Zacopride hydrochloride is a potent antagonist of 5-HT3 receptor with a Ki of 0.38 nM. Zacopride hydrochloride is also a agonist of 5-HT4 receptor with a Ki of 373 nM. Zacopride hydrochloride has anxiolytic activity. Zacopride hydrochloride has the potential for the research of Schizophrenia[1][2][3].
Dynorphin B (1-13) acts as an agonist on opioid κ-receptor.
Ala5-Galanin (2-11) is a galanin receptor 2 (GAL2R) specific agonist with a Ki of 258 nM[1].
Zafirlukast-d7 (ICI 204219-d7) is the deuterium labeled Zafirlukast. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects[1][2].
MF-766 (MF766) is a highly potent and selective EP(4) antagonist with binding Ki of 0.23 nM, displays no significant affinity (>7000-fold selectivity) against other PG receptors (IC50>1500 nM); behaved as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay; exhibits blockade of inhibition of TNFa-induced IP10 release by the specific EP4 agonist L-000902688 (IC50=9.5 nM); demonstrates potency and efficacy of in the rat AIA model measuring inhibition of paw swelling.
Siponimod (BAF-312) hemifumarate is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod hemifumarate is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10000, >1000, and 750 nM, respectively). Siponimod hemifumarate can be used for multiple sclerosis (MS) research[1][2].
Ebselen oxide, the selenone analogue of Ebselen, covalently modifies diguanylate cyclase (DGC) to inhibit c-di-GMP-receptor interactions and reduces DGC activity. Ebselen oxide also inhibits alginate production (IC50=14 μM) by Pseudomonas aeruginosa. Ebselen oxide inhibits HDAC1, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC9 (IC50 ranging from 0.2 to 4.7 μM)[1][2][3].
Medifoxamine is a monoamine re-uptake inhibiting antidepressive drug which preferentially inhibits dopamine reuptake[1].
A-836339 is a cannabinoid CB2 receptor-selective agonist; exhibits high potencies at CB(2) and selectivity over CB(1) receptors.IC50 value: 1.6 nM(EC50) [1]Target: CB2 agonistin vitro: In radioligand binding assays, A-836339 displays high affinities at CB(2) receptors and selectivity over CB(1) receptors in both human and rat.In addition A-836339 exhibits a profile devoid of significant affinity at other G-protein-coupled receptors and ion channels [1].in vivo: In the complete Freund's adjuvant model of inflammatory pain, A-836339 exhibits a potent CB(2) receptor-mediated antihyperalgesic effect that is independent of CB(1) or mu-opioid receptors. A-836339 has also demonstrated efficacies in the chronic constrain injury (CCI) model of neuropathic pain, skin incision, and capsaicin-induced secondary mechanical hyperalgesia models [1]. Similar to systemic delivery, intra-spinal injection of A-836339 (0.3 and 1 nmol) also attenuated both von Frey-evoked and spontaneous firing of WDR neurons in neuropathic rats. Intra-spinal injections of A-836339 were ineffective in sham rats [2]. Systemic A-836339 and AM1241 produced dose-dependent efficacy in both inflammatory and neuropathic pain models. Local administration of CB? agonists also produced significant analgesic effects in SNL (intra-DRG and i.t.) and CFA (intra-DRG) pain models [3].
N,N′-Diferuloylputrescine is a inhibitor of pigmentation with 57% reduction. N,N′-Diferuloylputrescine significantly reduces the protein level of MITF. N,N′-Diferuloylputrescine has strong antioxidant activities as radical scavengers against reactive oxygen species[1].
AL-438 is a potent, selective and orally active glucocorticoid receptor modulator with Kis of 2.5, 1786, 53, 1440, >1000 nM for glucocorticoid receptor, progesterone receptor, mineralocorticoid receptor, androgen receptor, estrogen receptor, respectively. AL-438 shows antiinflammatory activity[1][2].
Fenoterol is a β 2 adrenergic agonist designed to open up the airways to the lungs, is classed as sympathomimetic β2 agonist and asthma medication.
Ro 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETA receptors (IC50: 6800 nM)[1][2].
PF-06827443 (PF06827443) is a potent, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with EC50 of 47 nM, shows no activity against M2-M5 at 10 uM; induces cholinergic adverse events and convulsion at therapeutic indices similar to previous compounds with more agonist activity.
Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.Target: 5- HT3 ReceptorIC50 Value: in vitro: 5-HT evoked transient inward currents (EC50 = 3.4 microM; Hill coefficient = 1.8) that were blocked by the 5-HT3 receptor antagonist ondansetron (IC50 = 103 pM) [1]. The 5-HT3A receptor antagonist ondansetron (0.3 nM) reversibly inhibited the 5-HT (30 microM) signal by 70% and at 3 nM it abolished the response [2].in vivo: Acute ondansetron administration at the lowest dose (0.1 mg/kg, IP) tested had no effect, while other doses (0.33 and 1 mg/kg, IP) produced improvements in auditory gating [3]. Different doses of ondansetron were injected intraperitoneally (i.p.) at fixed times during the day to determine both the sublethal (TD50) and lethal (LD50) doses, which were, respectively, 3.7 +/- 0.6 mg/kg and 4.6 +/- 0.5 mg/kg [4]. ondansetron (0.25-1.0 mg/kg, subcutaneously) given before the challenge dose of ethanol (2.4 g/kg, intraperitoneally) injection, significantly and dose dependently attenuated the expression of sensitization. In addition, ondansetron (1.0 mg/kg, subcutaneously) given before ethanol injection on days 1, 4, 7, and 10 significantly blocked the development (days 1, 4, 7, and 10), and expression (day 15) of sensitization to the locomotor stimulant effect of ethanol injection [5]. Toxicity: Ondansetron may be safe in lower doses used to prevent nausea and vomiting in radiation treatment or postoperatively. However, as there is a report that a lower dose of ondansetron prolonged the QT interval in healthy volunteers, this needs to be clarified by the FDA [6].
