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Background of Adrenergic Receptors
The adrenergic receptors, also known as adrenoceptors, are a class of G protein-coupled receptors. The adrenergic receptors have served as targets of various catecholamines and medications, such as norepinephrine, epinephrine, beta-blockers, beta-2 (β2) agonists, and alpha-2 (α2) agonists.
Fig.1. Crystal Structures of α2AAR. (Qu, 2019)
Distribution and Function of Adrenergic Receptors
Adrenergic receptors can be observed in many cell types, the binding of a catecholamine to the adrenergic receptor would always stimulate the sympathetic nervous system (SNS). Adrenergic receptors are important membrane-bound proteins that mediate the physiological effects of norepinephrine, epinephrine, as well as adrenergic drugs.
Subtypes and Mechanisms of Adrenergic Receptors
Adrenergic receptors consist of three major types: alpha-1-adrenoceptors, alpha-2-adrenoceptors, and beta-adrenoceptors, each of which can be subdivided into three subtypes.
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Receptor
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Gene
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Mechanism
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Agonists
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Antagonists
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α1 receptor
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ADRA1A
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α1 receptor activating phospholipase C through Gq/11.
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α1 receptor activating the mitogen-activated protein kinase pathway.
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Cirazoline
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Methoxamine
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Midodrine
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Sdz-nvi-085
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Arotinolol
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Indoramin
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Quetiapine
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Trazodone
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α2 receptor
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ADRA2A
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α2 receptor inhibiting adenylate cyclase activity and downregulating cAMP formation through the Gi/Go mechanism.
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4-NEMD
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Apraclonidine
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Fadolmidine
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Mivazerol
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Idazoxan
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1-PP
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Olanzapine
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Phentolamine
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β1 receptor
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ADRB1
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β1 receptor activating adenylate cyclase through Gs.
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β1 receptor initiating a cAMP-dependent pathway via adenylate cyclase.
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Denopamine
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Dobutamine
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Xamoterol
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Acebutolol
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Atenolol
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Bisoprolol
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Esmolol
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Vortioxetine
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β2 receptor
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ADRB2
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β2 receptor coupling to Gi that response to the ligand is highly localized within cells.
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β2 receptor activating adenylate cyclase through Gs.
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Bitolterol
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Pirbuterol
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Formoterol
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Indacaterol
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Propranolol
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ICI-118,551
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Butoxamine
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β3 receptor
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ADRB3
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β3 receptor activating adenylate cyclase through the action of the G proteins of the type Gs.
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Amibegron
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BRL-37344
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L-742,791
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Ro40-2148
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L-748,328
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L-748,337
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SR 59230A
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Assay List of Adrenergic Receptors
Creative Biolabs can provide a range of assays of adrenergic receptors. You can choose the assay in the list or contact us for more information:
ADRA1A ADRA1B ADRA1D ADRA2A ADRA2B ADRA2C ADRB1 ADRB2 ADRB3
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Assay No.
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Assay Name
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Host Cell
|
Assay Type
|
Datasheet
|
|
cAMP Assay
|
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S01YF-1122-KX178
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Magic™ Human ADRA1A In Vitro cAMP Assay
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CHO-K1
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cAMP Assay
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|
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Calcium Flux Assay
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S01YF-0722-KX72
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Magic™ Human ADRA1A In Vitro Calcium Assay & Binding Assay, HEK293
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HEK293
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Calcium Flux Assay
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|
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IP1 Assay
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S01YF-0722-KX3
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Magic™ Human ADRA1A In Vitro Agonist & Antagonist IP1 Assay, HEK293
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HEK293
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IP1 Assay
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|
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Radioligand Binding Assay
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S01YF-1122-KX180
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Magic™ Human ADRA1A In Vitro Radioligand Binding Assay
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CHO-K1
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Radioligand Binding Assay
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|
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Assay No.
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Assay Name
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Host Cell
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Assay Type
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Datasheet
|
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Calcium Flux Assay
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S01YF-0722-KX73
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Magic™ Human ADRA1B In Vitro Calcium Assay & Binding Assay, HEK293
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HEK293
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Calcium Assay; Binding Assay
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|
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IP1 Assay
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S01YF-1122-KX182
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Magic™ Human ADRA1B In Vitro IP1 Assay
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CHO-K1
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IP1 Assay
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|
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Radioligand Binding Assay
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S01YF-1122-KX183
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Magic™ Human ADRA1B In Vitro Radioligand Binding Assay
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CHO-K1
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Radioligand Binding Assay
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|
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Assay No.
