Galanin (1-30), human is a 30-amino acid neuropeptide, and acts as an agonist of GalR1 and GalR2 receptors, with Kis of both 1 nM.
Lumateperone (ITI-007) is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia[1][2][3].
L-365260 is a potent and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance[1][2][3].
Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
Norfenefrine hydrochloride is an orally active, endogenously found α-adrenergic agonist and can be used for the research of female stress incontinence[1][2].
Ro 64-6198 is a nonpeptidic, selective, brain-penetrant agonist of nociceptin/orphanin FQ receptor (NOP receptor/ORL1) with pKi of 9.41; displays >100-fold selectivity for ORL1 over other members of opioid receptor family; elicits dose-dependent anxiolytic-like effects in models of distinct types of anxiety states in rata, with no efficient anti-panic-like activity, absence of anticonvulsant properties, and lack of effects on motor performance and cognitive function at anxiolytic doses (0.3 to 3 mg/kg i.p.). Anxiety Discontinued
Bifeprunox mesylate is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox mesylate is an antipsychotic for the research of schizophrenia[1][2].
Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).Target: α1 adrenergic receptorAlfuzosin, a new quinazoline derivative, acts as a selective and competitive antagonist of alpha 1-adrenoceptor-mediated contraction of prostatic, prostatic capsule, bladder base and proximal urethral smooth muscle, thereby reducing the tone of these structures. Consequently, urethral pressure and resistance, bladder outlet resistance, bladder instability and symptoms associated with benign prostatic hyperplasia are reduced. A limited range of clinical studies have shown oral alfuzosin to be more effective than placebo (in studies of < or = 6 months duration), to have sustained effects on long term administration (< or = 30 months), and to be comparable with the alpha 1-adrenoceptor antagonist prazosin, in the symptomatic treatment of benign prostatic hyperplasia.Oral alfuzosin 7.5 to 10 mg/day in divided doses appears to be a promising first-line agent for symptomatic treatment of noncomplicated mild to moderate benign prostatic hyperplasia in patients with a high dynamic component to their obstruction. In addition, alfuzosin offers an alternative to prostatectomy (the current 'gold standard') in patients who require surgery but are unfit for this treatment, and in patients requiring symptomatic relief while awaiting surgery.
Eptazocine (Sedapain) is a κ-opioid receptor agonist and μ-opioid receptor antagonist. Eptazocine has the effect of relieving pain[1].
SCH 58261 is the adenosine A2A receptor competitive antagonist. Displays 323-, 53- and 100-fold selectivity over A1, A2B and A3 receptors, respectively.target: adenosine A2A receptorIC50: 15 nM [3]in vitro: NK cells were cultured in NK cell media and preincubated with or without 1 uM SCH58261 30 min before simulation with indicated concentrations of IL-18 (R & D Systems) and IL-12p70 (Australian Biosearch) in the presence or absence of NECA (1 uM) or CGS-21680 (100 nM).[1]in vivo: it was demonstrated that the selective antagonist of the A2Areceptor, SCH58261, administered i.p. starting from the early minutes after ischemia induction, reduces ischemic brain damage and neurological deficit 24 h thereafter. vehicle-rats received saline with Tween 80 (1 %) administered (i.p.) .SCH58261 (0.01 mg/kg, i.p.), administered twice/day for 7 days [2]
Tridihexethyl (Pathilon) chloride is an orally active anticholinergic agent and mAChR antagonist, shows activities of antimuscarinic and anticholinergic. Tridihexethyl chloride shows pronounced antispasmodic and antisecretory effects on the gastrointestinal tract. Tridihexethyl chloride can be used in studies of peptic ulcer disease and acquired nystagmus [1][2].
KRAS inhibitor 11 is a first-in-class, high-affinity, noncovalent allosteric KRAS inhibitor, disrupts KRAS-Raf interaction with Kd of 1.2 uM; binds to activated KRAS with sub-micromolar affinity and disrupts effector binding, thereby inhibiting KRAS signaling and cancer cell growth; dose-dependently decreases both p-ERK and p-cRaf levels in BHK cells expressing KRASG12D and KRASG12V, suggesting inhibition of RAS signaling via the MAPK pathway.
Paliperidone palmitate (9-Hydroxyrisperidone palmitate), an atypical long-acting antipsychotic agent, is an ester prodrug of Paliperidone. Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class. Paliperidone palmitate shows efficacy against schizophrenia[1].
Olopatadine-d6 is the deuterium labeled Olopatadine[1]. Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis[2][3].
Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV)[1][2].
Hydrocortisone is a steroid hormone or glucocorticoid secreted by the adrenal cortex.
Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors.
CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity[1].
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used to treat for cognitive disorders associated with Alzheimer＇s disease[1][2][3].
Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes mellitus (T2DM). Sequence: His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-Lys-Lys-Lys-Lys-Lys-Lys-NH2.
JP1302 is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 shows antidepressant and antipsychotic-like effects. JP1302 can be used for neuropsychiatric disorders and renal dysfunction research[1][2][3].
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn107 and NPSR Ile107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia[1][2].
JHW007 hydrochloride is the hydrochloride of JHW007. JHW007 is an antagonist of cocaine[1].
BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM)[1].
ATP-γ-S tetrasodium, an ATP analogue, is a P2Y11 receptor agonist. ATP-γ-S tetrasodium is active in ATP hydrolysis. ATP-γ-S tetrasodium is also an antioxidant and neuroprotectant[1][2].
TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively.
ML193 (CID 1261822) is a potent, selective GPR55 antagonist with IC50 of 221 nM, shows >27-, >145- and >145-fold selectivity for GPR55 over CB1, GPR35 and CB2, respectively; reduces neuronal differentiation in vitro, increases anxiety-like behaviors while causing locomotor impairment by i.c.v. injection at the doses of 0.1 and 1 μg/rat.
MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases, with EC50 ranging from 16 μM to 120 μM. MLS000532223 prevents GTP binding to several GTPases. Small GTPases are key regulators of cellular activity [1].
Mequitazine is a potent, nonsedative and long-acting histamine H1 antagonist.
Piperidolate is an antimuscarinic, inhibits intestinal cramp induced by acetylcholine (rats and dogs).