TC-G 1004 (compound 16j) is an orally active A2A adenosine receptor antagonist, with Ki values of 0.44 nM and 80 nM for hA2A and hA1, respectively[1].
AA41612 is a potent antagonist of melanopsin-mediated phototransduction[1].
(p-Iodo-Phe7)-ACTH (4-10) is a adrenocorticotrophic hormone (ACTH) derivative, which is produced and secreted by the anterior pituitary gland. (p-Iodo-Phe7)-ACTH (4-10) serves as a melanocortin (MC) receptor antagonist and inhibits α-melanocyte-stimulating hormone (α-MSH)-induced excessive grooming behavior in rats[1].
Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a.
CE-224535 is a selective P2X7 receptor antagonist.
Thiothixene hydrochloride is an antipsychotic agent. Thiothixene hydrochloride can be used for borderline and schizotypal disorder research[1].
WAY-267464 is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder[1].
(R)-5-Hydroxymethyl Tolterodine(PNU-200577; Desfesoterodine) is a potent and selective muscarinic receptor antagonist with a Kb and a pA2 of 0.84 nM and 9.14, respectively. IC50 value: 0.84 nM (Kb)Target: mAChR(R)-5-Hydroxymethyl Tolterodine is a major pharmacologically active metabolite of tolterodine. In vitro, (R)-5-Hydroxymethyl Tolterodine prevented carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner. In vivo, (R)-5-Hydroxymethyl Tolterodine was significantly more potent at suppressing acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50=15 and 40 nmol/kg, respectively). In radioligand binding studies carried out in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors, (R)-5-Hydroxymethyl Tolterodine was not selective for any muscarinic receptor subtype. Thus, (R)-5-Hydroxymethyl Tolterodine is similar to tolterodine in terms of antimuscarinic potency, functional selectivity for the urinary bladder in vivo and absence of selectivity for muscarinic receptor subtypes in vitro. The results of this study clearly indicate that (R)-5-Hydroxymethyl Tolterodine contributes to the therapeutic action of tolterodine, in view of its high antimuscarinic potency, similar serum concentration and lower degree of protein binding.
D-AP4 (D-APB; D-2-Amino-4-phosphonobutyric acid), a phosphono analogue of glutamate, is an NMDA broad spectrum excitatory amino acid receptor antagonist. D-AP4 also is an agonist for a quisqualate-sensitized AP6 site in hippocampus. D-AP4 inhibits AMPA receptor-stimulated 57Co2+ influx in cultured cerebellar granule cells (IC50 ≥ 100 μM)[1][2][3].
[His7] Corazonin, a neurohormone, induces dark color in the cuticle and epidermis of Locusta migratoria[1].
1'-Hydroxymidazolam is a primary active metabolite of Midazolam, and it is a neuronal depressant agent. 1'-Hydroxymidazolam could inhibit neuronal activity add to the effects of Midazolam[1][2].
AT-121 hydrochloride is a bifunctional nociception and mu opioid receptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 hydrochloride is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects[1].
Revusiran (ALN-TTRSC) is a 1st-generation short interfering RNA, which directed against transthyretin (TTR) mRNA. Revusiran can be used for transthyretin (TTR)-mediated amyloidosis research[1].
Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM.Target: nAChRCatharanthine evokes a concentration-dependent attenuation of carbachol responses in the rat ileum preparation, producing rightward curve displacements and decreases in maximal agonist responses. The mixture of serpentine, plus ajmalicine and catharanthine reveals a concentration-dependent inhibitory effect of acethylcholinesterase (AchE), with an IC50 at ca. 2.25 μg/Ml [1]. Catharanthine can induce the self-association of tubulin into linear indefinite polymers with an efficacy that is 75% that of vinblastine or vincristine. Catharanthine binds to tubulin alpha-beta dimer with binding constant of 2.8 mM [2]. Catharanthine stimulates release of amylase from pancreatic fragments and to cause extensive degranulation of pancreatic acinar cells with accumulation of membrane material in the Golgi region. Catharanthine induces a delayed release of Ca2+ from prelabeled pancreatic fragments as compared to bethanechol [3]. Catharanthine inhibits epibatidine-induced Ca(2+) influx in TE671-α, -β, -γ, -δ cells in a noncompetitive manner with similar potencies IC50 of 17 mM-25 mM. Catharanthine inhibits [3H]TCP binding to the desensitized Torpedo AChR with higher affinity compared to the resting AChR. Catharanthine enhances [3H]cytisine binding to resting but activatable Torpedo AChRs, suggesting desensitizing properties [4].
Prasinezumab (PRX 002) is a humanized IgG1 monoclonal antibody directed against aggregated α-synuclein. Prasinezumab has the potential for Parkinson's disease research[1].
Metamizole sodium is a non-opioid compound with excellent analgesic and antipyretic effects. Metamizole (sodium) is a cyclooxygenase-3 (COX-3) inhibitor[1][2].
Venlafaxine-d6-1 is deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
MR2938 is a potent AChE inhibitor, with an IC50 of 5.04 μM. MR2938 also suppresses NO production obviously (IC50 = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research[1].
JNK-IN-11 (compound 1) is a potent JNK inhibitor with an IC50 value of 2.2, 21.4, 1.8 µM for JNK1, JNK2, JNK3, respectively. JNK-IN-11 has the potential for the research of alzheimer and parkinson disease[1].
MEN 15596 is a potent and selective tachykinin NK2 receptor antagonist with a pKi of 10.1.
CuATSM is a highly potent radical-trapping antioxidant (RTA) and inhibitor of (phospho)lipid peroxidation, thereby accounting for its (their) ability to inhibit ferroptosis.
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy[1][2].
A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1.
Sulthiame-d4 is the deuterium labeled Sultiame. Sultiame is a carbonic anhydrase inhibitor, widely used as an antiepileptic agent[1][2].
Dipraglurant (ADX 48621) is a mGluR5 antagonists with IC50 of 0.021 μM. IC50 Value: 0.021 μM [1]Target: mGluRDipraglurant (ADX-48621) from Addex Therapeutics showed in vivo activity in different anxiety models in rat50 and is currently in phase II for the treatment of dyskinesia in Parkinson's disease.
Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.
Captopril is a potent, competitive inhibitor of angiotensin-converting enzyme (ACE).Target: ACECaptopril has been shown to have similar morbidity and mortality benefits to those of diuretics and beta-blockers in hypertensive patients. Captopril has been shown to delay the progression of diabetic nephropathy, and enalapril and lisinopril prevent the development of nephropathy in normoalbuminuric patients with diabetes [1]. an equimolar ratio of the cis and trans states of captopril exists in solution and that the enzyme selects only the trans state of the inhibitor that presents architectural and stereoelectronic complementarity with its substrate binding groove [2].
Arvanil is a ligand for vanilloid receptor 1 (VR1) and cannabinoid 1 (CB1). Arvanil can inhibit spasticity, as a potent neuroprotectant[1].
Homatropine is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent[1].
S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests[1][2].