PMID- 9199488
OWN - NLM
STAT- MEDLINE
DCOM- 19970721
LR  - 20190701
IS  - 0024-3205 (Print)
IS  - 0024-3205 (Linking)
VI  - 60
IP  - 26
DP  - 1997
TI  - Comparison of the inhibitory effect of isothiourea and mercapto-alkylguanidine 
      derivatives on the alternative pathways of arginine metabolism in macrophages.
PG  - PL395-401
AB  - Novel, non-arginine based compounds have been identified as potent inhibitors of 
      nitric oxide synthase (NOS). Members of the isothiourea and 
      mercapto-alkylguanidine classes have generated much interest, as some members of 
      these classes show selectivity towards the inducible isoform of NOS (iNOS), which 
      plays a role in inflammation and shock. Here we compared the effect of a number 
      of these compounds as well as L-arginine based NOS inhibitor reference compounds 
      on macrophage-derived and liver arginase and macrophage iNOS activities. From the 
      non-arginine based NOS inhibitors studied only S-aminoethyl-isothiourea (AETU) 
      caused a slight inhibition of arginase activity. This inhibition was kinetically 
      competitive and due to the rearrangement of AETU to mercapto-ethylguanidine 
      (MEG). The weak inhibitory effect of non-arginine based iNOS inhibitors on 
      arginase activity further supports the view that such compounds may be of 
      practical use for inhibition of NO production in cells simultaneously expressing 
      iNOS and arginase.
FAU - Hrabak, A
AU  - Hrabak A
AD  - Department of Medical Chemistry, Molecular Biology and Pathobiochemistry, 
      Semmelweis University of Medicine, Budapest, Hungary.
FAU - Bajor, T
AU  - Bajor T
FAU - Southan, G J
AU  - Southan GJ
FAU - Salzman, A L
AU  - Salzman AL
FAU - Szabo, C
AU  - Szabo C
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Netherlands
TA  - Life Sci
JT  - Life sciences
JID - 0375521
RN  - 0 (Guanidines)
RN  - 22584-04-9 (Isothiuronium)
RN  - 94ZLA3W45F (Arginine)
RN  - EC 1.14.13.39 (Nitric Oxide Synthase)
RN  - GYV9AM2QAG (Thiourea)
SB  - IM
MH  - Animals
MH  - Arginine/*metabolism
MH  - Cattle
MH  - Guanidines/*pharmacology
MH  - Isothiuronium/analogs & derivatives/*pharmacology
MH  - Kinetics
MH  - Macrophages/*drug effects/metabolism
MH  - Nitric Oxide Synthase/*drug effects
MH  - Rats
MH  - Thiourea/analogs & derivatives/*pharmacology
EDAT- 1997/01/01 00:00
MHDA- 1997/01/01 00:01
CRDT- 1997/01/01 00:00
PHST- 1997/01/01 00:00 [pubmed]
PHST- 1997/01/01 00:01 [medline]
PHST- 1997/01/01 00:00 [entrez]
AID - S0024320597003287 [pii]
AID - 10.1016/s0024-3205(97)00328-7 [doi]
PST - ppublish
SO  - Life Sci. 1997;60(26):PL395-401. doi: 10.1016/s0024-3205(97)00328-7.