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Table 2 Molecules presented here that target adenosine receptors. None are approved for treatment

From: Involvement of adenosine signaling pathway in migraine pathophysiology: a systematic review of preclinical studies

Name

Target

Clinical use

Adenosine receptor agonists

GR79236

Highly potent and selective adenosine A1 receptor agonist [12]

Ischemic heart disease [3, 25], sleep apnea [5], modulation of lipolysis and insulin sensitivity [18]

GR79236X

Selective adenosine A1 receptor agonist [6]

Ischemic heart disease [44] and dental pain [41]

GR190178

Low efficacy (partial) adenosine A1 receptor agonist [13]

Cluster headache [13]

CGS21680

Selective adenosine A2A receptor agonist [6]

Huntington’s disease [7], spinal cord injury [36], bone regeneration [33] and overactive bladder [47]

2-CI-IB-MECA

Selective adenosine A3 receptor agonist [6]

Atrial function [49], damage of the optic nerve and white matter ischemic damage [14]

Adenosine receptor antagonists

Caffeine

Non-selective adenosine A1 and A2A antagonist [34]

Treatment of headache, pain, apnea in premature children and neurodegenerative diseases [10]

DPCPX

Selective adenosine A1 receptor antagonist [6, 13]

Depression [42], cancer [8, 30, 50] and neuroprotection [37]

SCH58261

Potent and highly selective A2A receptor antagonist [15]

Spinal cord injury [36], epilepsy [29] and preeclampsia [40]

JNJ-41942914, JNJ-39928122, JNJ-40529749, JNJ-40064440, and JNJ-41501798

A2A receptor antagonists [16]

None