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The dopamine receptors are members of the G protein-coupled receptors superfamily with seven transmembrane domains. Dopamine receptors have five subtypes, D 1 through D 5, the subtypes can be divided into two subclasses due to their mechanism of action on adenylate cyclase enzyme, D 1-like receptors (D 1 and D 5) and D 2-like receptors (D 2, D ...
A dopamine molecule consists of a catechol structure (a benzene ring with two hydroxyl side groups) with one amine group attached via an ethyl chain. [14] As such, dopamine is the simplest possible catecholamine, a family that also includes the neurotransmitters norepinephrine and epinephrine. [15]
The mechanisms of sympathomimetic drugs can be direct-acting (direct interaction between drug and receptor), such as α-adrenergic agonists, β-adrenergic agonists, and dopaminergic agonists; or indirect-acting (interaction not between drug and receptor), such as MAOIs, COMT inhibitors, release stimulants, and reuptake inhibitors that increase the levels of endogenous catecholamines.
The existence of multiple types of receptors for dopamine was first proposed in 1976. [3] [4] There are at least five subtypes of dopamine receptors, D 1, D 2, D 3, D 4, and D 5. The D 1 and D 5 receptors are members of the D 1-like family of dopamine receptors, whereas the D 2, D 3 and D 4 receptors are members of the D 2-like family.
Interactions between catechol-based agonists and three trans-membrane serine residues including S1985.42, S1995.43, and S2025.46 function as microswitches that are essential for receptor activation. [43] Dopamine D1 CryoEM structure in complex with dopamine (PDB code: 7LJD), Dopamine D1 receptor in orange, dopamine in cyan, interactions are in ...
Apomorphine's R-enantiomer is an agonist of both D 1 and D 2 dopamine receptors, with higher activity at D 2. [ 7 ] [ 12 ] The members of the D 2 subfamily, consisting of D 2 , D 3 , and D 4 receptors, are inhibitory G protein–coupled receptors .
It is a dopamine agonist and works by triggering dopamine D 2 receptors. [4] It was approved for medical use in the United States in 1997. [4] It is available as a generic medication. [3] In 2022, it was the 163rd most commonly prescribed medication in the United States, with more than 3 million prescriptions. [6] [7]
Dopamine receptor flow chart. Dopamine receptors are all G protein–coupled receptors, and are divided into two classes based on which G-protein they are coupled to. [1] The D 1-like class of dopamine receptors is coupled to Gα s/olf and stimulates adenylate cyclase production, whereas the D 2-like class is coupled to Gα i/o and thus inhibits adenylate cyclase production.