α-MSH(11-13) (ACTH-(11-13)) is the 11-13 amino acid (lysine-proline-valine) sequence of α-MSH, which reduces fever in rabbits.

Setmelanotide (monoacetate) is a melanocortin 4 receptor (MC4R) agonist that acts on human and rat MC4R with EC50 values of 0.27 nM and 0.28 nM, respectively.

RO27-3225 trifluoroacetate is a peptide agonist of melanocortin receptor 4 (MC4R) with neuroprotective and anti-inflammatory activity with an EC50 value of 1 nM, while 8 nM for MC1R. RO27-3225 trifluoroacetate reverses hemorrhagic shock, reduces brain edema, blood-brain barrier (BBB) permeability, and hippocampal IL-1β and TNF-α levels in a rat model of intra-abdominal hypertension induced by hemorrhagic shock and resuscitation.

Delmadinone acetate is an orally active compound that can control estrus and ovulation in female and male pets. Delmadinone acetate causes adrenal suppression from inhibition of release of ACTH from the pituitary gland.

ATMW-2 is a NeuralGenThesis (NGT)-derived antagonist targeting the melanocortin type 2 receptor (MC2R).

VU0467319 (Compound VU319) is a highly selective and blood-brain-permeable, orally active M1 positive allosteric modulator (PAM) (EC50: 492 nM). VU0467319 is selective (EC50 > 30 μM) versus M2-5 for both human and rat. VU0467319 improves cognitive impairment in Alzheimer's disease (AD) through central M1 muscarinic receptors. VU0467319 does not induce cholinergic adverse reactions and has potential in AD research.

Solifenacin N-oxide (Solifenacin N1-oxide) is an inactive metabolite of the muscarinic receptor antagonist Solifenacin.

SCH 211803 is a selective antagonist of the M2 muscarinic receptor. SCH 211803 is promising for research of cardiovascular and nervous system diseases.

p-F-HHSiD (p-Fluorohexahydrosiladifenidol) hydrochloride is a selective M3 mAChR antagonist. p-F-HHSiD hydrochloride blocks Acetylcholine-mediated vasodilatation in human umbilical vein endothelial cells (HUVECs).

Oxotremorine is an agonist for mAChR, that activates M1 and M3 acetylcholine receptors. Oxotremorine exhibits nicotine-like effects in drug discrimination experiments in macaques.

Lu 25-077 is a brain-penetrant and pharmacologically active N-demethyl metabolite of Lu 25-109, a DNA topoisomerase I (topoisomerase I) inhibitor.

KTX-005 is the agonist for mAChR that regulates the signaling pathway of the neurotransmitter acetylcholine, and can be used for research of schizophrenia.

Imidafenacin Metabolite M4 is a metabolite of the muscarinic acetylcholine receptor antagonist Imidafenacin.

Desiodomethyl 4-DAMP is a muscarinic receptor antagonist.

Caramiphen hydrochloride is a muscarinic antagonist. Caramiphen hydrochloride shows anticonvulsive properties. Caramiphen hydrochloride offers partial protection against Soman-induced seizures and neuropathology.

Betovumeline is the agonist for muscarinic receptor and can be used for researchs of neurological disorders.

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.