PMID- 8485021
OWN - NLM
STAT- MEDLINE
DCOM- 19930610
LR  - 20190512
IS  - 0306-5251 (Print)
IS  - 1365-2125 (Electronic)
IS  - 0306-5251 (Linking)
VI  - 35
IP  - 4
DP  - 1993 Apr
TI  - Stereoselective sulphate conjugation of salbutamol in humans: comparison of 
      hepatic, intestinal and platelet activity.
PG  - 413-8
AB  - 1. The oral bioavailability of the beta 2-adrenoceptor agonist salbutamol has 
      been proposed to be stereoselective, presumably due to presystemic sulphate 
      conjugation. In the present study we examined the stereochemistry of the 
      sulphation reaction in vitro using human tissue preparations. 2. Sulphation of 
      salbutamol was studied with partially purified hepatic M and P form phenol 
      sulphotransferases (PSTs), 100,000 g cytosol of jejunal mucosa and platelet 
      homogenate. The cosubstrate PAP35S was used as the sulphate donor. The acceptor 
      substrate was either (+)-, (-)-or (+/)-salbutamol. 3. Sulphation was catalyzed by 
      the M form PST of the liver but not the P form. The sulphation efficiency 
      (Vmax/Km) was 11.9-fold greater for the (-)- than for the (+)- enantiomer, due 
      entirely to a lower apparent Km for (-)-salbutamol, 103 microM, than for 
      (+)-salbutamol, 1394 microM. 4. Sulphation by the jejunal mucosa (n = 3) was very 
      similar to that of the M form PST with the efficiency being 9.8-fold greater for 
      the (-)-enantiomer and apparent Km values 95 microM and 889 microM for (-)- and 
      (+)-salbutamol, respectively. 5. Sulphation by the platelet (n = 3) was also very 
      similar to that of the M form PST with the efficiency being 9.9-fold greater for 
      the (-)-enantiomer and apparent Km values 141 microM and 1190 microM for (-)- and 
      (+)-salbutamol, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
FAU - Walle, U K
AU  - Walle UK
AD  - Department of Cell and Molecular Pharmacology and Experimental Therapeutics, 
      Medical University of South Carolina, Charleston 29425.
FAU - Pesola, G R
AU  - Pesola GR
FAU - Walle, T
AU  - Walle T
LA  - eng
GR  - GM46000/GM/NIGMS NIH HHS/United States
GR  - HL07260/HL/NHLBI NIH HHS/United States
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - England
TA  - Br J Clin Pharmacol
JT  - British journal of clinical pharmacology
JID - 7503323
RN  - 0 (Isoenzymes)
RN  - 0 (Sulfates)
RN  - 0 (Sulfur Radioisotopes)
RN  - 482-67-7 (Phosphoadenosine Phosphosulfate)
RN  - EC 2.8.2.1 (Arylsulfotransferase)
RN  - QF8SVZ843E (Albuterol)
SB  - IM
MH  - Albuterol/blood/*metabolism/pharmacokinetics
MH  - Arylsulfotransferase/metabolism
MH  - Blood Platelets/*metabolism
MH  - Cytosol/metabolism
MH  - Humans
MH  - Isoenzymes/metabolism
MH  - Jejunum/*metabolism
MH  - Kinetics
MH  - Liver/*enzymology
MH  - Phosphoadenosine Phosphosulfate/metabolism
MH  - Stereoisomerism
MH  - Sulfates/blood/*metabolism/pharmacokinetics
MH  - Sulfur Radioisotopes
PMC - PMC1381553
EDAT- 1993/04/01 00:00
MHDA- 1993/04/01 00:01
PMCR- 1993/10/01
CRDT- 1993/04/01 00:00
PHST- 1993/04/01 00:00 [pubmed]
PHST- 1993/04/01 00:01 [medline]
PHST- 1993/04/01 00:00 [entrez]
PHST- 1993/10/01 00:00 [pmc-release]
AID - 10.1111/j.1365-2125.1993.tb04159.x [doi]
PST - ppublish
SO  - Br J Clin Pharmacol. 1993 Apr;35(4):413-8. doi: 
      10.1111/j.1365-2125.1993.tb04159.x.