BOMA (Compound 7) is a potent and selective metabotropic glutamate receptor 5 (mGluR 5) antagonist with an IC50 value of 3 nM and an Ki value of 3 nM. BOMA is promising for research of various pain states, including acute, persistent and chronic pain, inflammatory pain and neuropathic pain.

AZD-2066 hydrochloride is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 hydrochloride activates the BDNF/trkB signaling pathway. AZD 2066 hydrochloride can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease.

A-850002 is a metabotropic glutamate receptor (mGluR) antagonist (IC50=27 nM) that significantly attenuates spontaneous pain behavior after skin incision in rats. A-850002 can be used for analgesia research.

1-Benzyl-APDC acts as an agonist for mGluR6, with an EC50 of 20 μM in CHO cells. 1-Benzyl-APDC is a weak antagonist of mGluR2, with an IC50 of 200 μM.

Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate composed of Melatonin and Tamoxifen, which is a potent antagonist of ERα (IC50=863 nM). Melatonin-Tamoxifen Conjugate binds to MLT receptor (Ki=3.1 nM) and promotes β-arrestin (EC50=914 nM) and ERK activation (EC50=98 nM) in cells expressing hMT1 receptor. Melatonin-Tamoxifen Conjugate against several common cell lines MCF-7, MDA-MB-231, and HT-1080 with IC50s of 6.8 μM, 6.4 μM, and 1.7 μM, respectively.

DH97 is a potent melatonin receptor 2 (MT2) antagonist with Ki values of 252 nM and 1100 nM for MT2 and MT1, respectively.

(R)-Ramelteon ((R)-TAK-375) is an orally active inactive isomer of the melatonin receptor 1 and 2. (R)-Ramelteon is promising for research of regulating sleep.

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.