206862-30-8
Chemical Structure
MS-377
- CAS No.: 206862-30-8
- Formula:C18H26ClN3O2
- Molecular Weight:351.87
IUPAC Name: (R)-1-(4-chlorophenyl)-3-((4-(2-methoxyethyl)piperazin-1-yl)methyl)pyrrolidin-2-one
InChIKey: DKVVPXLIRYCKCS-OAHLLOKOSA-N
SMILES: O=C1N(C2=CC=C(Cl)C=C2)CC[C@@H]1CN3CCN(CCOC)CC3
Biological Activity: MS-377 is a selective and orally active sigma-1 receptor ligand (Ki=73 nM) with weak affinity for sigma-2 receptor (Ki=6900 nM) and no affinity for any other receptors including dopamine, serotonin, PCP site, glutamate, γ-aminobutylic acid, adenosine, adrenergic receptors, etc. (Ki: >10 μM). MS-377 indirectly modulates the NMDA receptor ion-channel complex. MS-377 is a antipsychotic agent. MS-377 inhibits PCP-induced behaviors by inhibition of the increase in dopamine and serotonin release in the rat medial prefrontal cortex. MS-377 can be used for research of schizophrenia[1][2].
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MS-377 | MS-377 is a selective and orally active sigma-1 receptor ligand (Ki=73 nM) with weak affinity for sigma-2 receptor (Ki=6900 nM) and no affinity for any other receptors including dopamine, serotonin, PCP site, glutamate, γ-aminobutylic acid, adenosine, adrenergic receptors, etc. (Ki: >10 μM). MS-377 indirectly modulates the NMDA receptor ion-channel complex. MS-377 is a antipsychotic agent. MS-377 inhibits PCP-induced behaviors by inhibition of the increase in dopamine and serotonin release in the rat medial prefrontal cortex. MS-377 can be used for research of schizophrenia. | |||||||||||||||||||||
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- [1]. Karasawa, et al. MS-377, a selective sigma receptor ligand, indirectly blocks the action of PCP in the N-methyl-D-aspartate receptor ion-channel complex in primary cultured rat neuronal cells. Life Sci. 2002 Feb 22;70(14):1631-42. [Content Brief]
- [2]. Takahashi S, et al. MS-377, a novel selective sigma(1) receptor ligand, reverses phencyclidine-induced release of dopamine and serotonin in rat brain. Eur J Pharmacol. 2001 Sep 21;427(3):211-9. [Content Brief]
Keywords
