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Beta-1 adrenergic receptor

Historical Context and General Information: – In 1933, W. B. Cannon postulated the existence of two chemical transmitters, E and I sympathins. – Raymond Ahlquist […]

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Historical Context and General Information:
– In 1933, W. B. Cannon postulated the existence of two chemical transmitters, E and I sympathins.
– Raymond Ahlquist established the concept of adrenaline acting on alpha and beta receptors in 1948.
– Eli Lilly Laboratories synthesized the first beta-blocker, dichloroisoproterenol.
– The Beta-1 adrenergic receptor (ADRB-1) is a transmembrane protein belonging to the G-Protein-Coupled Receptor (GPCR) family.
– GPCRs have seven transmembrane helices with intracellular and extracellular loops and are coupled to heterotrimeric G-proteins.
– Ligand binding induces a conformational change in ADRB-1, activating downstream signaling pathways.

Function and Clinical Significance of ADRB-1:
– ADRB-1 is activated by adrenaline and noradrenaline, regulating glucose metabolism, peripheral clock synchronization, neuropeptide release, and immunity.
– Dysregulation of the β-AR signaling pathway is associated with cardiac failure.
– ADRB-1 plays a crucial role in various physiological functions and is implicated in metabolic disorders like diabetes and obesity.
– Circadian oscillations in catecholamine signals influence immune cell function.
– Familial Natural Short Sleep (FNSS) is linked to a rare mutation in the ADRB-1 receptor.

Polymorphisms and Mutation Effects:
– Polymorphisms in ADRB-1 include changes at codon positions 49 and 389, affecting blood pressure, heart rates, and cardiac functions.
– The ADRB1-A187V mutation is associated with FNSS behavior traits and altered cAMP production.
– Mice with the mutation show increased activity time and altered sleep patterns.
– Mutations in ADRB-1 affect protein stability, post-translational modifications, and sleep-wake behavior.

Pharmaceutical Interventions and Agonists:
– Medications target ADRB-1 functions for regulating blood pressure and cardiac output.
– Dobutamine, isoprenaline, denopamine, xamoterol, and isoproterenol are agonists targeting ADRB-1 for various cardiovascular conditions.
– Caution is advised against illicit drug use affecting ADRB-1 due to potential medical emergencies.

Studies, Interactions, and External Resources:
– Various studies focus on ADRB-1 polymorphisms, genetic variations, and the receptor’s role in cardiovascular responses.
– Interactions with beta-arrestin, PSD-95, MAGI-2, and G protein-coupled receptor kinase 5 influence ADRB-1 behavior.
– External resources like the UCSC Genome Browser, IUPHAR Database, and UniProt provide detailed information on the Beta-1 adrenergic receptor.

Beta-1 adrenergic receptor (Wikipedia)

The beta-1 adrenergic receptor1 adrenoceptor), also known as ADRB1, can refer to either the protein-encoding gene (gene ADRB1) or one of the four adrenergic receptors. It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein that is expressed predominantly in cardiac tissue. In addition to cardiac tissue, beta-1 adrenergic receptors are also expressed in the cerebral cortex.

Available structures
PDBOrtholog search: PDBe RCSB
AliasesADRB1, ADRB1R, B1AR, BETA1AR, RHR, adrenoceptor beta 1, FNSS2
External IDsOMIM: 109630 MGI: 87937 HomoloGene: 20171 GeneCards: ADRB1
RefSeq (mRNA)



RefSeq (protein)



Location (UCSC)Chr 10: 114.04 – 114.05 MbChr 19: 56.71 – 56.72 Mb
PubMed search
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