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L-765314

CAS No. : 189349-50-6

MCE 站：L-765314

产品活性：L-765314 是 α1b 肾上腺素能受体 (α1b adrenergic receptor) 的一个有效的、选择性拮抗剂，其在大鼠和人体中的 K_i 值分别为 5.4 nM 和 2.0 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Adrenergic Receptor

In Vitro: L-765314 exhibits two displacement sites. The high-affinity site accounts for approximately 25% of binding (IC₅₀) 1.90 nM and represents binding to the R1b sites. The low-affinity site accounts for the residual 75% of binding (IC₅₀) 790 nM and represents binding to the R1a sites.

In Vivo: The results of plasma assayed by liquid chromatograph/mass spectrometer (LCMS) show that the mean C_max of L-765314 (A322312) is 1.05 μM and the t_1/2 is 0.5 h. L-765314 shows weak potency for inhibiting the pressor response to either phenylephrine or A-61603 (AD₂₅>3 mg/kg for each). On the basis of the inhibition of pressor responses to the R1a subtype selective agonist A-61603, L-765314 appears to be selective versus the R1a receptor up to a dose of 0.3 mg/kg. The results of hypotensive potency in rats show that both L-765314 and terazosin tend to decrease heart rate (about 25 bpm at 1 mg/kg iv).

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