1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
  3. L-765314


Cat. No.: HY-101385
Handling Instructions

L-765314 is a potent and selective α1b adrenergic receptor antagonist with Kis of 5.4 nM and 2.0 nM for rat and human α1b adrenergic receptor, respectively.

For research use only. We do not sell to patients.

L-765314 Chemical Structure

L-765314 Chemical Structure

CAS No. : 189349-50-6

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L-765314 is a potent and selective α1b adrenergic receptor antagonist with Kis of 5.4 nM and 2.0 nM for rat and human α1b adrenergic receptor, respectively.

IC50 & Target

Ki: 5.4±0.6 nM (rat α1b receptor ), 2.0±0.66 nM (human α1b receptor), 50±8 nM (rat α1d receptor), 34±6 nM (human α1d receptor), 500±20 nM (rat α1b receptor ), 420±62 nM (human α1b receptor)[1].

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[1].

In Vivo

The results of plasma assayed by liquid chromatograph/mass spectrometer (LCMS) show that the mean Cmax of L-765314 (A322312) is 1.05 μM and the t1/2 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)[1].

Molecular Weight







O=C(N1[[email protected]](C(NC(C)(C)C)=O)CN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)OCC4=CC=CC=C4


Room temperature in continental US; may vary elsewhere.


Please store the product under the recommended conditions in the Certificate of Analysis.

Animal Administration

The potency of terazosin and L-765314 for inhibiting the pressor responses to phenylephrine and A-61603 is evaluated in anesthetized male Sprague-Dawley rats (n=4). The rats are dosed i.v with either vehicle or ascending doses of test compounds, and the peak changes in mean arterial pressure are measured. The dose of antagonist eliciting a 25 mmHg decrease in mean arterial pressure (AD25) is calculated as an index of hypotensive potency. The rats are dosed i.v with L-765314 at 3 mg/kg , and the plasma is assayed by LCMS for parent compound[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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L-765314L765314L 765314Adrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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