Target intelligence / Profile preview

Octopamine receptor, alpha-adrenergic type 1 (Octα1R)

Target
Octα1R
Molecular classification
G protein-coupled receptor, Receptor, Rhodopsin-like receptor
01

Overview

The Octopamine receptor, alpha-adrenergic type 1 (Octα1R) is a G protein-coupled receptor (GPCR) found in invertebrates, structurally and functionally similar to mammalian adrenergic alpha-1 receptors[4][7]. It binds the biogenic amine octopamine, which acts as the invertebrate counterpart to norepinephrine, and mediates physiological processes such as locomotion, aggression, arousal, modulation of muscle contraction, and metabolic regulation[3][4][5]. Octα1R (sometimes also called OctαR or OAMB in Drosophila) is notable for orchestrating nervous and muscular system outputs and is involved in behavioral regulation, especially in response to stress or environmental challenges. It is not expressed in vertebrates; in these animals, octopamine shows low affinity for adrenergic and trace amine-associated receptors, but with no established physiological function[4][7]. The invertebrate Octα1R is a critical target for insecticides due to its absence in mammals, making it a selective neuro-toxicological site[4].

Other names
OctαRalpha-adrenergic-like octopamine receptorOAMB (in Drosophila; though this is an isoform-specific name)alpha-1 adrenergic-like octopamine receptor
02

Mechanism of action

Agonists (octopamine and synthetic compounds) stimulate cAMP or calcium signaling depending on the specific receptor and isoform - Antagonists (mianserin, phentolamine, chlorpromazine) block octopaminergic signaling

03

Biological functions

Signal transductionNeuromodulationRegulation of locomotionModulation of aggression and arousalMuscle contraction regulation
04

Disease associations

Other (target of insecticides in pest control, not directly implicated in mammalian disease)
05

Safety considerations

Selectivity is a concern in insecticide development to avoid off-target effects in beneficial insects or non-target organismsNot applicable to human therapeutics, as specific octopamine receptors are not present in vertebrates[4][7]
06

Interacting drugs

Mianserin

4 more in the full profile.

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