Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA).
Article Details
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Peddi S, Roth BL, Glennon RA, Westkaemper RB
Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA).
Bioorg Med Chem Lett. 2004 May 3;14(9):2279-83.
- PubMed ID
- 15081025 [ View in PubMed]
- Abstract
The synthesis and 5-HT(2A) receptor affinities of ring altered derivatives of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (4), a structurally unique tetracyclic 5-HT(2A) receptor antagonist, are described. The characteristics of the parent compound prove to be necessary for optimal 5-HT(2A) receptor affinity. However, expansion of the size of the pyrrolidine and central rings produce compounds with reasonably high 5-HT(2A) receptor affinities. In addition, the parent compound is shown to have high 5-HT(2) receptor selectivity.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Imipramine Dopamine D2 receptor Protein Humans UnknownBinderDetails - Binding Properties
Drug Target Property Measurement pH Temperature (°C) Cyproheptadine 5-hydroxytryptamine receptor 2A Ki (nM) 3 N/A N/A Details Cyproheptadine 5-hydroxytryptamine receptor 2C Ki (nM) 11 N/A N/A Details Imipramine 5-hydroxytryptamine receptor 2A Ki (nM) 94 N/A N/A Details Imipramine 5-hydroxytryptamine receptor 2C Ki (nM) 160 N/A N/A Details Imipramine Dopamine D2 receptor Ki (nM) 726 N/A N/A Details Imipramine Sodium-dependent noradrenaline transporter Ki (nM) 16 N/A N/A Details Imipramine Sodium-dependent serotonin transporter Ki (nM) 5 N/A N/A Details