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Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Songorine is a diterpenoid alkaloid which can be isolated from the genus Aconitum. Songorin has demonstrated anti-inflammatory, anti-anxiolytic and the ability to promote wound healing. The Anti-anxiolytic properties appear to be linked to the agonistic activity of the Dopamine D2 receptor as shown in rat hippocampal slices. The wound healing effect is the result of songorine's ability to stimulate the development of mesenchymal progenitor cells, although the exact mechanism of action remains unclear.
Fumitremorgin A (FTA) is the most potent mycotoxin among fumitremorgins, a series of tremorgenic toxins isolated from Aspergillus fumigatus by Yamazaki et al. in 1971. When injected intravenously in experimental animals, FTA causes tremor and generalized tonic-clonic convulsion. Both dopaminergic and gamma-aminobutyric acid (GABA)-ergic systems are involved in FTA-induced abnormal behaviors. On the other hand insignificant participation of serotonergic mechanism in modulation of those behavioral states elicited by FTA is conclusively suggested.
MK-3328 is azabenzoxazole derivative patented by American multinational pharmaceutical company Merck & Co., Inc. as amyloid binding compound useful for diagnostic evaluation changes of amyloid plaque level in living patients with Alzheimer’s disease. In preclinical trials MK-3328 was identified as a promising candidate, exhibiting amyloid binding potency balanced with low levels of nonspecific binding. In vivo,[18F]MK-3328 demonstrates favorable kinetics, exhibiting high brain uptake and good washout in normal rhesus monkey PET imaging studies. In 2011 MK-3328 was studied in phase I clinical trials but no further development reports were published.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
The sesquiterpene trilactone bilobalide is one of the active constituents of the 50:1 Ginkgo biloba leaf extract widely used to enhance memory and learning. Bilobalide was found to antagonise the direct action of gamma-aminobutyric acid (GABA) on recombinant alpha(1)beta(2)gamma(2L) GABA(A) receptors. Bilobalide showed anticonvulsant properties through the activation of glutamic acid decarboxylase (GAD) enzyme, which is a key enzyme in biosynthesis of GABA. Bilobalide has been proposed to exert protective and trophic effects on neurons. Bilobalide may be useful in developing therapy for diseases involving age-associated neurodegeneration. Bilobalide is an active component of EGb, a standardised extract of Ginkgo biloba leaves. Bilobalide accounts for about 3% of the total extract.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
SCH-442416 is a selective antagonist of the adenosine A2a receptor with a Ki of 0.48 nM. It was first designed and developed as an [11C] radioisotope for PET imaging and has seen some use as an investigational and diagnostic tool, including one human study (see: SCH-442416 C-11). The non-radiolabeled compound has garnered less interest. SCH-442416 has been investigated in rats as a treatment for learned cocaine addiction; However, another study in rats indicates that SCH-442416 upregulates expression of glutamate synthase (GS) and glutamate aspartate transporter (GAST) in Muller Cells which can exacerbate conditions such as Ocular Hypertension.
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Norfluoxetine is an active N-desmethyl metabolite of the antidepressant fluoxetine that inhibits serotonin uptake. Norfluoxetine is selective serotonin reuptake inhibitor (SSRI) but little is known about its pharmacological actions. Seproxetine (S- Norfluoxetine) was being investigated by Eli Lilly as an antidepressant but development was never completed and the drug was never marketed.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Echinocystic acid (EA) is a pentacyclic triterpene isolated from the fruits of Gleditsia sinensis Lam, has potent antioxidant, anti-inflammatory and anti-tumor properties. Echinocystic acid (EA) inhibit the formation of osteoclast. EA inhibit RANKL-induced NF-κB activation and ERK phosphorylation in BMMs. Echinocystic acid inhibits IL-1β-induced COX-2 and iNOS expression in human osteoarthritis chondrocytes. Echinocystic acid also inhibited TPA-induced myeloperoxidase activity, as well as COX-2, iNOS, TNF-α and IL-1β expressions. Echinocystic acid inhibited NF-κB in TPA-treated mouse ears, as well as in lipopolysaccharide-stimulated peritoneal macrophages. Its potency is comparable with that of dexamethasone. These findings indicate that echinocystic acid may ameliorate inflammatory diseases, such as dermatitis. EA inhibited ACAT and DGAT, with IC50 values of 103 and 139 uM, respectively, and exhibited no significant effect on HMG-CoA reductase activity. The present findings suggest that EA may exert hypolipidemic effect by inhibiting the activity of ACAT and DGAT.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Olomoucine acts as a competitive inhibitor of ATP in cyclin-dependent kinase 1/2/5, and mitogen-activated protein kinase 1. Olomoucine is an anti-mitotic compound that induces cell death preferentially in cancer cell lines, but also at a slower rate in non-cancer cells. It has been studied pre-clinically in a number of cancer models but has not been reported in any human trials. Olomoucine has also seen some preliminary investigation in mouse models of Herpes Simplex Viral Encephalitis.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
JWH-018 is a full agonist synthetic cannabinoid with a high binding affinity to CB1 and CB2 cannabinoid receptors. JWH-018 has not been used in therapy. Many of the risks linked to cannabis use are also present in the case of JWH-018, among them complications in patients suffering from cardiovascular diseases and triggering of acute psychosis. JWH-018 has not been used in therapy. Studies in mice showed anti-inflammatory and cancer chemopreventive properties of JWH-018.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Kalopanaxsaponin B is the main component of stem bark of Kalopanax pictus Nakai (KP, family Araliaceae), which has been used for inflammation in Chinese traditional medicine. Kalopanaxsaponin B also exhibits pro-cognitive action in mouse models of memory deficit.