Spiro[9,10-dihydroanthracene]-9,3′-pyrrolidine - A structurally unique tetracyclic 5-HT2A receptor antagonist

European Journal of Pharmacology

Volumn 482, Issue 1-3, 2003, Pages 335-337

  Peddi, Srinivas ^a   Roth, Bryan L ^b   Glennon, Richard A ^a   Westkaemper, Richard B ^a  

^a VIRGINIA COMMONWEALTH UNIVERSITY   (United States)

^b CASE WESTERN RESERVE UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

5 HT receptor; 5 HT2A receptor antagonist; SpAMDA

Indexed keywords

ANTHRACENE DERIVATIVE; PHENETHYLAMINE; SEROTONIN 2A ANTAGONIST; SPIRO[9,10 DIHYDROANTHRACENE] 9,3' PYRROLIDINE; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; DRUG ACTIVITY; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG STRUCTURE; GEOMETRY; PHARMACOPHORE; PRIORITY JOURNAL; STRUCTURE ANALYSIS;

EID: 0344737662     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2003.09.059     Document Type: Article

References (8)

1. Glennon R.A., Dukat M., Westkaemper R.B. Serotonin receptors and ligands. Bloom F.E., Kupfer D.J. Psychopharmacology: The Fourth Generation of Progress. CD-ROM ed. 1999;Raven Press, New York, NY.
2. Palczewski K., Kumasaka T., Hori T., Behnke C.A., Motoshima H., Fox B.A., Le Trong I., Teller D.C., Okada T., Stenkamp R.E., Yamamoto M., Miyano M. Crystal structure of rhodopsin: a G protein-coupled receptor. Science. 289:2000;739-745.
3. Roth B.L. Multiple serotonin receptors: clinical and experimental aspects. Ann. Clin. Psychol. 6:1994;67-78.
4. Roth B.L., Shoham M., Choudhary M.S., Khan N. Identification of conserved aromatic residues essential for agonist binding and second messenger production at 5-hydroxytryptamine receptors. 2A Mol. Pharmacol. 52:1997;259-266.
5. Runyon S.P., Peddi S., Savage J.E., Roth B.L., Glennon R.A., Westkaemper R.B. Geometry-affinity relationships of the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene. J. Med. Chem. 45:2002;1656-1664.
6. Westkaemper R.B., Glennon R.A. Application of ligand SAR, receptor modeling and receptor mutagenesis to the discovery and development of a new class of 5-HT(2A) ligands. Curr. Top. Med. Chem. 2:2002;575-598.
7. 2 receptor model. Med. Chem. Res. 1:1992;401-408.
8. Westkaemper R.B., Runyon S.P., Bondarev M.L., Savage J.E., Roth B.L., Glennon R.A. 9-(Aminomethyl)-9,10-dihydroanthracene is a novel and unlikely 5-HT2A receptor antagonist. Eur. J. Pharmacol. 380:1999;R5-R7.