Target intelligence / Profile preview

Serotonin 6 receptor and Adrenergic receptor (5-HT6 receptor and Adrenergic receptor)

Target
5-HT6 receptor and Adrenergic receptor
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The Serotonin 6 receptor (5-HT6 receptor) is a G protein-coupled receptor highly expressed in the central nervous system, where it modulates neurotransmission, cognition, learning, and mood, and is a therapeutic target for psychiatric and neurodegenerative disorders[1][3]. The Adrenergic receptors are a family of G protein-coupled receptors (including alpha and beta subtypes) that respond to catecholamines (epinephrine, norepinephrine) and mediate effects in the cardiovascular system, smooth muscle, metabolism, and central and peripheral nervous system. They are primary targets for drugs treating hypertension, heart failure, asthma, and anxiety disorders[3].

Other names
5-HT6 receptorAlpha-adrenergic receptorBeta-adrenergic receptorAdrenoceptor
02

Mechanism of action

Serotonin 6 receptor: Agonism or antagonism, usually CNS-selective, leading to modulation of cAMP signaling via Gs protein coupling, affecting cognition, mood, feeding. Adrenergic receptors: Agonism or antagonism, modulating G protein-coupled signaling (Gs, Gi/o, Gq/11) to affect heart rate, vascular tone, smooth muscle contraction/relaxation, neurotransmitter release

03

Biological functions

Signal transductionModulation of neurotransmissionRegulation of cognition, learning, mood, and feeding behaviorRegulation of cardiovascular function, smooth muscle tone, metabolism, CNS activity
04

Disease associations

Neurodegenerative diseaseAlzheimer's diseaseDepressionAnxietyObesitySchizophreniaCardiovascular diseaseHypertensionHeart failureAsthmaAnxiety disordersOther CNS and peripheral pathologies
05

Safety considerations

Serotonin 6 receptor: Potential for CNS-specific side effects (e.g., cognitive impairment, psychiatric symptoms), but generally favorable safety in trialsAdrenergic receptors: Cardiovascular side effects (arrhythmia, hypotension/hypertension), CNS effects (anxiety, tremor), numerous peripheral effects depending on receptor subtype
06

Interacting drugs

SB-399885

10 more in the full profile.

07

Biomarkers

No validated routine clinical biomarkers for 5-HT6 or adrenergic receptor expression/activity in current practice; response to drugs may be inferred from pharmacodynamic markers (e.g., cognitive performance, heart rate)

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