10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Desiccated,Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D 4 receptor antagonist with a K i of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D 2 ( K i of 960 nM) and D 3 ( K i of 2300 nM) receptors, and exhibits moderate affinity for 5-HT 2 receptors, sigma sites and α-adrenoceptors .
In Vitro
L-745870 is capable of antagonizing the ability of D 4 receptors to inhibit agonist-induced stimulation of [ 35 S]-GTPgS binding; blocking the inhibition of forskolin-stimulated adenylate cyclase activity in transfected human embryonic kidney (HEK293) and Chinese hamster ovary (CHO) cells; blocking dopamine-induced inhibition of Ca 2+ currents in transfected GH4C1 pituitary cells; inhibiting D 4 activation of cloned G protein-coupled inwardly rectifying K + channels; and antagonizing dopamine-induced stimulation of extracellular acidification in transfected cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t 1/2 2.1-2.8 hours) in both rat and monkey, and excellent brain penetration with high brain to plasma ratios in rat . Following oral administration to squirrel monkeys, L745870 (10 mg/kg p.o.) induces mild sedation and extrapyramidal motor symptoms, notably bradykinesia, became apparent at 30 mg/kg. Lower doses of L-745870 has no observable behavioural effects in monkeys . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Isomeric SMILES | C1CN(CCN1CC2=CNC3=C2C=CC=N3)C4=CC=C(C=C4)Cl.Cl |
|---|---|
| Alternate CAS | 1173023-36-3 |
| PubChem CID | 11957618 |
| Molecular Weight | 363.28 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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