Description
(±)-McN 5652 is a highly potent inhibitor of serotonin (5-HT, 5-hydroxytryptamine) uptake with a Ki value of approximately 0.6 nM in rat brain synaptosomes in vitro and an ED50 value of approximately 2 mg/kg p.o. ex vivo . 5-HT is a monoaminergic neurotransmitter to modulate numerous sensory, behavioural processes and motor in the mammalian nervous system . There are at least three main groups of 5-HT receptor: 5-HT1, 5-HT2, and 5-HT3. Each group is not only structurally but also operationally distinct. Each receptor group has its own distinct transduction system. 5-HT4 is the more recently identified receptor. It almost represents a fourth 5-HT receptor class . Receptor binding experiments indicated that McN-5652 has a weak affinity for serotonin 5-HT2 receptor (apparent Ki approximately 200 nM) and a very low affinity for serotonin 5-HT1 receptor . In vivo, McN-5652 was required in low doses to potentiate the serotonin syndrome in rats. For this serotonin syndrome, the ED50 value was 1.5 mg/kg 2 hr after p.o. dosing. To potentiate head twitches which were induced by L-5-hydroxytryptophan (L-5HTP) in mice, the ED50 value is just 0.4 mg/kg 2 hr after p.o. dosing. That means McN-5652 is of high potency as a serotonin uptake inhibitor .
Product information
CAS Number: 96795-89-0
Molecular Weight: 295.44
Formula: C19H21NS
Chemical Name: (6R,10bS)-6-[4-(methylsulfanyl)phenyl]-1H,2H,3H,5H,6H,10bH-pyrrolo[2,1-a]isoquinoline
Smiles: CSC1C=CC(=CC=1)[C@H]1CN2CCC[C@H]2C2=CC=CC=C21
InChiKey: YVKDUIAAPBKHMJ-MOPGFXCFSA-N
InChi: InChI=1S/C19H21NS/c1-21-15-10-8-14(9-11-15)18-13-20-12-4-7-19(20)17-6-3-2-5-16(17)18/h2-3,5-6,8-11,18-19H,4,7,12-13H2,1H3/t18-,19+/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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