BML-241 fails to display selective antagonism at the sphingosine-1- phosphate receptor, S1P 3

British Journal of Pharmacology

Volumn 149, Issue 3, 2006, Pages 277-282

  Jongsma, M ^a   Hendriks Balk, M C ^a   Michel, M C ^a   Peters, S L M ^a   Alewijnse, A E ^a  

^a UNIVERSITY OF AMSTERDAM   (Netherlands)

Author keywords

1 adrenoceptor; BML 241; S1P receptor; S1P 3 antagonist; Sphingosine 1 phosphate

Indexed keywords

ADENOSINE TRIPHOSPHATE; ALPHA ADRENERGIC RECEPTOR; BML 241; CALCIUM ION; CYCLIC AMP; FORSKOLIN; NUCLEOTIDE; PHENYLEPHRINE; PRAZOSIN; SPHINGOSINE 1 PHOSPHATE RECEPTOR ANTAGONIST; TIMONACIC; TRITIUM; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; CHO CELL; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DRUG POTENCY; FEMALE; GENETIC TRANSFECTION; MESENTERIC ARTERY; NONHUMAN; PRIORITY JOURNAL; RAT; RAT STRAIN;

ANIMALS; CALCIUM; CHO CELLS; CRICETINAE; CYCLIC AMP; PRAZOSIN; RECEPTORS, ADRENERGIC, ALPHA-1; RECEPTORS, LYSOSPHINGOLIPID; RECEPTORS, PURINERGIC P2; THIAZOLIDINES; VASOCONSTRICTION;

EID: 33749018836     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0706872     Document Type: Article

References (13)

1. Alewijnse AE, Peters SL, Michel MC (2004). Cardiovascular effects of sphingosine-1-phosphate and other sphingomyelin metabolites. Br J Pharmacol 143: 666-684.
2. Bakker RA, Weiner DM, ter Laak T, Beuming T, Zuiderveld OP, Edelbroek M et al. (2004). 8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist. Mol Pharmacol 65: 538-549.
3. Davis MD, Clemens JJ, Macdonald TL, Lynch KR (2005). Sphingosine 1-phosphate analogs as receptor antagonists. J Biol Chem 280: 9833-9841.
4. Hla T, Maciag T (1990). An abundant transcript induced in differentiating human endothelial cells encodes a polypeptide with structural similarities to G-protein-coupled receptors. J Biol Chem 265: 9308-9313.
5. Holdsworth G, Slocombe P, Hutchinson G, Milligan G (2005). Analysis of endogenous S1P and LPA receptor expression in CHO-K1 cells. Gene 350: 59-63.
6. 1- adrenoceptor subtypes differentially couple to growth promotion and inhibition in Chinese hamster ovary cells. Biochem Biophys Res Commun 272: 906-911.
7. Koide Y, Hasegawa T, Takahashi A, Ende A, Mochizuki N, Nakagawa M et al. (2002). Development of novel EDG3 antagonists using a 3D database search and their structure-activity relationships. J Med Chem 45: 4629-4638.
8. Koop EA, Gebbink MF, Sweeney TE, Mathy MJ, Heijnen HF, Spaan JA et al. (2005). Impaired flow-induced dilation in mesenteric resistance arteries from receptor protein tyrosine phosphatase-mu-deficient mice. Am J Physio Heart Circ Physiol 288: H1218-H1223.
9. Lee MJ, Van Brocklyn JR, Thangada S, Liu CH, Hand AR, Menzeleev R et al. (1998). Sphingosine-1-phosphate as a ligand for the G protein-coupled receptor EDG-1. Science 279: 1552-1555.
10. Liu Y, Wada R, Yamashita T, Mi Y, Deng CX, Hobson JP et al. (2000). Edg-1, the G protein-coupled receptor for sphingosine-1-phosphate, is essential for vascular maturation. J Clin Invest 106: 951-961.
11. Spiegel S, Milstien S (2003). Sphingosine-1-phosphate: an enigmatic signalling lipid. Nat Rev Mol Cell Biol 4: 397-407.
12. Watterson KR, Ratz PH, Spiegel S (2005). The role of sphingosine-1- phosphate in smooth muscle contraction. Cell Signal 17: 289-298.
13. Yatomi Y, Igarashi Y, Yang L, Hisano N, Qi R, Asazuma N et al. (1997). Sphingosine 1-phosphate, a bioactive sphingolipid abundantly stored in platelets, is a normal constituent of human plasma and serum. J Biochem Tokyo 121: 969-973.