Family

Beta 1 adrenoceptor (IPR000507)

Short name: ADRB1_rcpt

Family relationships

Description

The adrenoceptors (or adrenergic receptors) are rhodopsin-like G protein-coupled receptors that are targets of the catecholamines, especially norepinephrine (noradrenaline) and epinephrine (adrenaline). Many cells possess these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system, effect blood pressure, myocardial contractile rate and force, airway reactivity, and a variety of metabolic and central nervous system functions. The clinical uses of adrenergic compounds are vast. Agonists and antagonists interacting with adrenoceptors have proved useful in the treatment of a variety of diseases, including hypertension, angina pectoris, congestive heart failure, asthma, depression, benign prostatic hypertrophy, and glaucoma. These drugs are also useful in several other therapeutic situations including shock, premature labour and opioid withdrawal, and as adjuncts to general anaesthetics.

There are three classes of adrenoceptors, based on their sequence similarity, receptor pharmacology and signalling mechanisms [PMID: 18882199]. These three classes are alpha 1 (a Gq coupled receptor), alpha 2 (a Gi coupled receptor) and beta (a Gs coupled receptor), and each can be further divided into subtypes [PMID: 2855960]. The different subtypes can coexist in some tissues, but one subtype normally predominates.

There are three subtypes of beta adrenoceptors (beta 1-3), the division is mainly based on their affinities to adrenergic agonists and antagonists. All three subtypes act in the main by activating a Gs protein [PMID: 11053129], activating adenylate cyclase activity. The beta 2 subtype also couples to Gi/o protein [PMID: 11053129, PMID: 12063255]. Beta adrenoceptor selective agonists (beta blockers) are used in the treatment of asthma, angina, cardiac conditions and have proven useful in the treatment of migraine, anxiety disorders and hyperthyroidism, and, when applied topically, are useful in the treatment of glaucoma [PMID: 15655528].

This entry represents the beta 1 adrenoceptors, which are located mainly in cardiac tissue [PMID: 1695899], where they increase cardiac output by altering the heart rate and force of contraction [PMID: 8693001] and in kidney, where they enhance renin [PMID: 6107894]. Beta 1 adrenoceptors are also found in the liver, lung and brain [PMID: 8917438] and the sphincter part of the gastrointestinal tract [PMID: 14711933]. They also causes amylase secretion from the salivary glands [PMID: 25100]. Presynaptically, their activation causes an increase in noradrenaline release.

GO terms

Biological Process

GO:0007189 adenylate cyclase-activating G-protein coupled receptor signaling pathway
GO:0045823 positive regulation of heart contraction

Molecular Function

GO:0004940 beta1-adrenergic receptor activity

Cellular Component

GO:0016021 integral component of membrane

Contributing signatures

Signatures from InterPro member databases are used to construct an entry.
PRINTS