Target intelligence / Profile preview

Alpha-Adrenergic Receptor (Alpha-1A/Alpha-1B/Alpha-2A) (α1A/α1B/α2A-AR)

Target
α1A/α1B/α2A-AR
Molecular classification
G protein-coupled receptor (GPCR), Alpha-adrenergic receptor, Receptor
01

Overview

Alpha-adrenergic receptors are a class of G protein-coupled receptors (GPCRs) that respond to the endogenous catecholamines norepinephrine and epinephrine. They play a central role in mediating sympathetic nervous system responses, particularly those involving smooth muscle contraction, cardiovascular regulation, and neurotransmitter release. The subtypes alpha-1A and alpha-1B are coupled to Gq proteins and primarily located postsynaptically to induce smooth muscle contraction. Alpha-2A is coupled to Gi proteins, primarily located presynaptically, and inhibits norepinephrine release. These receptors are implicated in various clinical conditions like hypertension and ADHD, making them therapeutic targets for various drugs.

Other names
Adrenergic Receptor Alpha 1AAdrenergic Receptor Alpha 1BAdrenergic Receptor Alpha 2AADRA1AADRA1BADRA2Aalpha1A-adrenergic receptoralpha1B-adrenergic receptoralpha2A-adrenergic receptor
02

Mechanism of action

Agonist or antagonist at alpha-adrenergic receptors influencing downstream signaling pathways (Gq/Gi) to modulate smooth muscle contraction, neurotransmitter release, and other physiological processes.

03

Biological functions

Signal transductionSmooth muscle contractionVasoconstrictionNeurotransmitter release regulationPlatelet aggregationMydriasisUrinary retentionEjaculation facilitationCardiovascular regulation
04

Disease associations

HypertensionAttention Deficit Hyperactivity Disorder (ADHD)Opioid Use DisorderSubstance Abuse Disorders
05

Safety considerations

Cardiovascular side effects (e.g., changes in blood pressure)Central nervous system effects (e.g., dizziness, sedation)Drug interactions
06

Interacting drugs

Norepinephrine

4 more in the full profile.

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