Tomelukast (LY171883) is an orally active leukotriene D4 and E4 antagonist. Tomelukast can be used for the research of asthma[1].
AS1269574 is a potent, orally available GPR119 agonist, with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes[1][2].
PG106 is a potent and selective human melanocortin 3 (hMC3) receptor antagonist (IC50=210 nM) and has noactivity at hMC4 receptors (EC50=9900 nM) and hMC5 receptor[1].
UCB-35440, a 5-lipoxygenase inhibitor and a histamine H1 receptor antagonist, is used potentially for the treatment of dermatitis.
AZD8529 is a novel potent, selective mGluR2 positive allosteric modulator with EC50 of 195 nM, does not produce any positive allosteric modulator responses for mGluR1 and 3-8 subtypes; potentiates agonist-induced activation of mGluR2 in the membrane-binding assay and in primate cortex, hippocampus and striatum; decreases nicotine self-administration at doses (0.3-3 mg/kg) in monkeys, also reduces nicotine priming- and cue-induced reinstatement of nicotine seeking, decreases nicotine-induced accumbens dopamine release in rats. Schizophrenia Phase 2 Discontinued
CTCE-0214 is a chemokine CXC receptor 4 (CXCR4) agonist, SDF-1α (stromal cell-derived factor-1α) peptide analog. CTCE-0214 shows anti-inflammatory activity, and can be used in inflammation sepsis and systemic inflammatory syndromes research[1][2][3].
Ziprasidone(CP88059) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.Target: 5-HT receptor; Dopamine receptorZiprasidone (hydrochloride) is the salt form of ziprasidone, which possesses an in vitro 5-HT2A/dopamine D2 receptor affinity ratio higher than any clinically available antipsychotic agent. In vivo, ziprasidone antagonizes 5-HT2A receptor-induced head twitch with 6-fold higher potency than for blockade of d-amphetamine-induced hyperactivity, a measure of central dopamine D2 receptor antagonism. Ziprasidone also has high affinity for the 5-HT1A, 5-HT1D and 5-HT2C receptor subtypes, which may further enhance its therapeutic potential [1]. Ziprasidone sulfoxide and sulfone were the major metabolites in human serum. The affinities of the sulfoxide and sulfone metabolites for 5-HT2 and D2 receptors are low with respect to ziprasidone, and are thus unlikely to contribute to its antipsychotic effects [2]. Ziprasidone was associated with significant differential adverse effects relative to placebo in BPM, BPD, and schizophrenia with no significant difference in weight gain in all 3 groups. Self-reported somnolence was increased across the 3 conditions. Subjects with BPM were more vulnerable to EPS than those with BPD or schizophrenia [3].Clinical indications: Bipolar I disorder; Bipolar disorder; Mania; SchizophreniaFDA Approved Date: February 2001
S1P1 agonist 3 is a selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist for endothelial protection.
Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.
α1 adrenoceptor-MO-1, an S enantiomer, has affinity at alpha 1 adrenergic receptor, shows alphalytic activity, and possesses analgesic action; more active than R enantiomer.
Substance P TFA (Neurokinin P TFA) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R)[1].
PF-6870961 hydrochloride is an inverse agonist of GHSR1a with Ki values of 73.6 nM (human GHSR), 239 nM (rat GHSR), and 217 nM (dog GHSR), respectively. PF-6870961 hydrochloride inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 hydrochloride also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM[1].
Naratriptan is a selective 5-HT1 receptor subtype agonist and is a triptan drug that is used for the treatment of migraine headaches.Target: 5-HT1 ReceptorNaratriptan is a triptan drug marketed by GlaxoSmithKline and is used for the treatment of migraine headaches. Naratriptan is available in 2.5 mg tablets. It is a selective 5-HT1 receptor subtype agonist. Naratriptan is used for the treatment of the acute migraine attacks and the symptoms of migraine, including severe, throbbing headaches that sometimes are accompanied by nausea and sensitivity to sound or light.The causes of migraine are not clearly understood; however, the efficacy of naratriptans and other triptans is believed to be due to their activity as 5HT (serotonin) agonists.A meta-analysis of 53 clinical trials has shown that all triptans are effective for treating migraine at marketed doses and that naratriptan, although less effective than sumatriptan and rizatriptan was more effective than placebo in reducing migraine symptoms at two hours and efficacy was demonstrated in almost two thirds of subjects after four hours of treatment.
HAEGTFT is the first N-terminal 1-7 residues of GLP-1 peptide.
TFLLRN-NH2 is a biological active peptide. (PAR-1 Agonist)