Adrenergic GPCR Family Subtypes and Products

What Are Adrenergic Receptors?

Adrenergic receptors are a family of G protein-coupled receptors (GPCRs) targeted by catecholamines, such as norepinephrine and epinephrine, that consists of two main groups: ɑ receptors and β receptors. ɑ agonists are used to treat rhinitis, and ɑ antagonists can be used to treat pheochromocytoma. β agonists are used in the treatment of heart failure, circulatory shock, or anaphylaxis, while β antagonists can treat conditions such as heart arrhythmia, coronary artery disease, hyperthyroidism, and glaucoma.

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Adrenergic Receptor Information

Clickable Text Interaction

alpha1A

alpha1B

alpha1D

alpha2A

alpha2B

alpha2C

beta1

beta2

beta3

The α1a-adrenoceptor is highly expressed in human vasculature. As with the other α1-ARs, α1a is used by the sympathetic nervous system to regulate systemic arterial blood pressure and blood flow. The α1-ARs also play a major role in cardiac and vascular smooth muscle cells. The knockout mouse models lacking the α1a-adrenergic receptors have highlighted the potential implications of this receptor subtype in variety of functions including the regulation of renal artery contractions, smooth muscle contractions, and vasoconstriction.

The α1B-adrenoceptor expresses in brain, heart, kidney, and artery of various mammalian species and mediate diverse effects on cardiac functions, muscle contractions and cell growth. The knockout mouse models lacking the α1b-adrenergic receptor has highlighted the potential implication of this receptor subtype in variety of functions including the regulation of blood pressure, glucose homeostasis, reproduction, and the rewarding response to drugs of abuse. In vitro and in vivo studies also indicate that the α1b gene can function as an oncogene inducing neoplastic transformation.

The α1D-adrenoceptor is found mainly intracellularly. As with the other α1-ARs, α1D is used by the sympathetic nervous system to regulate systemic arterial blood pressure and blood flow. The α1-ARs also play a major role in mediating growth responses in cardiac and vascular smooth muscle cells. Studies have shown that the α1D-adrenoceptor is responsible for regulating arterial blood pressure by vasoconstriction. Knockout mice lacking the α1D gene maintained significantly lower basal systolic and mean arterial blood pressures, compared to wild type mice. Also, the contractile response of the aorta and the pressor response of isolated perfused mesenteric arterial beds to α1-AR stimulation were reduced in mice lacking α1D.

Adrenergic α2a receptor belongs to the group of nine adrenoceptors that mediate the biological actions of adrenaline and noradrenaline. The α2a receptor is expressed in the brain, spleen, kidney, heart and gastrointestinal tract. It is centrally predominant and exerts a tonic sympathoinhibitory function, whereas peripherally it has a vasoconstrictive effect. The α2a receptor is also involved in sedation, digestive functions and analgesia.

Adrenergic α2b receptor belongs to the group of nine adrenoceptors that mediate the biological actions of the endogenous catecholamines adrenaline and noradrenaline. While α2a receptor exerts a tonic sympathoinhibitory function, the α2b is responsible for the central hypertensive sympathoexcitatory response. Development of agents capable of selectively activating the α2a or blocking the α2b may further improve our capability to treat hypertension, ischemic heart disease and heart failure. The α2b receptor also contributes to the peripheral regulation of vascular tone.

The human adrenergic α2c receptor is a 458-amino acid, 7- transmembrane protein. It belongs to the group of nine adrenoceptors that mediate the biological actions of the endogenous catecholamines adrenaline and noradrenaline. All three alpha2-receptor subtypes may operate as presynaptic inhibitory feedback receptors to control the release of neurotransmitters. The α2c receptor is of particular importance as it appears to regulate venous vasoconstriction.

The human ß1-adrenergic receptor is a 477–amino acid protein found in various heart and brain tissues. ß1 has an important role in the contractile action of valves in cardiac and digestive systems.

The human ß2-adrenergic receptor was the first 7- transmembrane receptor for a hormone or neurotransmitter to have its crystal structure solved. It has been suggested that the β2-adrenoceptor may form homodimers as well as oligomers with other receptors. The β2-adrenoceptor mediates the actions of catecholamines in multiple tissues. They are responsible for relaxation of vascular, uterine, and airway smooth muscle, and are involved in metabolic and endocrine functions.

The ß3-adrenoceptor is also known as the atypical beta- adrenoceptor. It was considered as a potential anti-obesity target by increasing energy expenditure and lipolysis in brown and white adipose tissues of rodents. The functional receptor has been demonstrated in a variety of other tissues including blood vessel, gastrointestinal tract, muscle, and retinal endothelial cells, and its agonist evokes relaxation in some of these tissues such as gall bladder, stomach, small intestine, prostate, colon and bladder.

Adrenergic Cell Lines

Receptor Family	Receptor	Species	Parental	Stable Cell Lines	Division-Arrested Cells	Membranes
Adrenergic	alpha1A	human	CHO-K1	C1431-1	DC1431-1	MC1431-1
	alpha1B	human	CHO-K1	C1432-1	DC1432-1	MC1432-1
	alpha1D	human	CHO-K1	C1433-1	DC1433-1	MC1433-1
	alpha2A	human	CHO-K1	C1434-1	DC1434-1	MC1434-1
	alpha2A	human	CHO-K1	C1434-1a	DC1434-1a	MC1434-1a
	alpha2A	human	CHO-K1 Gqi5	CG1434-1	DCG1434-1	MCG1434-1
	alpha2B	human	CHO-K1	C1435-1	DC1435-1	MC1435-1
	alpha2B	human	CHO-K1 Gqi5	CG1435-1	DCG1435-1	MCG1435-1
	alpha2C	human	CHO-K1	C1436-1	DC1436-1	MC1436-1
	alpha2C	human	CHO-K1 Gqi5	CG1436-1	DCG1436-1	MCG1436-1
	beta1	human	HEK293T	H1437	H1437	H1437
	beta1	human	CHO-K1	C1437-1	DC1437-1	MC1437-1
	beta2	human	CHO-K1	C1438-1a	DC1438-1a	MC1438-1a
	beta2	human	HEK293T β-Arrestin1	CA1438BA1	DCA1438BA1	MCA1438BA1
	beta2	human	HEK293T β-Arrestin2	CA1438BA2	DCA1438BA2	MCA1438BA2
	beta3	human	HEK293T	C1439a	DC1439a	MC1439a