Alpha receptors can be classified as a subtype of adrenergic receptor, their activation triggers a complex range of autonomic responses that

will be detailed in the following article. We recommend our readers to check our article on beta receptors for further information on autonomic pharmacology.

Article contents:

Alpha 1 receptors Alpha 2 receptors Drugs affecting alpha receptors

Alpha 1 receptors

The image below shows the synaptic cleft, presynaptic and postsynaptic membranes. Alpha 1 receptors are located on the postsynaptic membrane of effector organs.

Activation of alpha 1 receptors increases vascular smooth muscle contraction, producing increases in blood presure. These receptors also influence activity of genitourinary smooth muscle.

Effects of alpha 1 receptor activation on different tissues and systems:

Vascular smooth muscle. Activation of vascular smooth muscle receptors causes vasoconstriction, leading to an increase in peripheral resistance and in blood pressure. Alpha 1 antagonists are used in the treatment of hypertension because of their properties as peripheral vasodilators.

Mydriasis. Mydriasis is mediated by both alpha 1 and 2 activation.

Genitourinary tract smooth muscle. Alpha 1A receptors are located at the external sphincter of the bladder. Blockade of alpha 1A receptors decreases tone in the smooth muscle of the bladder neck and prostate, thus improving urinary flow. Tamsulosine is used for the treatment of benign prostatic hyperplasia because of its ability to selectively block alpha 1A receptors.

Alpha 2 receptors

Although alpha 2 receptors are found on both presynaptic neurons and postynaptic cells, they work mainly as autoreceptors to mediate feedback inhibition of sympathetic transmission.

In addition to neurons, alpha 2 receptors are located in other regions, like pancreatic beta cells and platelets. The diagram below shows how when activated, these receptors act as inhibitory autoreceptors (they inhibit norepinephine release from adrenergic neurons) and as inhibitory heteroreceptors (they inhibit acetylcholine release from cholinergic neurons). In addition, activation of alpha 2 receptors on pancreatic beta cells membranes inhibits insulin release.