AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively). AF-DX 384 reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine.

AZ-GHS-22 is a potent, non-CNS penetrant GHS-R1a inverse agonist (IC50=0.77 nM).

RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites.

PG01037 (dihydrochloride) is a potent and selective dopamine D3 receptor antagonist with a Ki of 0.7 nM.

Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma.

Ifetroban is a long-acting thromboxane A2 receptor antagonist, with antiplatelet activity.

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

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

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.

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

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

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.

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

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.

Prifinium bromide is antimuscarinic agent with antispasmodic, antiemetic effect.

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

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

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.

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.

Neldazosin is a potent alpha1-adrenoceptor antagonist.

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.

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

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

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.

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

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

UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT5AR with a more restricted off-target profile and decreased assay liabilities. UCSF678 is a selective probe with which to study the function of the 5-HT5AR.

(R)-Preclamol is a dopamine (DA) agonist with autoreceptor as well as postsynaptic receptor stimulatory properties. (R)-Preclamol inhibits the locomotor activity of mice and rats in low doses.

UCSF686 is a probe with which to study the function of the 5-HT5AR. UCSF686 loses affinity at 5-HT5AR (>10 000 nM) but not at 5-HT1AR, 5-HT2BR, and 5-HT7R. UCSF686 controls for off-target effects.

Octamylamine is an anticholinergic and antispasmodic agent.