Assessment of affinities of propranolol and bopindolol to membranes from COS-7 cell transiently transfected with beta-1-and beta-2-adrenoceptors using a radioligand-binding assay method

Pharmacology

Volumn 61, Issue 1, 2000, Pages 6-10

  Nakamura, Takashi ^a   Suzuki, Ayako ^a   Ohnuki, Toshio ^a   Hattori, Kaoru ^a   Watanabe, Kenichi ^a   Kurose, Hitoshi ^b   Nagao, Taku ^b   Nagatomo, Takafumi ^a  

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

^b NONE

Author keywords

3H CGP12177; Bopindolol; COS 7 cell; Propranolol; Radioligand binding assay; Adrenoceptor

Indexed keywords

4 (3 TERT BUTYLAMINO 2 HYDROXYPROPOXY) 2 BENZIMIDAZOLONE; ATENOLOL; BETA 1 ADRENERGIC RECEPTOR; BETA 2 ADRENERGIC RECEPTOR; BOPINDOLOL; METOPROLOL; PINDOLOL; PROPRANOLOL;

ANIMAL CELL; ARTICLE; DRUG EFFECT; DRUG RECEPTOR BINDING; LIGAND BINDING; MEMBRANE BINDING; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; RECEPTOR AFFINITY;

EID: 0033932205     PISSN: 00317012     EISSN: None     Source Type: Journal    
DOI: 10.1159/000028373     Document Type: Article

References (13)

1. Nagatomo T, Ishiguro M, Ohnuki T, Hattori K, Hosohata Y, Takatsu N, Katayama H, Watanabe K: Studies on relationships between chemical structure and β-blocking potency of bopindolol and its two metabolites. Life Sci 1998;62:1597-1600.
2. Hattori K, Muramatsu I, Ishiguro M, Ohnuki T, Nakamura T, Nagatomo T: Identification of binding sites of bopindolol and its two metabolites with betal-adrenoceptor by molecular modeling: Comparison with beta2-adrenoceptor. Pharmacology 1999;58:183-189.
3. 125I-iodocyanopindolol to β-adrenergic and serotonin-1B receptors of rat brain: Selectivity of β-adrenergic agents. Jpn J Pharmacol 1990;52: 195-200.
4. Sakuma N, Tsuchihashi H, Hosohata Y, Akashi H, Kinami J, Nagatomo T: Beta-blocking potency and selectivity of bopindolol and its two metabolites for beta 1- and beta 2-adrenergic receptors as assessed by radioligand binding assay. J Pharmacobiodyn 1991;14:250-255.
5. 2-adrenoceptor in the bovine mesenteric artery. Biol Pharm Bull 1994;17:1296-1298.
6. Hosohata Y, Sasaki K, Suzuki M, Karakisawa Y, Maruyama K, Tsuchihashi H, Nagatomo T: Alpha-1 and beta-adrenergic receptor blocking potencies of bopindolol and its two metabolites (18-502 and 20-785) as assessed by radioligand binding assay methods. Gen Pharmacol 1995; 26:743-747.
7. Sato Y, Kurosc H, Isogaya M, Nagao T: Molecular characterization of pharmacological properties of T-0509 for β-adrenoceptors. Eur J Pharmacol 1996;315:363-367.
8. Cullen BR: Use of eukaryotic expression technology in the functional analysis of a cloned genes; in Berger SL, Kimmel AR (eds): Methods in Enzymology. San Diego, Academic Press, 1987, pp 684-704.
9. Lowry OH, Rosebrough NJ, Farr AL, Randall RJ: Protein measurement with the Folin phenol reagent. J Biol Chem 1951;193:265-275.
10. Cheng Y, Prusoff WH: Relationship between the inhibition constant (K1) and the concentration of inhibition which causes 50% inhibition (150) of an enzymatic reaction. Biochem Pharmacol 1973;22:3099-3108.
11. Strader CD, Candelore MR, Hill WS, Dixon RA, Sigal IS: A single amino acid substitution in the β-adrenergic receptor promotes partial agonist activity from antagonists. J Biol Chem 1989;264:16470-16477.
12. 2-adrenergic receptor increases its affinity for a family of β receptor antagonists. J Biol Chem 1991;266: 15488-15492.
13. 2-adrenergic receptors. Proc Natl Acad Sci USA 1988;85:9494-9498.