MIPS-521 is a novel and potent positive allosteric modulator of the A1R. Rererences: Positive allosteric mechanisms of adenosine A1 receptor-mediated analgesia

Metipranolol is a potent non-selective beta blocker (β adrenergic receptor antagonist) used in eye drops to treat glaucoma.

Ciforadenant (formerly known as CPI-444; V-81444) is a potent, selective and orally bioactive small molecule inhibitor of the adenosine-A2a receptor (A2AR) on T-lymphocytes with anticancer and immunomodulatory activities and the potential to be used in cancer immunotherapy.

NBMPR( NBTI) is a nucleoside analog that competitively inhibits the equilibrative nucleoside transporter 1 (Kd = 0.1-1.0 nM, IC50s = 4.6 and 3.6 nM in rat and human, respectively).

Norepinephrine bitartrate monohydrate (Levarterenol; L-Noradrenaline) is a potent and β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.

Todralazine hydrochloride is a novel and potent antihypertensive agent.

Proxyphylline is a derivative of methylxanthine that is clinically used as a cardiac stimulant, a vasodilator and a bronchodilator.

A2A receptor antagonist 1 is a novel and potent antagonist of the adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.

Acefylline (also known as Theophylline-7-acetic acid and Theophyllineacetic acid), is an antagonist of the adenosine receptor and an activator of the peptidylarginine deiminase (PAD).

Sulmazole (Vardax; AR-L 115BS; AR-L 115-BS) is an A1 adenosine receptor antagonist that inhibits the function of guanine nucleotide regulatory proteins by affecting GTP turnover.