AE9C90CB, muscarinic receptor antagonist, has greater affinity for M3 muscarinic receptors with pKi of 9.90 and was 20-fold more selective for M3 than for M2 muscarinic receptors.

5-Hydroxymethyl tolterodine (formate) (PNU-200577 (formic)) is an active metabolite of the muscarinic acetylcholine receptor antagonists Tolterodine and Fesoterodine. 5-Hydroxymethyl tolterodine (formate) is formed from tolterodine by the cytochrome P450 (CYP) isoform CYP2D6 and from fesoterodine by plasma esterases.

(S)-Oxybutynin (Esoxybutynin) hydrochloride is a potent muscarinic receptor antagonist.

Zafirlukast metabolite M1 (compound 15) is an inhibitor of allergic lung diseases such as asthma and can antagonize the activity of leukotrienes.

T-10430 is a potent and orally active leukotriene B4 receptor 2 (BLT2) agonist. T-10430 has the potential for the research of psoriasis.

Ricinelaidic acid, a 12-hydroxy fatty acid，is a leukotriene B4 (LTB4) receptor antagonist with the Ki of 2 μM in porcine neutrophil membranes. Ricinelaidic acid inhibits chemotaxis and calcium flux induced by LTB4 in isolated human neutrophils (IC50=10 and 7 μM, respectively). Ricinelaidic acid inhibits bronchoconstriction induced by LTB4 in rats.

14,15-Dehydro Leukotriene B4 (Compound 4) is a LTB4 receptor antagonist. 14,15-Dehydro Leukotriene B4 also has a higher binding affinity for BLT1 with a Ki value of 27 nM and BLT2 with a Ki value of 473 nM. 14,15-Dehydro Leukotriene B4 inhibits LTB4-induced release of lysozymes from rat polymorphonuclear leukoctyes with an IC50 value of 1 µM.

Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).

Promethazine sulfoxide is a metabolite of the histamine H1 receptor antagonist Promethazine. It is formed from promethazine by the cytochrome P450 (CYP) isoform CYP2D6.

Gizzerosine is an H2 receptor agonist. It can stimulate the gastric acid secretion of broiler chickens, thus causing gizzard erosion in them. Gizzerosine has significant research value in the fields of agricultural farming and feed science.

BL 6341A is an antagonist for histamine H2 receptor with Ki of 3.5-4.4 nM, that inhibits histamine-induced acid secretion and cAMP formation. BL 6341A can be used in research of gastric acid secretion related diseases, such as gastric ulcer or gastroesophageal reflux.

Arpromidine (BU-E-50) is the agonist for histamine H2 receptor and the antagonist for histamine H1 receptor. Arpromidine exhibits positive inotropic effect with less risks in causing arrhythmias. Arpromidine can be used in research of congestive heart failure.

ADS1017 is the antagonist for histamine receptor and muscarinic receptor, that exhibits good affinities to hH3R, hH4R, hM2R and hM4R with pKi of 6.8, 5.5, 7.4 and 7.2. ADS1017 exhibits analgesic and anti-allodynic efficacy in mice Capsaicin-or Oxaliplatin-induced pain models.

(S)-Cetirizine dihydrochloride ((S)-P071) is an orally active antagonist of the histamine H1 receptor with a Ki value of 39.1 nM. (S)-Cetirizine dihydrochloride exerts anti-allergic activity by binding to the histamine H1 receptor and blocking the action of histamine. (S)-Cetirizine dihydrochloride is promising for research of allergic diseases such as allergic rhinitis.

(-)-Brompheniramine is a H1 receptor antagonist with antiallergic activity.

TUG-2181 is an antagonist of GPR84 with an IC50 value of 34 nM. TUG-2181 inhibits GPR84 agonists-induced reactive species oxygen (ROS) production and IL-8 release in human neutrophils. TUG-2181 can be used for inflammation and fibrosis study.

Pyrone-211 is a potent GPR84 agonist and AKR1C3 inhibitor. Pyrone-211 participates in an expanded polyamine pathway.

Sulfatroxazole (Isosulfafurazole) (compound 12) is a selective antagonist of ETA receptor (IC50=0.26 μM).

K-8794 is an orally active selective endothelin receptor ETB antagonist that can be used in research on cardiovascular diseases.

Domperidone monomaleate (R33812 monomaleate) is a potent antagonist of dopamine D2 receptor that acts as an antiemetic and prokinetic agent by targeting the chemoreceptor trigger zone and motor function of the stomach and small intestine. It also inhibits cardiac Na⁺ channels such as Nav1.5, suggesting a potential molecular mechanism for cardiovascular side effects like malignant arrhythmias.

Trepipam (Trimopam; SCH-12679) is a D1-dopamine receptor antagonist. Trepipam can reduce the self-injurious behavior in 6-OHDA-lesioned rats. Trepipam can be used in the research of epilepsy and anxiety neurosis.

Thiopropamine hydrochloride is a thiol compound that can be used in research on duodenal ulcers.

Sibenadet (AR-C68397AA free base) is a dual dopamine D2/β2-adrenoceptor agonist with selective β2-adrenoceptor agonism. Sibenadet inhibits capsaicin-induced plasma protein extravasation in rat trachea. Sibenadet suppresses edema from sensory nerve fiber activation by activating β2-adrenoceptor. Sibenadet is promising for research of chronic obstructive pulmonary disease (COPD).

SCH-23390 is a dopamine D1-like receptor antagonist (with Ki values of 0.2 nM and 0.3 nM for the D1 and D5 receptor subtypes, respectively). SCH-23390 can shorten the latency period for cocaine-induced lever pressing behavior in rats. SCH-23390 can also eliminate generalized seizures caused by chemical convulsants, such as arecoline and strychnine, and is used in research on neurological disorders related to the dopamine system.

RG-15 is the orally active antagonist for dopamine receptor that exhibits goof affinity to human D2 receptor and human D3 receptor with pKi of 8.23 and 10.49. RG-15 inhibits dopamine-stimulated [35S]GTPγS binding with IC50 of 21.2 nM (rat striatal membranes), 36.7 nM (mouse A9 cells expressing human D2L receptors) and 7.2 nM (CHO cells expressing human D3 receptors). RG-15 increases the turnover and biosynthesis of dopamine in mouse striatum and olfactory bulb, exhibiting antipsychotic activity.

PF 219061 is an selective agonist for dopamine 3 receptor with an EC50 of 15 nM. PF 219061 exhibits a rapid absorption and a good liver blood clearance, and can be used for research of female sexual dysfunction.

PD 118717 is a selective dopamine (DA) D-2 autoreceptor agonist. PD 118717 has significant affinity for 5-HT1A but not 5-HT1B and 5-HT2 receptors. PD 118717 is active in antagonizing the tau-Butyrolactone-induced accumulation of dopa in rat striatum and mesolimbic regions. PD 118717 exhibits an antipsychotic-like profile.

Nolomirole (CHF 1035) is an orally active and selective DA2 dopaminergic receptor/α2-adrenoceptor agonist. Nolomirole attenuates the heart failure signs in the Monocrotaline-induced congestive heart failure model. Nolomirole increases cardiac output.

N-Methylspiroperidol is a D2 receptor antagonist. N-Methylspiroperidol can be labeled as [18F]N-Methylspiroperidol and used in PET (Positron Emission Tomography) to study how it binds to the 5-HT2C receptor and the competition and effects of neurotransmitters like dopamine on these receptors.

Nitracaine is a structural analog of Dimethocaine in the colon, offering various anti-inflammatory effects in areas of colitis, and it also exerts related anticancer effects by regulating the IL-6/STAT3 pathway.