PMID- 2787401
OWN - NLM
STAT- MEDLINE
DCOM- 19890817
LR  - 20191029
IS  - 0197-5110 (Print)
IS  - 0197-5110 (Linking)
VI  - 9
IP  - 2
DP  - 1989
TI  - Positive modulators of muscle acetylcholine receptor.
PG  - 107-25
AB  - A solution of succinic anhydride (SA) in buffer 
      N-tris(hydroxymethyl)methyl-2-aminoethane sulfonic acid (TES), the SATES 
      solution, potentiates the effect of carbonyl containing agonists on frog muscle 
      (del Castillo et al., Br. J. Pharmac. 84: 275-288, 1985). Here we report that the 
      main compound in the SATES solution is a monosuccinyl ester of TES (MST). This 
      compound is not an agonist of the acetylcholine (ACh) receptor nor is it an 
      inhibitor of ACh esterase, yet MST potentiates the ACh-induced tension and 
      depolarization in frog muscle to a new maximum. It increases the amplitude of 
      miniature endplate potentials but has no effect on the time course of miniature 
      endplate currents. The acetylated analogue of MST (mono-acetyl-TES: MAT) had 
      similar but more pronounced effects on frog muscle. Neither MST nor MAT affect 
      [3H]Ach binding to receptor-rich membranes from the electric organ of Torpedo 
      californica, or the affinity state transition induced by agonists. Radiolabeled 
      MST does not bind to these membranes and MAT does not alter agonist-induced ion 
      flux. Therefore, these compounds seem to act as positive modulators of muscle ACh 
      receptor but are inactive in Torpedo vesicles.
FAU - Eterovic, V A
AU  - Eterovic VA
AD  - Department of Biochemistry, Universidad Central del Caribe School of Medicine, 
      Cayey, P.R. 00633.
FAU - Escalona de Motta, G
AU  - Escalona de Motta G
FAU - Hann, R M
AU  - Hann RM
FAU - Lasalde, J A
AU  - Lasalde JA
FAU - Prieto, J A
AU  - Prieto JA
FAU - Ferchmin, P A
AU  - Ferchmin PA
LA  - eng
GR  - NS07464/NS/NINDS NIH HHS/United States
GR  - RR08102/RR/NCRR NIH HHS/United States
PT  - Journal Article
PT  - Research Support, U.S. Gov't, Non-P.H.S.
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - United States
TA  - J Recept Res
JT  - Journal of receptor research
JID - 8008358
RN  - 0 (Receptors, Cholinergic)
RN  - 023C2WHX2V (Tromethamine)
RN  - 7365-44-8 (TES)
RN  - N9YNS0M02X (Acetylcholine)
SB  - IM
MH  - Acetylcholine/pharmacology
MH  - Action Potentials/drug effects
MH  - Animals
MH  - Chemical Phenomena
MH  - Chemistry
MH  - In Vitro Techniques
MH  - Muscle Contraction/*drug effects
MH  - Rana pipiens
MH  - Receptors, Cholinergic/*drug effects
MH  - Torpedo
MH  - Tromethamine/*analogs & derivatives/pharmacology
EDAT- 1989/01/01 00:00
MHDA- 1989/01/01 00:01
CRDT- 1989/01/01 00:00
PHST- 1989/01/01 00:00 [pubmed]
PHST- 1989/01/01 00:01 [medline]
PHST- 1989/01/01 00:00 [entrez]
AID - 10.3109/10799898909066048 [doi]
PST - ppublish
SO  - J Recept Res. 1989;9(2):107-25. doi: 10.3109/10799898909066048.