(S)-Amisulpride (Esamisulpride) is a potent dopamine D2/D3 receptor antagonist. (S)-Amisulpride is an antagonist at the 5-HT7 receptor with a KI of 900 nM. (S)-Amisulpride has antipsychotic and antidepressant effects[1][2].
ML 10302 is a potent agonist 5-HT4 receptor with Ki of 1.07 nM. 5-Hydroxytryptamine (5-HT4) receptor agonists stimulate gut motility through cholinergic pathways. ML10302 induces significant prokinesia both in the small bowel and colon through activation of cholinergic pathways. ML 10302 also has the potential for the research of neurology diseases[1].
CCR5 antagonist 2 (Compound 25) is a CCR5 antagonist with an IC50 of 8.34 nM. CCR5 antagonist 2 shows broad-spectrum anti-HIV-1 activities[1].
QF0301B is an α1 adrenergic receptor antagonist and a low α2 adrenoceptor, 5-HT2A, and histamine H1 receptor blocker.
MK-212 (CPP) monohydrochloride is a centrally acting 5-HT1C/5-HT2 agonist. MK-212 monohydrochloride can stimulate phosphoinositide hydrolysis in cerebral cortex[1].
Piriprost (U-60,257B) potassium is an inhibitor of leukotriene synthesis. Piriprost potassium inhibits the release of both leukotriene and histamine with an IC50 of 0.11 μM from isolated porcine lung cells. Piriprost potassium increases alkaline phosphatase (ALP) activity in cultured endometrial stromal cells[1][2].
Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.IC50 value: Target: D2DR/D4DR; 5-HT receptorin vitro: In the presence of Loxapine, [3H]ketanserin binds to 5-HT2 receptor in Frontal cortex of brain in human and bovine with ki value of 6.2 nM and 6.6 nM, respectively. Loxapine has the rank order of potency for the various receptors appears to be as follows:5-HT2≥D4>>>D1>D2 in comparing competition experiments involving the human membranes [1]. Loxapine 0.2 μM, 2 μM and 20 μM reduces IL-1beta secretion by LPS-activated mixed glia cultures after 1 and 3 days of exposure. Loxapine in concentrations of 0.2 μM, 2 μM and 20 μM reduces IL-2 secretion in mixed glia cultures after 1 and 3 days of exposure, and additionally Loxapine decreases IL-1beta and IL-2 secretion in LPS-induced microglia cultures in concentrations of 2 μM, 10 μM and 20 μM [2].in vivo: Loxapine (5 mg/kg) induces a very significant reduction (more than 50%) of serotonin (S2) receptor density after 4 weeks or 10 weeks of daily injection in the rat. Loxapine (5 mg/kg) does not change dopamine receptor density but greatly reduces serotonin receptor density by 47% in the brain of rats [3].
SORT-PGRN interaction inhibitor 1 is a potent inhibitor of the sortilin-progranulin interaction with an IC50 of 2 μM[1].
GSK1521498 free base is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs[1].
FR173657 is an orally active bradykinin B2 receptor antagonist (IC50: 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively). FR173657 (p.o.) inhibits BK-induced bronchoconstriction in guinea-pigs (ED50: 0.075 mg/kg). FR173657 (p.o.) also inhibits Carrageenin-induced paw oedema in mice (ED50: 6.8 mg/kg). FR173657 can be used for research of inflammatory disease[1].
H-Glu(OtBu)-OtBu hydrochloride is a glutamate derivative that can be used for substance P antagonist synthesis[1].
KRAS inhibitor-21 (22b) is a KRAS G12C inhibitor with an IC50 value of <0.01 μM. KRAS inhibitor-21 can be used in cancer research[1].
DSP-1053 is a novel potent serotonin reuptake (SERT) inhibitor with 5-HT1A partial agonistic activity that binds to human serotonin transporter and 5-HT1A receptor with Ki of 1.02 and 5.05 nM, respectively; inhibits serotonin transporter with IC50 of 2.74 nM and shows an intrinsic activity for 5-HT1A receptors of 70.0%; dose-dependently increases extracellular 5-HT levels in rat microdialysis at 3-10 mg/kg, demonstrates antidepressant-like effect in vivo. Depression Phase 1 Discontinued
TMPPAA is an allosteric agonist and positive allosteric modulator of the 5-HT3 receptor. TMPPAA enhances 5-HT-mediated 5-HT3AR signaling[1].
GPR119 agonist 2 (compound 43) is an orally active GPR119 agonist. GPR119 agonist 2 shows good pharmacokinetic characteristics in rodents and can effectively improve glucose tolerance in mice and rats. GPR119 agonist 2 has the potential to study type 2 diabetes[1].
