Hello solars-ga
My searches on Google, Medline and Scirus.com have shown that the term
“endorphinase” is very rarely used, and the term “endorphinase
inhibitor” even less so. In comparison, the term “enkephalinase
inhibitor” appears to be relatively common. I have therefore focused
on inhibitors of enkephalinase. I did also search more-generally on
“endopeptidase inhibitors”, but this broadened out the area of
compound activity too far to be useful.
Here is a list of enkephalinase inhibitors, with a link in each case
to a relevant study in the medical literature:
1. BL-2401 ((+/-)-3-[2-benzyl-3-(propionylthio)
propionyl]amino-5-methylbenzoic acid)
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, Deguchi T, Nakamura H of the
Department of Pharmacology I, Dainippon Pharmaceutical Co., Ltd.,
Suita/Osaka, Japan and the Welsh School of Pharmacy, University of
Wales, Cardiff, U.K
published in Japanese Journal Pharmacology 1997 December, vol 75 (no.
4): 337-346
http://www.biopsychiatry.com/enkeph.htm
2. SCH 34826 ((S)-N-[n-[1-[(2,2-dimethyl-1,3-dioxolan-4yl)
methoxy]carbonyl]-2-phenylethyl]-L-phenylalanine-B-alanine)
Antinociceptive effects of the enkephalinase inhibitor, SCH 34826, in
the snail, Cepaea nemoralis.
By Saksida LM, Galea LA, Kavaliers M.
Of Department of Psychology, University of British Columbia,
Vancouver, Canada.
Published in Peptides 1993 Jul-Aug, Vol. 14 (no.4):763-765
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8234022&dopt=Abstract
3. Acetorphan (racecadotril)
Racecadotril in the treatment of acute watery diarrhea in children.
By Salazar-Lindo E, Santisteban-Ponce J, Chea-Woo E, Gutierrez M.
Of Department of Pediatrics, Hospital Nacional Cayetano Heredia,
Lima, Peru.
Published in New England Journal of Medicine 2000 Aug 17, Vol.343 (no.
7):463-467
http://www.essentialdrugs.org/indices/hma/indices.200010/msg00014.php
4. Kelatorphan (1S,2R,2'S)-2-[2'-(N-hydroxycarbamoylmethyl)-3'-phenylpropionylamino]cyclohexane-1-carboxylic
acid)
The effects of kelatorphan, an enkephalinase inhibitor, on tonic and
stimulus-evoked opioid-mediated inhibition of a spinal reflex in the
decerebrated and spinalized rabbit
by Rob W. Clarke and Rena N.B. Bhandari
of the School of Biological Sciences, University of Nottingham, Sutton
Bonington Campus, Loughborough LE12 5RD
Published in Journal of Physiology (1998), 509.P, 165P
http://physiology.cup.cam.ac.uk/Proceedings/Abstracts/509P/Liverpool/Files/S299
5. Spinorphin
Spinorphin, an endogenous inhibitor of enkephalin-degrading enzymes,
potentiates leu-enkephalin-induced anti-allodynic and antinociceptive
effects in mice.
By Honda M, Okutsu H, Matsuura T, Miyagi T, Yamamoto Y, Hazato T, Ono
H.
Of the Laboratory of Pharmacology, Faculty of Pharmaceutical Sciences,
Science University of Tokyo, Japan.
Published in The Japanese Journal of Pharmacology Vol. 87 (2001) ,
No. 4 pp.261-267
http://jjp.jstage.jst.go.jp/cgi-bin/rs.cgi?SID=5b049aedd49267837f6fef54afc13d03
Available in full text:
http://jjp.jstage.jst.go.jp/cgi-bin/fs.cgi/87_261.pdf?SID=492bacd63b1b59eb868ff08d9b0e0c63
6. Thiorphan ((DL-mercapto-2-benzylpropanoyl)-glycine)
Thiorphan, an inhibitor of neutral endopeptidase/enkephalinase
(CD10/CALLA) enhances cell proliferation in bone marrow cultures of
patients with acute leukemia in remission.
