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Restrict the search for
m apalutamide
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Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have a nanomolar affinity for the 5-HT2B receptor (pKi = 9.5 /-0.1) and 1,000 fold selectivity for this receptor as compared to numerous other receptors and ion channel binding sites. RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pK(B) = 9.5 /-0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4 /-0.1). RS-127445 also blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5 /-1.1) and ( /-)alpha-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9 /-0.3). RS-127445 (MT-500) was being developed for the prophylactic treatment of migraine. POZEN acquired MT-500 from Roche in November 1999 and assumed full responsibility for its development for migraine prophylaxis.
Homoveratrylamine (3,4-dimethoxyphenethylamine, DMPEA) is an analog of the major neurotransmitter dopamine where 3- and 4- position hydroxyl groups are replaced with methoxy groups. DMPEA is a metabolite of dopamine and is reported to be produced at elevated levels in patients with schizophrenia and Parkinson's disease. DMPEA inhibited monoamine oxidase and demonstrated no peripheral and central antidopaminergic activity in vivo.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Sphingosine harbors two chiral centers and therefore exhibits four stereoisomers, only one of which, the D-erythro (2S,3R) is known to exist naturally. ERYTHRO-SPHINGOSINE, (±)- is a mixture of two isomers: inactive ERYTHRO-SPHINGOSINE, (+)- and the active ERYTHRO-SPHINGOSINE, (-), also known as D-erythro (2S,3R)-SPHINGOSINE or D-erythro –SPHINGOSINE. It was found, that D-erythro –SPHINGOSINE acts as a potent inhibitor of protein kinase C and of transient receptor potential melastatin 7 (TRPM7). Besides, was shown, that sphingosine may be efficacious against alveolar rhabdomyosarcoma, irrespective of TP53 mutation status. It also could evolve as alternative treatment options for aggressive lymphomas via PKC inhibition, apoptosis, and autophagy.
