PMID- 16442521
OWN - NLM
STAT- MEDLINE
DCOM- 20060418
LR  - 20181113
IS  - 0014-2999 (Print)
IS  - 0014-2999 (Linking)
VI  - 531
IP  - 1-3
DP  - 2006 Feb 15
TI  - Behavioral and neurobiological effects of the enkephalinase inhibitor RB101 
      relative to its antidepressant effects.
PG  - 151-9
AB  - Nonpeptidic delta-opioid receptor agonists produce antidepressant-like effects in 
      rodents, and compounds that inhibit the breakdown of endogenous opioid peptides 
      have antidepressant-like effects in animal models. In this study, the behavioral 
      effects of the enkephalinase inhibitor, RB101 (N-[(R, 
      S)-2-benzyl-3-[(S)(2-amino-4-methyl-thio)-butyldithio]-1-oxopropyl]-l-phenylalanine 
      benzyl ester), were examined. Specifically, the effects of RB101 on convulsive 
      activity, locomotor activity, and antidepressant-like effects in the forced swim 
      test were studied in Sprague-Dawley rats, and the opioid receptor types mediating 
      these effects were examined by antagonist studies. In addition, the effects of 
      RB101 on brain-derived neurotrophic factor (BDNF) mRNA expression were evaluated 
      in relation to its antidepressant effects. RB101 produced delta-opioid 
      receptor-mediated antidepressant effects (32 mg/kg i.v. and 100 mg/kg i.p.) and 
      increased locomotor activity (32 mg/kg i.v.) in rats. RB101 did not produce 
      convulsions or seizures and did not alter BDNF mRNA expression. In conclusion, 
      RB101 has the potential to produce antidepressant effects without convulsions.
FAU - Jutkiewicz, Emily M
AU  - Jutkiewicz EM
AD  - Department of Pharmacology, University of Michigan Medical School, Ann Arbor, MI 
      48109-0632, USA. ejutkiew@umich.edu
FAU - Torregrossa, Mary M
AU  - Torregrossa MM
FAU - Sobczyk-Kojiro, Katarzyna
AU  - Sobczyk-Kojiro K
FAU - Mosberg, Henry I
AU  - Mosberg HI
FAU - Folk, John E
AU  - Folk JE
FAU - Rice, Kenner C
AU  - Rice KC
FAU - Watson, Stanley J
AU  - Watson SJ
FAU - Woods, James H
AU  - Woods JH
LA  - eng
GR  - T32 GM007767/GM/NIGMS NIH HHS/United States
GR  - T32 GM07767/GM/NIGMS NIH HHS/United States
GR  - T32 DA007267/DA/NIDA NIH HHS/United States
GR  - T32 DA07267/DA/NIDA NIH HHS/United States
GR  - P01 DA000254/DA/NIDA NIH HHS/United States
GR  - DA00254/DA/NIDA NIH HHS/United States
GR  - K21 DA000254/DA/NIDA NIH HHS/United States
GR  - P50 DA000254/DA/NIDA NIH HHS/United States
PT  - Journal Article
PT  - Research Support, N.I.H., Extramural
DEP - 20060125
PL  - Netherlands
TA  - Eur J Pharmacol
JT  - European journal of pharmacology
JID - 1254354
RN  - 0 (Antidepressive Agents)
RN  - 0 (Benzamides)
RN  - 0 (Brain-Derived Neurotrophic Factor)
RN  - 0 (Disulfides)
RN  - 0 (Enzyme Inhibitors)
RN  - 0 (Narcotic Antagonists)
RN  - 0 (Piperazines)
RN  - 0 (RNA, Messenger)
RN  - 135949-60-9 (RB 101)
RN  - 156727-74-1 
      (4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide)
RN  - 47E5O17Y3R (Phenylalanine)
RN  - 5S6W795CQM (Naltrexone)
RN  - 9002-60-2 (Adrenocorticotropic Hormone)
RN  - EC 3.4.24.11 (Neprilysin)
RN  - G167Z38QA4 (naltrindole)
SB  - IM
MH  - Adrenocorticotropic Hormone/blood
MH  - Animals
MH  - Antidepressive Agents/*pharmacology
MH  - Behavior, Animal/*drug effects
MH  - Benzamides/pharmacology
MH  - Brain-Derived Neurotrophic Factor/blood/genetics
MH  - Disulfides/*pharmacology
MH  - Dose-Response Relationship, Drug
MH  - Electroencephalography/*drug effects
MH  - Enzyme Inhibitors/pharmacology
MH  - Frontal Lobe/metabolism
MH  - Hippocampus/metabolism
MH  - Injections, Intravenous
MH  - Male
MH  - Motor Activity/drug effects
MH  - Naltrexone/analogs & derivatives/pharmacology
MH  - Narcotic Antagonists/pharmacology
MH  - Neprilysin/*antagonists & inhibitors
MH  - Phenylalanine/*analogs & derivatives/pharmacology
MH  - Piperazines/pharmacology
MH  - RNA, Messenger/genetics/metabolism
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Swimming
PMC - PMC1828120
MID - NIHMS15858
EDAT- 2006/01/31 09:00
MHDA- 2006/04/19 09:00
PMCR- 2008/02/01
CRDT- 2006/01/31 09:00
PHST- 2005/08/04 00:00 [received]
PHST- 2005/12/08 00:00 [revised]
PHST- 2005/12/12 00:00 [accepted]
PHST- 2006/01/31 09:00 [pubmed]
PHST- 2006/04/19 09:00 [medline]
PHST- 2006/01/31 09:00 [entrez]
PHST- 2008/02/01 00:00 [pmc-release]
AID - S0014-2999(05)01303-8 [pii]
AID - 10.1016/j.ejphar.2005.12.002 [doi]
PST - ppublish
SO  - Eur J Pharmacol. 2006 Feb 15;531(1-3):151-9. doi: 10.1016/j.ejphar.2005.12.002. 
      Epub 2006 Jan 25.