By Stanovic S, Boranic M, Petrovecki M, Batinic D, Skodlar J, Nemet
D, Labar B.
Of Department of Molecular Medicine, Ruder Boskovic Institute,
Zagreb, Croatia.
Published in Haematologia (Budapest) 2000 Vol. 30 (no.1):1-10
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10841318&dopt=Abstract
7. and 8. hydrocinnamic acid and D-phenylalanine
Enkephalinase inhibition: regulation of ethanol intake in genetically
predisposed mice.
By Blum K, Briggs AH, Trachtenberg MC, Delallo L, Wallace JE.
Of Department of Pharmacology, University of Texas Health Science
Center, San Antonio 78234
Published in Alcohol 1987 Nov-Dec; Vol. 4 (no. 6):449-456
9. SCH 32615 (N-[L-(1-carboxy2-phenyl)ethyl]-L-phenylalanyl-á-alanine)
SCH 32615, an enkephalinase inhibitor, enhances pregnancy-induced
analgesia in mice.
By Jayaram A, Singh P, Carp H.
Of Department of Anesthesiology, Oregon Health Sciences, University,
Portland 97210-3098, USA.
Published in Anesthesia Analgesia 1995 May Vol. 80(no. 5): 944-948
10. Phosphoramidon
REM sleep deprivation decreases the grooming and shaking behaviour
induced by enkephalinase inhibitor or opiate withdrawal.
By Ukponmwan OE, vd Poel-Heisterkamp AL, Dzoljic MR
Published in Pharmacology and Biochemistry of Behavior 1985 September
Vol. 23: 385-389
http://reviews.bmn.com/medline/search/record?uid=MDLN.86017069
11. N-carboxymethyl-Phe-Leu
[The effect of multiple administrations of beta-endorphin and an
enkephalinase inhibitor into the rat caudate nucleus on the
realization of an avoidance conditioned reflex]
by Iakimovskiĭ AF
Published in Zhurnal Vyssh Nerv Deiat Im I P Pavlova 1995 Jan-Feb Vol.
45:101-6
http://reviews.bmn.com/medline/search/record?uid=MDLN.95274292&refer=scirus
12. Puromycin
Concentration-dependent effect of met-enkephalin on human
polymorphonuclear leukocytes.
By Fóris G, Medgyesi GA, Nagy JT, Varga Z
Published in Annals N Y Academy Science 1987 Vol. 496:151-157
http://reviews.bmn.com/medline/search/record?uid=MDLN.87269109
13. Sinorphan
Degradation of atrial natriuretic factor in mouse blood in vitro and
in vivo: role of enkephalinase (EC 3.4.24.11).
By Gros C, Souque A, Schwartz JC
Published in Neuropeptides 1990 Sep Vol. 17:1-5
http://reviews.bmn.com/medline/search/record?uid=MDLN.91109925
14. N-[(R,S)-3-hydroxyaminocarbonyl-2-benzyl-1-oxopropyl]-glycine
Binding of the bidentate inhibitor [3H]HACBO-Gly to the rat brain
neutral endopeptidase "enkephalinase".
By Waksman G, Bouboutou R, Devin J, Besselievre R, Fournie-Zaluski MC,
Roques BP
Published in Biochemical and Biophysical Research Communications 1985
Aug Vol. 131: 262-268
http://reviews.bmn.com/medline/search/record?uid=MDLN.85306963
15. Bestatin (inhibits enkephalinase as well as inhibiting enkephalin
aminopeptidase)
Peripheral opioid receptors mediating antinociception in inflammation.
Evidence for activation by enkephalin-like opioid peptides after cold
water swim stress.