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Assay Name
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Host Cell
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Assay Type
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Datasheet
|
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Calcium Flux Assay
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S01YF-0722-KX74
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Magic™ Human ADRA1D In Vitro Calcium Assay & Binding Assay, HEK293
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HEK293
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Calcium Assay; Binding Assay
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|
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S01YF-1122-KX184
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Magic™ Human ADRA1D In Vitro Calcium Flux Assay
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CHO-K1
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Calcium Flux Assay
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|
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IP1 Assay
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S01YF-1122-KX185
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Magic™ Human ADRA1D In Vitro IP1 Assay
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CHO-K1
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IP1 Assay
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|
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Radioligand Binding Assay
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S01YF-1122-KX186
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Magic™ Human ADRA1D In Vitro Radioligand Binding Assay
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CHO-K1
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Radioligand Binding Assay
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|
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Assay No.
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Assay Name
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Host Cell
|
Assay Type
|
Datasheet
|
|
cAMP Assay
|
|
S01YF-0722-KX4
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Magic™ Human ADRA2A In Vitro Agonist & Antagonist cAMP Assay, HEK293
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HEK293
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cAMP Assay
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|
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Calcium Flux Assay
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S01YF-0722-KX75
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Magic™ Human ADRA2A In Vitro Calcium Assay, CHO-K1-Ga15
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CHO-K1-Ga15
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Calcium Flux Assay
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|
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S01YF-0722-KX76
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Magic™ Human ADRA2A In Vitro Calcium Assay, HEK293-Ga16
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HEK293-Ga16
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Calcium Flux Assay
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|
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S01YF-1122-KX187
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Magic™ Human ADRA2A In Vitro Calcium Flux Assay
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HEK293-Gα16
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Calcium Flux Assay
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|
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[35S]GTPγS Binding Assay
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S01YF-1122-KX189
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Magic™ Human ADRA2A In Vitro [35S]GTPγS binding Assay
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CHO-K1
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[35S]GTPγS binding Assay
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|
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Radioligand Binding Assay
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S01YF-1122-KX190
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Magic™ Human ADRA2A In Vitro Radioligand Binding Assay
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CHO-K1
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Radioligand Binding Assay
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|
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Assay No.
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Assay Name
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Host Cell
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Assay Type
|
Datasheet
|
|
Calcium Flux Assay
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|
S01YF-0722-KX77
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Magic™ Human ADRA2B In Vitro Calcium Assay, HEK293-Ga15
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HEK293-Ga15
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Calcium Flux Assay
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|
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S01YF-1122-KX191
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Magic™ Human ADRA2B In Vitro Calcium Flux Assay
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CHO-K1
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Calcium Flux Assay
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|
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IP1 Assay
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|
S01YF-0722-KX5
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Magic™ Human ADRA2B In Vitro Agonist & Antagonist IP1 Assay, HEK293
|
HEK293
|
IP1 Assay
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|
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Radioligand Binding Assay
|
|
S01YF-1122-KX193
|
Magic™ Human ADRA2B In Vitro Radioligand Binding Assay
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CHO-K1
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Radioligand Binding Assay
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|
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Assay No.
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Assay Name
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Host Cell
|
Assay Type
|
Datasheet
|
|
cAMP Assay
|
|
S01YF-0722-KX6
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Magic™ Human ADRA2C In Vitro Agonist & Antagonist cAMP Assay, HEK293
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HEK293
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cAMP Assay
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|
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Calcium Flux Assay
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|
S01YF-0722-KX78
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Magic™ Human ADRA2C In Vitro Calcium Assay, HEK293-Ga15
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HEK293-Ga15
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Calcium Flux Assay
|
|
|
S01YF-1122-KX194
|
Magic™ Human ADRA2C In Vitro Calcium Flux Assay
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CHO-K1-Ga16
|
Calcium Flux Assay
|
|
|
Radioligand Binding Assay
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|
S01YF-1122-KX197
|
Magic™ Human ADRA2C In Vitro Radioligand Binding Assay
|
CHO-K1
|
Radioligand Binding Assay
|
|
|
Assay No.
|
Assay Name
|
Host Cell
|
Assay Type
|
Datasheet
|
|
Calcium Flux Assay
|
|
S01YF-1122-KX198
|
Magic™ Human ADRB1 In Vitro Calcium Flux Assay
|
CHO-K1-Ga16
|
Calcium Flux Assay
|
|
|
Radioligand Binding Assay
|
|
S01YF-1122-KX200
|
Magic™ Human ADRB1 In Vitro Radioligand Binding Assay
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CHO-K1
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Radioligand Binding Assay
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|
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Assay No.
