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Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
SB-277011 is a potent and selective dopamine D(3) receptor antagonist. SB-277011 attenuates reinforcing propertes of drugs of abuse incluting opiates, cocaine, methamphetamine, nicotine and ethanol. SB-277011A produced a significant decrease in food intake in obese rats. Clinical development of SB-277011A has been halted by GlaxoSmithKline Pharmaceuticals, due to poor bioavailability (~2%) and a very short half-life (<20 min) in primates.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
S-17092, a prolyl endopeptidase inhibitor, is in phase I investigations with Servier in France for its potential in cognition disorders. Prolyl endopeptidase is involved in the metabolic breakdown of a number of neuropeptide neurotransmitters in the brain, and so inhibiting the action of the enzyme increases the activity of these neuropeptides. This produces nootropic effects which make S-17092 a promising and novel treatment for neurodegenerative conditions such as Alzheimer's disease and Parkinson's disease.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
3-Methoxytyramine (3-MT) is a human trace amine that occurs as a metabolite of the neurotransmitter dopamine. It has been shown to act as an agonist of human TAAR1, and an inhibitor of mitochondrial respiration. 3-MT has garnered research interest for its potential links and implications to Parkinson's disease and other Neurological disorders.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
GW7647 is a potent and highly selective PPARα agonist (EC50 values are 6, 1100 and 6200 nM for human PPARα, PPARγ and PPARδ receptors respectively). GW7647 has being shown to protect the heart from ischemia/reperfusion injury in mouse model. GW7647 attenuated ischemia/reperfusion-induced release of multiple proinflammatory cytokines and inhibited neutrophil accumulation and myocardial expression of matrix metalloproteinases-9 and -2. Furthermore, GW7647 inhibited nuclear factor-kappaB activation in the heart, accompanied by enhanced levels of inhibitor-kappaBalpha.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
CBiPES is a selective positive allosteric modulator of the metabotropic glutamate receptor group II subtype mGluR2. CBiPES attenuated a stress-induced hyperthermia and PCP-induced hyperlocomotor activity in the mouse model.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
is a potent, selective, brain penetrant, orally active serotonin 5-HT(6) receptor antagonist with cognitive enhancing, anxiolytic and antidepressant properties. It is able to regulate sleep and wakefulness in rodents. In addition it demostrates antinociceptive and antiepileptic potentials.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Prostaglandin H2 (PGH2) is a type of Prostaglandin which is derived from arachidonic acid and is a precursor for many other biologically significant molecules. Prostaglandins are synthesized from arachidonic acid by the prostaglandin-endoperoxide synthase enzymes, which are also called Cyclooxygenases. These enzymes generate a reactive intermediate PGH2 which has a reasonably long half-life (90-100 s). PGH2 is converted into the biologically active prostaglandins by prostaglandin isomerases, yielding Prostaglandin E2, D2 and F2 (PGE2, PGD2, and PGF2), or by thromboxane synthase to make Thromboxane A2 (TxA2) or by prostacyclin synthase to make Prostaglandin I2 (PGI2). Prostaglandin H2 was first isolated from incubations of arachidonic acid with ovine seminal vesicle microsomes, and was described as a potent vasoconstrictor. Thromboxane receptors can be activated by PGH2 and TxA2, as well as isoprostanes, all of which produce vasoconstriction. Activation of TP receptors by either PGH2 or TxA2 contributes to hypertension of pregnancy and to the elevation of blood pressure in some forms of experimental hypertension, particularly those that involve activation of the renin-angiotensin system.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
BMS-794833 (N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-5-(4- fluorophenyl)-4-oxo-l,4-dihydropyridine-3-carboxamide) is an inhibitor of Met, VEGFR2, Ron, Axl and Flt-3 kinases. BMS-794833 demonstrated dose-dependent tumor
growth inhibition following oral administration in xenograft models. In cell culture, BMS-794833 inhibited
the proliferation of human tumor cell lines containing constitutively activated
Met receptor. BMS-794833 is an active moety of pro-drug BMS-817378. Bristol-Myers Squibb and Simcere Pharmaceutical Group are developing BMS-817378 for treatment of cancer.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
25CN-NBOH (or NBOH-2C-CN) is a compound indirectly derived from the phenethylamine series of hallucinogens, which was discovered in 2011 by Martin Hansen at the University of Copenhagen. This compound is notable as one of the most selective agonist ligands for the 5-HT2A receptor yet discovered, with a pKi of 8.88 at the human 5-HT2A receptor and with 100x selectivity for 5-HT2A over 5-HT2C, and 46x selectivity for 5-HT2A over 5-HT2B
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
(-)-∆8-Tetrahydrocannabinol (∆8-THC) has a very similar pharmacologic profile as (-)-∆9-tetrahydrocannabinol (∆9-THC), the most active constituent of cannabis. Delta-8-tetrahydrocannabinol (THC) has activity in man similar to that of its double-bond isomer, delta-9-THC. The spatial orientation of the side chain seems to play a pivotal role in cannabinergic activity. Introduction of a triple bond in the benzylic position of the n-heptyl-D8-THC analogue led to the classical cannabinoid AMG-1 with high CB1 and moderate CB2 affinity. AMG-1 is an analgesic drug which is a cannabinoid agonist.