5-HT2A receptor agonist-1 shows the agonist activity at the 5-HT2A receptor with an EC50 of 5.54 nM.

Tegaserod is a serotonin receptor 4 agonist (HTR4) used in the treatment of irritable bowel syndrome (IBS). Anti-tumor activity.

CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3+ T lymphocytes into the Pan02 tumor tissues.

Ro 01-6128 is a positive allosteric modulator of mGluR1.

Dioxopromethazine is an orally active antihistamine. Dioxopromethazine inhibits asthmatic symptoms.

Ridogrel (R 68070) is an orally active combined thromboxane A2 synthetase inhibitor and thromboxane A2/prostaglandin endoperoxide receptor blocker. Ridogrel is potent antiplatelet agent. Anti-inflammatory activities.

Neldazosin is a potent alpha1-adrenoceptor antagonist.

Lu AA33810 is a potent and selective antagonist of neuropeptide Y5 receptor with a Ki of 1.5 nM for the human receptor. Lu AA33810 exhibts antianxiolytic-like and antidepressant-like effects.

LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT2A receptor with a pA2 of 8.32 in a rat tail artery assay.

SB-328437 is a potent, selective non-peptide CCR3 antagonist with an IC50 of 4.5 nM.

GPBAR1-IN-3 (Compound 14) is a selective GPBAR1 agonist (EC50=0.17 μM) and a CysLT1R antagonist.

Sequifenadine is a H1-antihistamine. Sequifenadine has the potential for the research of inflammatory eye disease with allergic symptoms.

Prifinium bromide is antimuscarinic agent with antispasmodic, antiemetic effect.

S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism.

CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice.

(S)-Butaprost (free acid) is a potent and highly selective agonist of EP2 receptor.

Noladin ether is a potent and selective agonist of cannabinoid CB1 receptor, with a Ki of 21.2 nM. Noladin ether can cause hypothermia, intestinal immobility, and mild antinociception.

Benzomalvin B is the less active analogs of Benzomalvin A. Benzomalvin B is weakly active against substance P.

TP-16 is a novel and selective EP4 antagonist with an IC50 of 2.1 nM.

EP2 receptor antagonist-1 (compound 1) is a potent, reversible, and agonist dependent allosteric prostaglandin EP2 receptor antagonist. EP2 receptor antagonist-1 shows anti-inflammatory effects.

ONO-8713 is a selective prostaglandin E receptor subtype EP1 antagonist.

TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities.