fty-720p and Bradycardia

fty-720p has been researched along with Bradycardia* in 1 studies

Other Studies

1 other study(ies) available for fty-720p and Bradycardia

Article	Year
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists. Bioorganic & medicinal chemistry letters, 2005, Aug-01, Volume: 15, Issue:15 The novel immunosuppressant FTY720 has been demonstrated to elicit immunomodulating effects via interaction with the G-protein coupled receptor S1P(1). FTY720 induced agonism at the S1P(3) receptor, however, has been shown to result in mild bradycardia, a minor side-effect of initial FTY720 therapy. This report describes the synthesis of several potent 4(5)-phenylimidazole-based S1P(1) receptor agonists that are accompanied by poor agonist activity at S1P(3). For instance, compound 20 displayed an EC(50)=4.7+/-1.3 nM at the S1P(1) receptor and EC(50)=780+/-1.3 nM at the S1P(3) receptor using a [gamma-(35)S]GTP-binding assay as compared to phospho-FTY720 (S1P(1): EC(50)=1.3+/-1.3nM, S1P(3): EC(50)=2.0+/-2.4 nM). Topics: Animals; Benzimidazoles; Binding Sites; Bradycardia; CHO Cells; Cricetinae; Fingolimod Hydrochloride; Immunosuppressive Agents; Lethal Dose 50; Lysophospholipids; Propylene Glycols; Receptors, Lysosphingolipid; Sphingosine; Structure-Activity Relationship	2005

Article

Year

Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.

Bioorganic & medicinal chemistry letters, 2005, Aug-01, Volume: 15, Issue:15

The novel immunosuppressant FTY720 has been demonstrated to elicit immunomodulating effects via interaction with the G-protein coupled receptor S1P(1). FTY720 induced agonism at the S1P(3) receptor, however, has been shown to result in mild bradycardia, a minor side-effect of initial FTY720 therapy. This report describes the synthesis of several potent 4(5)-phenylimidazole-based S1P(1) receptor agonists that are accompanied by poor agonist activity at S1P(3). For instance, compound 20 displayed an EC(50)=4.7+/-1.3 nM at the S1P(1) receptor and EC(50)=780+/-1.3 nM at the S1P(3) receptor using a [gamma-(35)S]GTP-binding assay as compared to phospho-FTY720 (S1P(1): EC(50)=1.3+/-1.3nM, S1P(3): EC(50)=2.0+/-2.4 nM).

Topics: Animals; Benzimidazoles; Binding Sites; Bradycardia; CHO Cells; Cricetinae; Fingolimod Hydrochloride; Immunosuppressive Agents; Lethal Dose 50; Lysophospholipids; Propylene Glycols; Receptors, Lysosphingolipid; Sphingosine; Structure-Activity Relationship

2005