Alvimopan (also known as ADL 8-2698; LY 246736; HSDB-7704) is a novel peripheral micro opioid antagonist in clinical development for the management of post-operative ileus and opioid-induced bowel dysfunction.

Porcine dynorphin A(1-13) is a novel and potent κ opioid receptor agonist, antinociceptive agent

Racecadotril (also called acetorphan) is a potent and peripherally acting enkephalinase inhibitor used as an antidiarrheal medication.

LY2795050 is a novel, potent and selective κ-opioid Receptor (KOR) antagonist with an IC50 of 0.72 nM.

BAN ORL 24 is a novel, potent and selective NOP (nociceptin/orphanin FQ (N/OFQ) peptide receptor) receptor antagonist with IC50 values of 0.27, 2500, 6700 and > 10000 nM for NOP, κ-, μ- and δ-receptors respectively.

Aticaprant (formerly also known as JNJ-67953964; LY-2456302; CERC501) is a novel, potent, oral, selective, CNS-penetrant and short-acting antagonist of the kappa / κ-opioid receptor (KOR) with a Ki of 0.807 nM (versus 24.0 nM and 155 nM for the μ-opioid receptor (MOR) and δ-opioid receptor (DOR).

Lomerizine HCl (KB-2796; Migsis; KB2796; KB 2796), the dihydrochloride salt of Lomerizine, is a diphenylpiperazine-based, relatively new and potent L- and T-type CCB/calcium channel blocker used for the treatment of migraine.

JTC-801 HCl (JTC 801; JTC801), the hydrochloride salt of JTC801, is a potent, orally bioactive and selective opioid receptor-like1 (ORL1) receptor antagonist with potential analgesic activity.

SR17018 is an agonist of the μ-opioid-receptor (MOR) which binds to GTPγS with EC50 value of 97 nM.

DAMGO TFA is a novel, potent and selective μ-opioid receptor agonist with a Kd of 3.46 nM for native μ-OPR.