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Assay Name
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Host Cell
|
Assay Type
|
Datasheet
|
|
cAMP Assay
|
|
S01YF-0722-KX80
|
Magic™ Human ADRB2 In Vitro cAMP Assay & Binding Assay, HEK293-CRE-GFP
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HEK293-CRE-GFP
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cAMP Assay; Binding Assay
|
|
|
Radioligand Binding Assay
|
|
S01YF-0722-KX79
|
Magic™ Human ADRB2 In Vitro Reporter Assay & Binding Assay, HEK293
|
HEK293
|
Reporter Assay; Binding Assay
|
|
|
S01YF-1122-KX202
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Magic™ Human ADRB2 In Vitro Radioligand Binding Assay
|
CHO-K1
|
Radioligand Binding Assay
|
|
|
Assay No.
|
Assay Name
|
Host Cell
|
Assay Type
|
Datasheet
|
|
cAMP Assay
|
|
S01YF-0722-KX81
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Magic™ Human ADRB3 In Vitro cAMP Assay & Binding Assay, HEK293
|
HEK293
|
cAMP Assay; Binding Assay
|
|
|
S01YF-1122-KX204
|
Magic™ Human ADRB3 In Vitro cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
|
Calcium Flux Assay
|
|
S01YF-1122-KX203
|
Magic™ Human ADRB3 In Vitro Calcium Flux Assay
|
CHO-K1-Ga16
|
Calcium Flux Assay
|
|
|
Radioligand Binding Assay
|
|
S01YF-1122-KX205
|
Magic™ Human ADRB3 In Vitro Radioligand Binding Assay
|
CHO-K1
|
Radioligand Binding Assay
|
|
Published Data
|
Paper Title
|
Neurobiology of Cancer: The Role of β-Adrenergic Receptor Signaling in Various Tumor Environments
|
|
Journal
|
International Journal of Molecular Sciences
|
|
Published
|
2020
|
|
Abstract
|
The tumor microenvironment and macroenvironment, as well as the psychosocial and spiritual "environment", can influence cancer initiation and progression. Studies have shown that the nervous system can regulate cancer-related processes at both the tumor microenvironmental level and the macroenvironmental level through neural and humoral pathways. Over the past few decades, nervous system influences on cancer initiation, progression, and metastatic development have been largely mediated by the sympathetic-adrenal system through β-adrenergic receptor signaling. In this paper, we provide a novel view of the role of β-adrenoceptor signaling in the tumor micro- and macroenvironment and in regulating the influence of the psychosocial and spiritual environment. In addition, our field team conducted intensive research on potential prevention and treatment.
|
|
Result
|
In this review, it has been proven that β-adrenergic signaling represents important mechanisms to affect cancer via somatic, psychosocial, and noetic factors. Preclinical and clinical studies showed that attenuated β-adrenergic signaling reduces cancer development and progression. The importance of this signaling supported by preclinical and clinical findings showed that the attenuation of β-adrenergic signaling reduced cancer development and progression both in animal models of cancer and in cancer patients. However, it should be noted that the data from clinical studies are not completely clear. Therefore, the introduction of compounds that inhibit β-adrenergic signaling in cancer therapy requires a more precise characterization of the factors responsible for this observed ambiguity. Likewise, attenuation of β-adrenergic signaling using nonpharmacologic interventions requires further detailed and multidisciplinary-oriented studies.
 Fig.2. β-adrenergic signaling mediates the effect of the brain on the tumor micro- and macroenvironments. (Mravec, et al., 2020)
|
References
-
Qu, L.; et al. Structural basis of the diversity of adrenergic receptors. Cell reports. 2019, 29(10): 2929-2935. e4.
-
Mravec, B.; et al. Neurobiology of cancer: the role of β-adrenergic receptor signaling in various tumor environments. International Journal of Molecular Sciences. 2020, 21(21): 7958.
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