Adenosine receptor (central nervous system subtypes) (AR (sometimes further specified as A1R, A2AR, A2BR, A3R))

Adenosine receptors in the central nervous system are a family of G protein-coupled receptors (subtypes A1, A2A, A2B, and A3) that respond to the endogenous ligand adenosine. These receptors have diverse and often opposing roles in modulating neuronal excitability, synaptic transmission, neurotransmitter release, neuroprotection, and neuroinflammation. A1 and A2A are the most abundant and functionally significant CNS subtypes; A1 receptors generally mediate inhibitory and neuroprotective effects, while A2A receptors facilitate excitatory transmission and are implicated in neurodegenerative and psychiatric diseases. CNS adenosine receptor pharmacology underlies the effects of widely used stimulants such as caffeine, as well as newer drugs developed for neurological and psychiatric disorders

Other names

P1 receptor (collective)adenosine receptor familyCNS adenosine receptorsARs

Agonist or antagonist modulation of G protein-coupled adenosine receptors; Inhibitory modulation of excitatory neurotransmission (A1); Excitatory facilitation (A2A); Inhibition of adenylate cyclase (A1, A3); Stimulation of adenylate cyclase (A2A, A2B); Antagonism by xanthines provides CNS stimulation