VU6024945 is an orally active negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGlu5 NAM) with an IC50 value of 110 nM. VU6024945 can be used in the research of anti-anxiety, anti-depression and Parkinson's disease and other neurological diseases.

VU6024578 (BI02982816) is a selective, orally active positive allosteric modulator (PAM) for metabotropic glutamate receptor (mGluR1), that activates human mGluR1 and rat mGluR1 with EC50 of 54 nM and 46 nM. VU6024578 exhibits antipsychotic activity in rats amphetamine-induced hyperactivity models and MK-801, and has anti-tumor activity.

UBP 1112 is a selective group III mGluR antagonist, with a Kd of 5.1 μM.UBP 1112 shows 96-fold affinity for group III over group II mGlu receptor (Kd, 488 μM), and shows no significant activity at group I mGlu receptor or iGlu receptor.

Troriluzole hydrochloride is a third-generation peptide precursor of Riluzole and is an orally active glutamate modulator. Troriluzole hydrochloride can reduce synaptic glutamate levels and enhance the uptake of synaptic glutamate. Troriluzole hydrochloride shows potential for treating Alzheimer's disease and Generalized Anxiety Disorder (GAD).

Oxomemazine hydrochloride is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine hydrochloride is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki= 84 nM, M1 receptor) and low (Ki= 1.65 μM, M2 receptor) affinity sites[1]. Oxomemazine hydrochloride an antihistamine and anticholinergic agent used for the study of cough treatment.

GSK1331268 is a selective, orally active agonist for mGluR2 with a pEC50 of 6.9. GSK1331268 exhibits good blood-brain barrier penetration. GSK1331268 regulates glutamate signaling, and can be used in research of neurodegenerative and neuropsychiatric diseases.

FO-4-15 is an mGluR1/CaMKIIα activator. FO-4-15 has a protective effect against H2O2 in human neuroblastoma (SH-SY5Y) cells. FO-4-15 can improve cognitive impairment in Alzheimer’s disease mice by activating the mGluR1/CaMKIIα pathway, and can reduce Aβ accumulation, hyperphosphorylated Tau, and synaptic damage.

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.