Target intelligence / Profile preview

Alpha-1L adrenergic receptor (Alpha-1L)

Target
Alpha-1L
Molecular classification
G protein-coupled receptor, Adrenergic receptor family
01

Overview

The Alpha-1L adrenergic receptor is a functional phenotype of the alpha-1A adrenergic receptor (ADRA1A), characterized by its uniquely low affinity for the antagonist prazosin. It is the predominant alpha-1 adrenoceptor subtype found in the human lower urinary tract, specifically within the prostatic smooth muscle, bladder neck, and urethra. Under physiological conditions, its activation by norepinephrine leads to smooth muscle contraction, which regulates urinary resistance. In the context of disease, overexpression or overactivity of this receptor contributes to the dynamic component of urinary obstruction in benign prostatic hyperplasia (BPH). Therapeutic interventions typically involve the use of uroselective alpha-1 blockers, such as tamsulosin and silodosin, which antagonize these receptors to relax the prostatic and urethral smooth muscle, thereby improving urine flow and alleviating lower urinary tract symptoms.

Other names
Low-affinity alpha-1A adrenoceptoralpha-1L adrenoceptoralpha-1L ARProstatic alpha-1 adrenoceptor
02

Mechanism of action

Antagonism of the post-synaptic alpha-1L receptors in the prostate and urethra, leading to smooth muscle relaxation and reduced resistance to urinary outflow.

03

Biological functions

Signal transductionSmooth muscle contractionRegulation of urinary flow
04

Disease associations

Benign prostatic hyperplasia (BPH)Lower urinary tract symptoms (LUTS)Urethral obstruction
05

Safety considerations

Intraoperative Floppy Iris Syndrome (IFIS)Retrograde ejaculationOrthostatic hypotensionDizziness
06

Interacting drugs

Tamsulosin

4 more in the full profile.

07

Biomarkers

International Prostate Symptom Score (IPSS)Peak urinary flow rate (Qmax)Post-void residual (PVR) volume

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