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Conopeptide rho-TIA, a peptide from Conus tulipa venom, acts as a selective, noncompetitive inhibitor at the human α1B-Adrenergic Receptor and as a competitive inhibitor at the α1A and α1D-Adrenergic Receptors. Binding to these subtypes, conopeptide rho-TIA may inform the creation of new α1-Adrenergic Receptor subtype-selective drugs [1].
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Description | Conopeptide rho-TIA, a peptide from Conus tulipa venom, acts as a selective, noncompetitive inhibitor at the human α1B-Adrenergic Receptor and as a competitive inhibitor at the α1A and α1D-Adrenergic Receptors. Binding to these subtypes, conopeptide rho-TIA may inform the creation of new α1-Adrenergic Receptor subtype-selective drugs [1]. |
In vitro | Conopeptide rho-TIA at a concentration of 100 nM applied for 24-48 hours interacts with human α1B-Adrenergic Receptor non-competitively and reversibly, suggesting its potential role as an allosteric inhibitor [1]. At 30 nM for 2 hours, conopeptide rho-TIA acts as a non-competitive inhibitor for the α1B-Adrenergic Receptor but competitively inhibits the α1A and α1D-Adrenergic Receptor subtypes [1]. Additionally, a single application of 10 μM conopeptide rho-TIA inhibits the increase in cytoplasmic Ca2+ concentration mediated by the α1-Adrenergic Receptor activation by norepinephrine, without affecting the presynaptic α2-Adrenergic Receptor-mediated responses [2]. |
Molecular Weight | 2390.88 |
Formula | C105H160N36O21S4 |
Cas No. | 381725-58-2 |
Storage | keep away from moisture | Shipping with blue ice. |
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