetorphine Etorphine JNJ-19385899 Levomethorphan Levorphanol Levorphanol Lexanopadol MCOPPB MT-7716 NNC 63-0532 Nociceptin
Nociceptin
(orphanin FQ) Nociceptin
Nociceptin
(1-11) Nociceptin
Nociceptin
(1-13)NH2 Norbuprenorphine Racemethorphan Racemorphan Ro64-6198 Ro65-6570 SCH-221510 SCH-486757 SR-8993 SR-16435 TH-030418

Antagonists: (Nphe1)Nociceptin(1-13)NH2 AT-076 BAN-ORL-24 BTRX-246040
BTRX-246040
(LY-2940094) J-113397 JTC-801 NalBzOH Nociceptin
Nociceptin
(1-7) Nocistatin SB-612111 SR-16430 Thienorphine Trap-101 UFP-101

Unsorted

β-Casomorphins Amidorphin BAM-20P Cytochrophin-4 Deprolorphin Gliadorphin
Gliadorphin
(gluteomorphin) Gluten exorphins Hemorphins Kava
Kava
constituents MEAGL MEAP NEM Neoendorphins Nepetalactone
Nepetalactone
(catnip) Peptide
Peptide
B Peptide
Peptide
E Peptide
Peptide
F Peptide
Peptide
I Rubiscolins Soymorphins

Others

Enkephalinase inhibitors: Amastatin BL-2401 Candoxatril D -Phenylalanine Dexecadotril (retorphan) Ecadotril
Ecadotril
(sinorphan) Kelatorphan Racecadotril
Racecadotril
(acetorphan) RB-101 RB-120 RB-3007 Opiorphan Selank Semax Spinorphin Thiorphan Tynorphin Ubenimex
Ubenimex
(bestatin)

Propeptides: β-Lipotropin (proendorphin) Prodynorphin Proenkephalin Pronociceptin Proopiomelanocortin
Proopiomelanocortin
(POMC)

Others: Kyotorphin
Kyotorphin
(met-enkephalin releaser/degradation stabilizer)

See also: Receptor/signaling modulators • Signaling peptide/protein receptor modulators

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