Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent[1][4].
3-Indolepropionic acid is shown to be a powerful antioxidant and has potential in the treatment for Alzheimer’s disease.
L-Hyoscyamine sulfate (Daturine sulfate) is a tropane alkaloid that is a secondary metabolite found in certain plants of the solanaceae family. In vitro it has been shown to be an antagonist of mAChR[1].
CNS-11 is a compoud that disaggregates tau fibrils. CNS-11 can be used for Alzheimer's disease (AD) research[1].
AMG 8379 (AMG-8379, AMG8379) is a potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM; potently blocks endogenous tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglion (DRG) neurons with IC50 of 3.1 nM in whole-cell patch clamp electrophysiology assays; displays100- to 1000-fold selectivity over other NaV family members, including NaV1.4 and NaV1.5; blocks mechanically induced action potential firing in C-fibers, reduces the frequency of thermally induced C-fiber spiking; exhibits pharmacodynamic effects in translatable models of both itch and pain.
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent[1].
Dianicline is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of drugs that includes varenicline and cytisine for smoking cessation. Dianicline increases cessation rates in a dose-dependent manner[1].
(Des-Bromo)-Neuropeptide B (1-23) (human) is an orphan G-protein coupled receptor agonist with Kis of 1.2 nM and 341 nM for GPR7 (NPBW1) and GPR8 (NPBW2), respectively[1].
JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.IC50 value: 7.6/14/3.7 nM(mouse/rat/human MAGL) [1]Target: MAGL inhibitorJW 642 is selective for MAGL, requiring much higher concentrations to effectively inhibit fatty acid amide hydrolase activity (IC50s = 31, 14, and 20.6 μM for mouse, rat, and human brain membranes, respectively).
S-Methyl-L-cysteine is a natural product that acts as a substrate in the catalytic antioxidant system mediated by methionine sulfoxide reductase A (MSRA), with antioxidative, neuroprotective, and anti-obesity activities.
Vanoxerine dihydrochloride is a potent and selective dopamine reuptake inhibitor.
A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 0.12 uM, >400-fold selectivity over ChoKβ; demonstrates in vitro antiproliferative activity against HT29 cells with IC50 of 2.08 uM.
Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1 mice[1][2].
(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects[1][2].
Tampramine fumarate is a potent, selective, noncompetitive NE reuptake inhibitor. Tampramine fumarate has antidepressant activity. Tampramine fumarate can be used in research of depression[1].
6-Demethoxytangeretin is a citrus flavonoid isolated from Citrus depressa. 6-Demethoxytangeretin exerts anti-inflammatory activity and anti-allergic activity, suppresses production and gene expression of interleukin-6 in human mast cell-1 via anaplastic lymphoma kinase (ALK) and mitogen-activated protein kinase (MAPK) pathways[1]. 6-Demethoxytangeretin facilitates the CRE-mediated transcription associated with learning and memory in cultured hippocampal neurons[2].
Eltoprazine (DU 28853) dihydrochloride is a 5-HT1A/5-HT1B receptors agonist and a 5-HT2C receptor antagonist. Eltoprazine dihydrochloride shows antiaggressive and anxiogenic effects[1][2].
BZAD-01 is a potent, selective and orally active inhibitor of NMDA NR2B subunit, with a Ki of 72 nM. BZAD-01 can improve postural asymmetry as well as Apomorphine-induced rotation[1].
Rocuronium Bromide is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia, to facilitate endotracheal intubation and to provide skeletal musclerelaxation during surgery or mechanical ventilation.IC50 Value:in vitro: Rocuronium reduced the indirectly elicited twitch tensions in normal (50% inhibitory concentration [IC(50)], 9.84 [9.64-10.04] μM, mean [95% confidence interval]) and all pretreated diaphragms (P < .01, n = 6) in a concentration-dependent fashion [1]. The ED95 of rocuronium is essentially the same for children as for adults. Its duration of action is similar to vecuronium, and it is shorter for children than for adults. Rocuronium is readily reversed with conventional doses of cholinesterase-inhibiting drugs [2]. Onset time until maximum block, duration until 25% recovery of twitch height, and recovery from 25 until 75% of twitch height were 1.7 (32), 53 (19) and 20 (37) min, respectively [3].in vivo: Only 8.7 +/- 5.7% (SD) and 6.0 +/- 2.8% of an injected dose of ORG 9426 and ORG 9616 was excreted into the urine, respectively. Conversely, 54.4 +/- 9.2% and 52.4 +/- 9.2% of an injected dose of ORG 9426 and 35.7 +/- 12.2% and 46.8 +/- 9.7% of ORG 9616 were excreted into the bile in cats without and with renal pedicle ligation, respectively [4].