By Parsons CG, Herz A
Published in Journal of Pharmacology and Experimental Therapy 1990 Nov
Vol. 255:795-802
http://reviews.bmn.com/medline/search/record?uid=MDLN.91056486
16. ES52 (a derivative of thiorphan)
Failure of ES 52, a highly potent enkephalinase inhibitor, to affect
nociceptive transmission by rat dorsal horn convergent neurones.
By Villanueva L, Cadden S, Chitour D, Le Bars D
Published in Brain Research 1985 April Vol. 333: 156-160
http://reviews.bmn.com/medline/search/record?uid=MDLN.85200823
17 ONO-9902
Antinociceptive effects of ONO-9902, an enkephalinase inhibitor, after
visceral stress condition in rats.
By Yamamori Y, Saito Y, Kaneko M, Kirihara Y, Sakura S, Kosaka Y
Published in Canadian Journal of Anaesthesia 1996 Nov Vol.
43:1175-1179
http://reviews.bmn.com/medline/search/record?uid=MDLN.97081534
18. Other (4S)-4-[(2S)-benzyl-3-mercaptopropionylamino]-4-(N-phenylcarbamoyl
)-butyric acids
New orally active enkephalinase inhibitors: their synthesis,
biological activity, and analgesic properties.
By Senokuchi K, Nakai H, Nagao Y, Sakai Y, Katsube N, Kawamura M
Published in Bioorganic Med Chem 1998 Apr Vol. 6:441-463
http://reviews.bmn.com/medline/search/record?uid=MDLN.98259476
19 Gly-Gly-Phe-Leu,
Synthesis of an Enkephalinase Inhibitor, Gly-Gly-Phe-Leu,
by Continuous-Flow Peptide Synthesizer
by Iskander, M. N. and P. A. Jones,
Published in Journal of Chemical Education., 1990, Vol. 67 (no. 2),
70-172.
This reference is in a bibliography at
http://www.colby.edu/chemistry/Grants/refs00.pdf
20. RB-101
CCK-B receptors in the limbic system modulate the antidepressant-like
effects induced by endogenous enkephalins
by Smadja C, Ruiz F, Coric P, Fournie-Zaluski MC, Roques BP, Maldonado
R
of Departement de Pharmacochimie Moleculaire et Structurale, INSERM
U266, CNRS D 1500,
UFR des Sciences Pharmaceutiques et Biologiques, Paris, France.
Published in Japanese Journal of Pharmacology 1997 Dec; Vol. 75 (no.
4):337-346
http://www.biopsychiatry.com/enkantidep.htm
20 and 21 RB 38A (mixed inhibitor of enkephalin catabolism) RB 38B
(selective inhibitor of neutral endopeptidase EC)
Effect of mixed (RB 38A) and selective (RB 38B) inhibitors of
enkephalin degrading enzymes on a model of depression in the rat
by Tejedor-Real P, Mico JA, Maldonado R, Roques BP, Gibert-Rahola J
of Department of Neurosciences, School of Medicine, Cadiz, Spain.
Biological Psychiatry 1993 Jul Vol 34 (no 1-2):100-107
http://opioids.com/enkephalinase/
22. Retrothiorphan (derivative of thiorphan)
Effects of the selective neutral endopeptidase inhibitor,
retrothiorphan, on renal function and blood pressure in conscious
normotensive Wistar and hypertensive DOCA-salt rats.
By Pham I, el Amrani AI, Fournie-Zaluski MC, Corvol P, Roques B,
Michel JB.
Of INSERM U 367, Universite Paris V, France.
Published in Journal of Cardiovascular Pharmacology 1992 Dec; Vol 20
(no 6):847-857
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1282584&dopt=Abstract
Cited as an enkephalinase inhibitor on p. 8 of “Opioid Peptides:
Medicinal Chemistry” http://www.nida.nih.gov/pdf/monographs/69.pdf
I hope this information will be of use to you. Please request further
clarification if you feel something is lacking.
Search strategy: as detailed in the first paragraph of this answer |
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