Alpha-2B adrenergic receptor

UniProt P18089 Organism Homo sapiens Gene ADRA2B, ADRA2L1, ADRA2RL1

Also known as: ADRA2B, ADRA2L1, ADRA2RL1

Function

Alpha-2 adrenergic receptors are G protein-coupled receptors for catecholamines that activate G(i/o) protein pathway, thereby promoting adenylyl cyclase inhibition, ERK1/2 stimulation, and voltage-gated calcium channels suppression. Control a variety of physiological processes, such as regulation of blood pressure, lipolysis and insulin release. The rank order of potency for agonists of ADRA2B is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phentolamine > mianserine > spiperone > prazosin > alprenolol > propanolol > pindolol.

Classification

Family (Pfam): PF00001 7tm_1
InterPro: ADR_fam, ADRA2B_rcpt, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM
Functional cluster: G Protein-Coupled Receptors

Experimental structures · PDB · 2

6K41 EM 2.90A
6K42 EM 4.10A

A predicted model is available from AlphaFold.

Gene Ontology · 20

Disease associations

epilepsy, familial adult myoclonic, 2 MONDO:0011930

Drugs targeting this protein · 39

IDAZOXAN antagonist
LABETALOL HYDROCHLORIDE antagonist
TIZANIDINE HYDROCHLORIDE agonist
APRACLONIDINE HYDROCHLORIDE agonist
BRIMONIDINE TARTRATE agonist
TETRAHYDROZOLINE HYDROCHLORIDE agonist
METHYLDOPATE HYDROCHLORIDE agonist
GUANFACINE HYDROCHLORIDE agonist
GUANABENZ ACETATE agonist
HYDROXYAMPHETAMINE HYDROBROMIDE agonist
PHENOXYBENZAMINE HYDROCHLORIDE antagonist
OXYMETAZOLINE HYDROCHLORIDE agonist
DIPIVEFRIN HYDROCHLORIDE agonist
PHENTOLAMINE MESYLATE antagonist
FIPAMEZOLE antagonist
XYLOMETAZOLINE HYDROCHLORIDE agonist
EPINEPHRINE BITARTRATE agonist
CLONIDINE agonist
NOREPINEPHRINE BITARTRATE agonist
EPHEDRINE SULFATE agonist
MOXISYLYTE antagonist
TOLAZOLINE HYDROCHLORIDE antagonist
CLONIDINE HYDROCHLORIDE agonist
NAPHAZOLINE HYDROCHLORIDE agonist
LOFEXIDINE HYDROCHLORIDE agonist
AVIPTADIL antagonist
DROXIDOPA agonist
DEXMEDETOMIDINE HYDROCHLORIDE agonist
FADOLMIDINE HYDROCHLORIDE agonist
ESMIRTAZAPINE MALEATE antagonist
EPHEDRINE HYDROCHLORIDE agonist
ERGOLOID MESYLATES antagonist
ERGOTAMINE TARTRATE agonist
CELIPROLOL antagonist
MEPHENTERMINE SULFATE agonist
METHYLDOPA agonist
MIRTAZAPINE antagonist
LEVONORDEFRIN agonist
EPINEPHRINE agonist

Related proteins · sequence + function similarity

Co-cited proteins · studied together in the literature

Neurabin-2 1 shared papers
Ras-related protein Rab-43 1 shared papers
Ras-related protein Rab-26 1 shared papers
Alpha-2A adrenergic receptor 1 shared papers
ADP-ribosylation factor-binding protein GGA3 1 shared papers
ADP-ribosylation factor-binding protein GGA2 1 shared papers
ADP-ribosylation factor-binding protein GGA1 1 shared papers

Literature · 13 cited papers

Activation of the alpha2B adrenoceptor by the sedative sympatholytic dexmedetomidine. Nat. Chem. Biol. · 2020
The GTPase Rab43 Controls the Anterograde ER-Golgi Trafficking and Sorting of GPCRs. Cell Rep. · 2017
Regulation of alpha2B-Adrenergic Receptor Cell Surface Transport by GGA1 and GGA2. Sci. Rep. · 2016
GGA3 Interacts with a G Protein-Coupled Receptor and Modulates Its Cell Surface Export. Mol. Cell. Biol. · 2016
The alpha2B-adrenergic receptor is mutant in cortical myoclonus and epilepsy. Ann. Neurol. · 2014
Rab26 modulates the cell surface transport of alpha2-adrenergic receptors from the Golgi. J. Biol. Chem. · 2012
Generation and annotation of the DNA sequences of human chromosomes 2 and 4. Nature · 2005
The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
Cloning, characterisation and identification of several polymorphisms in the promoter region of the human alpha2B-adrenergic receptor gene. Biochem. Pharmacol. · 2004
Polymorphic deletion of three intracellular acidic residues of the alpha 2B-adrenergic receptor decreases G protein-coupled receptor kinase-mediated phosphorylation and desensitization. J. Biol. Chem. · 2001
In vitro amplification by polymerase chain reaction of a partial gene encoding the third subtype of alpha-2 adrenergic receptor in humans. Biochem. Biophys. Res. Commun. · 1990
Cloning, expression, and pharmacological characterization of a human alpha 2B-adrenergic receptor. Mol. Pharmacol. · 1990
… and 1 more in the literature graph

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