866021-03-6
Chemical Structure
L-745870 trihydrochloride
- CAS No.: 866021-03-6
- Formula:C18H22Cl4N4
- Molecular Weight:436.21
IUPAC Name: 3-((4-(4-chlorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo[2,3-b]pyridine trihydrochloride
InChIKey: KJSOYZLYCFYXFC-UHFFFAOYSA-N
SMILES: ClC(C=C1)=CC=C1N(CC2)CCN2CC3=CNC4=NC=CC=C43.Cl.Cl.Cl
Biological Activity: L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors[1][2][3].
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L-745870 trihydrochloride | L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors. | |||||||||||||||||||||
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- [1]. Bristow LJ, et al. Schizophrenia and L-745,870, a novel dopamine D4 receptor antagonist. Trends Pharmacol Sci. 1997 Jun;18(6):186-8. [Content Brief]
- [2]. Patel S, et al. Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor. J Pharmacol Exp Ther. 1997 Nov;283(2):636-47. [Content Brief]
- [3]. Kulagowski JJ, et al. 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. J Med Chem. 1996 May 10;39(10):1941-2. [Content Brief]
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