Identification of a key amino acid of the human 5-HT2B serotonin receptor important for sarpogrelate binding

Journal of Pharmacological Sciences

Volumn 104, Issue 3, 2007, Pages 274-277

  Muntasir, Habib Abul ^a   Hossain, Murad ^a   Bhuiyan, Mohiuddin Ahmed ^a   Komiyama, Tadazumi ^a   Nakamura, Takashi ^a   Ozaki, Masanobu ^a   Nagatomo, Takafumi ^a  

^a NIIGATA UNIVERSITY OF PHARMACY AND APPLIED LIFE SCIENCES   (Japan)

Author keywords

5 HT2B receptor; Sarpogrelate; Site directed mutagenesis

Indexed keywords

1,2,3,5 TETRAHYDRO 5 METHYL 1 (3 PYRIDYLCARBAMOYL)PYRROLO[2,3 F]INDOLE; AMINO ACID; CYPROHEPTADINE; INOSITOL PHOSPHATE; RAUWOLSCINE; SARPOGRELATE; SEROTONIN 2B RECEPTOR;

AMINO ACID ANALYSIS; AMINO ACID SUBSTITUTION; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG RECEPTOR BINDING; EMBRYO; HUMAN; HUMAN CELL; MODEL; MUTATION; SITE DIRECTED MUTAGENESIS;

EID: 34547203507     PISSN: 13478613     EISSN: 13478648     Source Type: Journal    
DOI: 10.1254/jphs.SC0060241     Document Type: Article

References (15)

1. Barnes NM, Sharp T. A review of central 5-HT receptors and their function. Neuropharmacology. 1999;38:1083-1152.
2. Nebigil CG, Launay JM, Hickel P, Tournois C, Maroteaux L. 5-Hydroxytryptamine 2B receptor regulates cell-cycle progression: cross-talk with tyrosine kinase pathways. Proc Natl Acad Sci U S A. 2000;97:2591-2596.
3. 2B receptors. Int J Dev Neurosci. 2001;19:365-372.
4. 2B receptors in the cardiopathy associated with fenfluramine. Mol Pharmacol. 2000;57:75-81.
5. Ito K, Notsu T. Effect of sarpogrelate hydrochloride (MCI-9042) on peripheral circulation of chronic arterial occlusive diseases. J Clin Ther Med. 1991;7:1243-1251.
6. 2A serotonin receptor. J Pharmacol Sci. 2006;102;55-63.
7. 2C receptor: identification of amino acids responsible for sarpogrelate binding. Biol Pharm Bull. 2006;29:1645-1650.
8. 2C receptor subtypes by molecular modeling. Life Sci. 2003;73:193-207.
9. 2F receptor. Mol Pharmacol. 1992;43:419-426.
10. Lowry OH, Rosebrough NJ, Farr AL, Randall RJ. Protein measurement with the Folin phenol reagent. J Biol Chem. 1951;193:265-275.
11. Cheng Y-C, Prusoff WH. Relationship between the inhibition (Ki) and concentration of inhibitor which causes 50 per cent inhibition (IC50) of an enzymatic reaction. Biochem Pharmacol. 1973;22:3099-3108.
12. Furchgott RF. The classification of adrenoceptors (adrenergic receptors). An evaluation from the standpoint of receptor theory. In: Blaschko H, Muscholl E, editors. Catecholamines. Handbook of experimental pharmacology. Berlin: Springer; 1972: p. 283-335.
13. Wu C, Yoder EJ, Shih J, Chen K, Dias P, Shi LR, et al. Development and characterization of monoclonal antibodies specific to the serotonin 5-HT2A receptor. J Histochem Cytochem. 1998;46:811-824.
14. Wang CD, Gallaher TK, Shih JC. Site-directed mutagenesis of the serotonin 5-hydroxytryptamine 2 receptors: identification of amino acids necessary for ligand binding and receptor activation. Mol Pharmacol. 1993;43:931-940.
15. 2B receptors; molecular modeling and site-directed mutagenesis. J Biol Chem. 2002;277:17170-17178.