Study of the interaction between aryloxypropanolamines and Asn386 in helix VII of the human 5-hydroxytryptamine(1A) receptor

Molecular Pharmacology

Volumn 51, Issue 5, 1997, Pages 889-896

  Kuipers, Wilma ^a   Link, Regina ^b   Standaar, Piet J ^a   Stoit, Axel R ^a   Van Wijngaarden, Ineke ^a   Leurs, Rob ^b   Ijzerman, Adriaan P ^b  

^a Solvay Pharmaceuticals Inc   (Netherlands)

^b LEIDEN UNIVERSITY   (Netherlands)

Author keywords

[No Author keywords available]

Indexed keywords

PENBUTOLOL; PROPANOLAMINE DERIVATIVE; PROPRANOLOL; SEROTONIN 1A RECEPTOR;

ARTICLE; BINDING AFFINITY; DRUG STRUCTURE; HYDROGEN BOND; MUTATION; PRIORITY JOURNAL; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

EID: 0030910261     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.51.5.889     Document Type: Article

References (20)

1. Howe, R., and B. S. Rao. β-adrenergic blocking agents III. The optical isomers of pronethalol, propranolol, and several related compounds. J. Med. Chem. 11:1118-1121 (1968).
2. Boess, F. G., and I. L. Martin. Molecular biology of 5-HT receptors. Neuropharmacology 33:275-317 (1993).
3. 1b autoreceptor blocking properties of the β adrenoceptor antagonist (-)penbutolol. J. Pharmacol. Exp. Ther. 265:707-712 (1993).
4. 1a) receptor antagonist in rat brain. J. Pharmacol. Exp. Ther. 265:739-744 (1993).
5. 1a receptors. Mol. Pharmacol. 41:695-698 (1992).
6. 2 adrenergic receptor increases its affinity for a family of β-receptor antagonists. J. Biol. Chem. 266:15488-15492 (1991).
7. 1b receptors. J. Neurochem. 60:380-383 (1993).
8. 1B receptors. Nature (Lond.) 360:161-163 (1992).
9. 1F receptors for β-adrenergic antagonists. Neuropharmacology 33:387-391 (1994).
10. Kuipers, W., L. Oliveira, A. C. M. Paiva, F. Rippmann, C. Sander, and A. P. IJzerman. Analysis of G protein-coupled receptor function, in Membrane Protein Models (J. Findlay, ed.). Bios Scientific Publishers Ltd., Oxford, 27-45 (1996).
11. 1A receptor. Agonist and antagonist binding sites. Drug Design Disc. 11:231-249 (1994).
12. Henderson, R., J. M. Baldwin, T. A. Ceska, F. Zemlin, E. Beckmann, and K. H. Downing. Model for the structure of bacteriorhodopsin based on high-resolution electron cryo-microscopy. J. Mol. Biol. 213:899-929 (1990)
13. 1a serotonin receptor. Mol. Pharmacol. 43:516-520 (1993).
14. 1A receptors in rat brain membranes. Eur. J. Pharmacol. 288:173-186 (1995).
15. 1dβ T255N mutant receptors may involve formation of two hydrogen bonds to asparagine. Mol. Pharmacol. 49:198-200 (1996).
16. Rix, M. J., and B. R. Webster. Electron impact-induced eliminations of acetaldehyde. J. Chem. Soc. B 3:254-258 (1968).
17. Howe, R. β-adrenergic blocking agents. VIII. Reactions of β-haloalkylamines related to pronethalol and propranolol. J. Med. Chem. 13:398-403 (1970).
18. 3H]-8-OH-DPAT. Biochem. Pharmacol. 35:1943-1949 (1986).
19. Stewart, J. J. P. MOPAC. A semiempirical molecular orbital program. J. Comput.-Aided Mol. Des. 4:1-105 (1990).
20. Pierson, M. E., R. A. Lyon, M. Titeler, P. Kowalski, and R. A. Glennon. Design and synthesis of propranolol analogues as serotonergic agents. J. Med. Chem. 32:859-863 (1989).