Adrenergic receptor From Wikipedia, the free encyclopedia


Noradrenaline The adrenergic receptors (or adrenoceptors) are a class of G protein-coupled receptors that are targets of the catecholamines, especially noradrenaline (norepinephrine) and adrenaline (epinephrine). Although dopamine is a catecholamine, its receptors are in a different category. Many cells possess these receptors, and the binding of an agonist will generally cause a sympathetic response (e.g. the fight-or-flight response). For instance, the heart rate will increase and the pupils will dilate, energy will be mobilized, and blood flow diverted from other non-essential organs to skeletal muscle. Contents [hide] 1 Subtypes o 1.1 Roles in circulation o 1.2 Comparison o 1.3 receptors  1.3.1 1 receptor  1.3.2 2 receptor o 1.4 receptors  1.4.1 1 receptor

The G protein associates with adenylate . All three are linked to Gs proteins (although 2 also couples to Gi)[1]. Isoprenaline is a selective agonist. 2 and 3.1.4.  and . Downstream effectors of cAMP include cAMP-dependent protein kinase(PKA). which mediates some of the intracellular events following hormone binding.3 3 receptor 2 See also 3 References 4 Further reading 5 External links  [edit]Subtypes There are two main groups of adrenergic receptors. several subtypes. which in turn are linked to adenylate cyclase.2 2 receptor  1.4. receptors have the subtypes 1. Agonist binding thus causes a rise in the intracellular concentration of the second messenger cAMP. with  receptors have the subtypes 1 (a Gq coupled receptor) and 2 (a Gi coupled receptor). that associates with an heterotrimeric G protein. Epinephrine binds its receptor. Phenylephrine is a selective agonist of the receptor.

they . 2. 1 couples to Gq. when activated. 2 or -adrenergic receptors. smooth muscle relaxation. resulting in e. which results in increased intracellular Ca2+ which results in smooth muscle contraction.) The mechanism of adrenergic receptors. on the other hand. causing vasoconstriction and vasodilation.. Although receptors are less sensitive to epinephrine. spreading the signal (more details.cyclase that converts ATP to cAMP.g.and -adrenoreceptors. and increases intracellular cAMP activity. heart muscle contraction. receptors couple to Gs. resulting in e.. which causes a decrease of cAMP activity. respectively. smooth muscle relaxation andglycogenolysis.g. couples to Gi. [edit]Roles in circulation Adrenaline reacts with both . Adrenaline or noradrenaline are receptor ligands to either 1.

override the vasodilation mediated by -adrenoreceptors. producing an overall vasodilation. IP3 and cal action  cium up   (TCA:s) Amitriptyli ne  Clomipra mine   Doxepin Trimipram ine 2: A. adrenoreceptor stimulation dominates.c AMP down (Alpha-2 agonists)  Dexmedetomi (Alpha-2 blockers)  Phentolam . At lower levels of circulating epinephrine. B. D‚ Norepinephrine >epinephrine >> isoprenaline Gq: phospholipase Smooth  C (PLC) muscle contr activated. B. C Epinephrine •norepinephrine >>isoprenaline Smooth muscle cons triction and neurotransm itter inhibition Gi: adenylate cyclase inactivated. [edit]Comparison Rece ptor Agonist potency order Selected action of agonist Mechanism Agonists Antagonists (Alpha-1 blockers)    Alfuzosin Doxazosin Phenoxybe nzamine  (Alpha-1 agonists)  Noradrenaline Phenylephrine Methoxamine Cirazoline Xylometazoli ne     Phentolam ine Prazosin Tamsulosi n Terazosin 1: A. The result is that high levels of circulating epinephrine cause vasoconstriction.