Ropinirole hydrochloride(SKF101468 hydrochloride) a selective dopamine D2 receptor inhibitor with IC50 of 29 nM.Target: Dopamine D2 ReceptorRopinirole (50 mg/kg, i.p.) causes biphasic spontaneous locomotor activity in mice. Ropinirole (0.05-1.0 mg/kg SC) dose-dependently inhibits the dyskinesias induced by 2-di-n-propylamino-5,6-di-hydroxytetralin in mice. Ropirtirole, at doses of 1 and 10 μg, injected unilaterally directly into the striatum of the rat causes marked, contralateral (away from the side of injection) asymmetry and circling in mice. Ropinirole (0.05-1.0 mg/kg SC or 0.1 mg/kg PO) reverses all motor and behavioural deficits induced by MPTP in marmosets [1]. Ropinirole (2 mg/kg, i.p.) for 7 days increases GSH, catalase and SOD activities in the striatum and protected striatal dopaminergic neurons against 6-hydroxydopamine (6-OHDA) in mice [2]. Ropinirole (0.2 mg/kg, i.p.) improves the use of previously akinetic forelimb and produced robust circling behavior in lesioned rats with striatal over-expression of both D2R and D3R compared to lesioned animals that received blank vector. The subtherapeutic dose of ropinirole generates only modest motor effects in lesioned rats with sole over-expression of D2R or D3R [3]. Ropinirole (1-8 mg t.i.d.) is rapidly and completely absorbed with oral bioavailability of 55%, clearance of 780 mL/min, elimination half-life of 6 hours in healthy volunteer. Since the major route of elimination for Ropinirole is by the CYP enzyme system, mainly by CYP1A2 and also by CYP3A4, inhibition of the former and possibly the latter may reduce the agent's clearance and lead to drug accumulation [4].
Mad1 (6-21) is the 6-21 fragment of Mad1 protein. Mad1 (6-21) binds to mammalian Sin3A PAH2 with a Kd of ~29 nM[1].
(S)-MCPG is the active isomer of (RS)-MCPG (Cat. No. HY-100371), non-selective group I/group II metabotropic glutamate receptor antagonist. In vivo: (S)-MCPG (20.8 μg) injected intraventricularly (i.c.v.) before testing impaired the performance of rats in the spatial version of the Morris water maze, but 1/10 of this dose did not. Memory retention, evaluated 24 hr post-training, is also affected by the high dose of MCPG.
Kinetin (N6-furfuryladenine) belongs to a group of plant growth hormones involved in cell division, differentiation and other physiological processes.IC50 Value: Target:Kinetin is one of the widely used components in numerous skin care cosmetics and cosmeceuticals, such as Valeant products kinerase. Recently, kinetin has the potential to be a treatment for the human splicing disease familial dysautonomia.in vitro: Kinetin-induced cell death reflected by the morphological changes of nuclei including their invagination, volume increase, chromatin condensation and degradation as well as formation of micronuclei showed by AO/EB and 4,6-diamidino-2-phenylindol staining was accompanied by changes including increase in conductivity of cell electrolytes secreted to culture media, decrease in the number of the G1- and G2-phase cells and appearance of fraction of hypoploid cells as the effect of DNA degradation without ladder formation [1]. The plant cytokinin kinetin dramatically increases exon 20 inclusion in RNA isolated from cultured FD cells [3].in vivo: Subjects received 23.5 mg/Kg/d for 28 d. An increase in WT IKBKAP mRNA expression in leukocytes was noted after 8 d in six of eight individuals; after 28 d, the mean increase compared with baseline was significant (p = 0.002) [2].Toxicity: On mice with leukaemia P388, kinetin has no effect on the tumour growth, and it appears to be toxic at the dose of 25 mg/kg [4].
GAT-211 (GAT211) is a selective cannabinoid 1 receptor (CB1R) positive allosteric modulator with pKb of 7.26, Arrestin2 EC50 of 775 nM; engages CB1R allosteric site(s), enhances the binding of the orthosteric full agonist [3H]CP55,490, and reduces the binding of the orthosteric antagonist/inverse agonist [3H]SR141716A; displayed both PAM and agonist activity in HEK293A and Neuro2a cells expressing human recombinant CB1R (hCB1R) and in mouse-brain membranes rich in native CB1R.
Carabersat is a potent anticonvulsant agent.
ERB-196 is a nonsteroidal selective estrogen receptor-β (ERβ) agonist.
MRS2698 is a potent and highly selective P2Y2 receptor agonist with an EC50 of 8 nM. MRS2698 is >300-fold P2Y2-selective versus the P2Y4 and P2Y6 receptors[1][2].
Saredutant is a selective NK2 receptor antagonist.
Piribedil is a dopamine D2 receptor (D2R) agonist which also displays antagonist property at hα1A-adrenoceptor (hα1A-AR).