Biochem/physiol Actions Pyr3 is a pyrazole compound that potently and selectively antagonizes TRPC3. Pyr3 inhibits TRPC3 by binding to the extracellular side of the receptor, resulting in suppression of B cell activation and cardiac hypertrophy.Members of the canonical transient receptor potential (TRPC) channel family are ion channels which conduct Ca+2 and are activated by membrane receptor-mediated stimulation of phospholipase C (PLC) activity. However, TRPC3 and other family members are also activated by membrane-independent diacylglycerol (DAG). BTP1 and BTP2 are pyrazoles that block TRPC channels, but they are not specific for TRPC subtypes. This channel is implicated in various processes, including B cell receptor (BCR)-mediated Ca+2 oscillations, activation of nuclear factor of activated T cells (NFAT), and promotion of cardiac hypertrophy. Pyr3 is a selectively inhibitor of TRPC3. It acts by binding to the extracellular side of the receptor, resulting in suppression of B cell activation and cardiac hypertrophy.Members of the canonical transient receptor potential (TRPC) channel family are Ca2+ ion channels that are activated by membrane receptor-mediated stimulation of phospholipase C (PLC). However, TRPC3 and other family members are also activated by membrane-independent diacylglycerol (DAG). This channel is implicated in various processes, including B cell receptor (BCR)-mediated Ca2+ oscillations, activation of nuclear factor of activated T cells (NFAT), and promotion of cardiac hypertrophy. |
Biochem/physiol Actions Pyr3 is a pyrazole compound that potently and selectively antagonizes TRPC3. Pyr3 inhibits TRPC3 by binding to the extracellular side of the receptor, resulting in suppression of B cell activation and cardiac hypertrophy.Members of the canonical transient receptor potential (TRPC) channel family are ion channels which conduct Ca+2 and are activated by membrane receptor-mediated stimulation of phospholipase C (PLC) activity. However, TRPC3 and other family members are also activated by membrane-independent diacylglycerol (DAG). BTP1 and BTP2 are pyrazoles that block TRPC channels, but they are not specific for TRPC subtypes. This channel is implicated in various processes, including B cell receptor (BCR)-mediated Ca+2 oscillations, activation of nuclear factor of activated T cells (NFAT), and promotion of cardiac hypertrophy. Pyr3 is a selectively inhibitor of TRPC3. It acts by binding to the extracellular side of the receptor, resulting in suppression of B cell activation and cardiac hypertrophy.Members of the canonical transient receptor potential (TRPC) channel family are Ca2+ ion channels that are activated by membrane receptor-mediated stimulation of phospholipase C (PLC). However, TRPC3 and other family members are also activated by membrane-independent diacylglycerol (DAG). This channel is implicated in various processes, including B cell receptor (BCR)-mediated Ca2+ oscillations, activation of nuclear factor of activated T cells (NFAT), and promotion of cardiac hypertrophy. |