Sequifenadine is a H1-antihistamine. Sequifenadine has the potential for the research of inflammatory eye disease with allergic symptoms[1][2].
FK888 is a potent, selective, and high affinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration[1].
NSC 23766 trihydrochloride is an inhibitor of Rac1 activation.
Guanfacine is a selective α2A receptor agonist.Target: α2A ReceptorGuanfacine is a sympatholytic. It is a selective α2A receptor agonist. These receptors are concentrated heavily in the prefrontal cortex and the locus coeruleus, with the potential to improve attention resulting from interaction with receptors in the former. Guanfacine lowers both systolic and diastolic blood pressure by activating the central nervous system α2A norepinephrine autoreceptors, which results in reduced peripheral sympathetic outflow and thus a reduction in peripheral sympathetic tone [1, 2].
TRAP-5 amide is a protease-activated receptor 1 (PAR 1) agonist peptide[1].
(S)-Veliflapon ((S)-BAY X 1005; (S)-DG-031) is an orally active inhibitor of leukotriene biosynthesis and 5-lipoxygenase activating protein (FLAP). (S)-Veliflapon inhibits the formation of leukotriene B4 (LTB4) in rat, mouse and human leukocytes with IC50 values of 0.026 µM, 0.039 µM and 0.22 µM respectively. (S)-Veliflapon showes enantioselectivity in human whole blood[1][2][3].
Triprolidine is an orally active H1R Antagonist antagonist. Triprolidine has the function of spinal cord motor and sensory block. Triprolidine can be used for the research of allergic rhinitis[1][2][3].
Sumatriptan succinate (GR 43175) is a serotonin1 (5-HT1) receptor agonist, which is effective in the acute treatment of migraine headache.Target: 5-HT 1d receptor agonistSumatriptan succinate is a serotonin1 (5-HT1) receptor agonist, which is effective in the acute treatment of migraine headache. Its antimigraine activity is believed to derive from selective vasoconstriction of cranial blood vessels which are dilated and distended during migraine headache and/or from inhibition of neurogenically mediated inflammation in the dura mater [1].For sumatriptan succinate 50 mg versus placebo the NNTs were 6.1, 7.5, and 4.0 for pain-free at two hours and headache relief at one and two hours, respectively. NNTs for sustained pain-free and sustained headache relief during the 24 hours postdose were 9.5 and 6.0, respectively [2]. Difference in time-weighted (0-2.5 h) mean arterial pressure MAP (90% confidence interval) was 1.2 mmHg (-0.2, 2.7) between telcagepant and placebo, 4.0 mmHg (2.5, 5.5) between sumatriptan succinate and placebo, and 1.5 mmHg (0.0, 3.0) between telcagepant with sumatriptan succinate vs sumatriptan succinate alone. When coadministered with telcagepant, the AUC0-6h and C(max) of sumatriptan succinate were increased by 23% and 24%, respectively. The small MAP increases observed after coadministration could possibly be associated with the slight elevations in sumatriptan succinate levels [3].Clinical indications: Cluster headache; MigraineToxicity: Symptoms of overdose include convulsions, tremor, paralysis, inactivity, ptosis, erythema of the extremities, abnormal respiration, cyanosis, ataxia, mydriasis, salivation, and lacrimation
VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM[1].
Doxazosin D8 (UK 33274 D8) is a deuterium labeled Doxazosin (UK 33274). Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1 adrenergic receptors[1].
Arborine, isolated from Glycosmis arborea, inhibits the peripheral action of acetylcholine and induces a fall in blood pressure[1][1].
Tropisetron(SDZ-ICS 930) is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. IC50 value: 70.1 ± 0.9 nM [1]Target: 5-HT3 receptorin vitro: Tropisetron specifically inhibited both IL-2 gene transcription and IL-2 synthesis in stimulated T cells. tropisetron inhibited both the binding to DNA and the transcriptional activity of NFAT and AP-1. We also observed that tropisetron is a potent inhibitor of PMA plus ionomycin-induced NF-(kappa)B activation but in contrast TNF(alpha)-mediated NF-(kappa)B activation was not affected by this antagonist [2]. Tropisetron prevents the phosphorylation and thus activation of the p38 MAPK, which is involved in post-transcriptional regulation of various cytokines [3].in vivo: Two different doses of tropisetron (5 and 10 mg/kg) or vehicle were administered intraperitoneally 30 min before pMCAO. Neurological deficit scores, mortality rate and infarct volume were determined 24 h after permanent focal cerebral ischemia [4].
Pilocarpine nitrate is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
(1S,3R)-ACPD is a mGluR agonist that can depolarize pyramidal cells[1].
Piribedil hydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil hydrochloride is also a α2-adrenoceptors antagonist. Piribedil hydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil hydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4].