dine  Medetomidin e             Romifidine Clonidine Brimonidine Detomidine Lofexidine Xylazine Tizanidine Guanfacine Amitraz    ine Yohimbine Idazoxan Atipamezo le (Beta blockers) 1 Heart Gs: adenylate Isoprenaline > epinephrine =n muscle contr cyclase activated.cA muscle relax MP up (also Gi.cA orepinephrine action MP up Noradrenaline Isoprenaline Dobutamine   Metoprolol Atenolol (Short/long)  Salbutamol(A lbuterol in USA)  Gs: adenylate Smooth cyclase activated. ation see 2) Bitolterol mesylate     Formoterol Isoprenaline Levalbuterol Metaproteren ol    Isoprenaline =norepinephrine > epinephrine Enhance lip olysis Gs: adenylate cyclase activated.cA MP up   Salmeterol Terbutaline Ritodrine L-796568 [2] Amibegron  SR 59230A   Butoxamin e Propranolo l (Beta blockers) 2 Isoprenaline > epinephrine>> norepinephrine 3 .

there was a subtype known as C. Upon activation. The former interacts with calcium channels of endoplasmic and sarcoplasmic reticulum thus changing the calcium content in a cell. Solabegron There is no 1C receptor. but was found to be identical to one of the previously discovered subtypes. Common (or still unspecified) effects include: Vasoconstriction of arteries to heart (coronary artery). [edit] receptors receptors have several functions in common. Gq. kidney (renal artery)[6] and brain[7]. Specific actions of the 1 receptor mainly involve smooth muscle contraction. but also individual effects. activates phospholipase C (PLC). gastrointestinal system. This triggers all other effects. The PLC cleaves phosphatidylinositol 4. naming was continued with the letter D. It causes vasoconstriction in many blood vessels including those of the skin. At one time.5-bisphosphate (PIP2) which in turn causes an increase in inositol triphosphate (IP3) and diacylglycerol (DAG). Other areas of smooth muscle contraction are:    ureter vas deferens hair (arrector pili muscles) .[3] [4]  Vasoconstriction of veins [5]  Decrease motility of smooth muscle in gastrointestinal tract [edit] 1 receptor Main article: Alpha-1 adrenergic receptor  ‚ Alpha1-adrenergic receptors are members of the G proteincoupled receptor superfamily. a heterotrimeric G protein. To avoid confusion.

Specific actions of the  2 receptor include: inhibition of insulin release in pancreas.  Increase Renin secretion from juxtaglomerular cell of kidney. as well as secretion from sweat glands[8] and Na+ reabsorption from kidney.[8]  Antagonists may be used in hypertension. and 2C. by raising heart rate (positive chronotropic effect) and increasing impulse conduction and increasing contraction thus increasing the volume expelled with each beat (increased ejection fraction). [edit] 2 receptor Main article: Alpha-2 adrenergic receptor There are 3 highly homologous subtypes of 2 receptors: 2A.[8]  induction of glucagon release from pancreas. 2 .  contraction of sphincters of the gastrointestinal tract  negative feedback in the neuronal synapses [edit] receptors [edit] 1 receptor Main article: Beta-1 adrenergic receptor Specific actions of the  1 receptor include: Increase cardiac output. [9]  increase ghrelin secretion from the stomach [edit] 2 receptor .uterus (when pregnant)  urethral sphincter  bronchioles (although minor to the relaxing effect of 2 receptor on bronchioles)  blood vessels of ciliary body (stimulation causes mydriasis) Further effects include glycogenolysis and gluconeogenesis from adipose tissue[8] and liver.

Beta-3 activating drugs could theoretically be used as weight-loss agents. .g.Main article: Beta-2 adrenergic receptor Specific actions of the  2 receptor include the following: Smooth muscle relaxation. in bronchi.[8] [10]  Lipolysis in adipose tissue. e. but are limited by the side effect of tremors. [11][12]  Anabolism in skeletal muscle.  Inhibit histamine-release from mast cells  Increase renin secretion from kidney [edit] 3 receptor Main article: Beta-3 adrenergic receptor Specific actions of the  3 receptor include: Enhancement of lipolysis in adipose tissue.  Relax non-pregnant uterus  Relax detrusor urinae muscle of bladder wall  Dilate arteries to skeletal muscle  Glycogenolysis and gluconeogenesis  Contract sphincters of GI tract [8]  Thickened secretions from salivary glands.

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