L-745870 hydrochloride | CAS#1173023-36-3 | D4 receptor antagonist

MedKoo Cat#: 559121 | Name: L-745870 hydrochloride

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist. L-745870 hydrochloride has excellent brain penetration.

Chemical Structure

L-745870 hydrochloride

CAS#1173023-36-3 (HCl)

Theoretical Analysis

MedKoo Cat#: 559121

Name: L-745870 hydrochloride

CAS#: 1173023-36-3 (HCl)

Chemical Formula: C18H20Cl2N4

Exact Mass: 362.1065

Molecular Weight: 363.29

Elemental Analysis: C, 59.51; H, 5.55; Cl, 19.52; N, 15.42

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 340.00	2 Weeks
50mg	USD 850.00	2 Weeks

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Related CAS #

866021-03-6 (3HCl) 158985-00-3 (free base) 1173023-36-3 (HCl)

Synonym

L-745870 hydrochloride; L-745870; L 745870; L745870;

IUPAC/Chemical Name

3-((4-(4-chlorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo[2,3-b]pyridine hydrochloride

InChi Key

GFFJYISJZJIKAF-UHFFFAOYSA-N

InChi Code

InChI=1S/C18H19ClN4.ClH/c19-15-3-5-16(6-4-15)23-10-8-22(9-11-23)13-14-12-21-18-17(14)2-1-7-20-18;/h1-7,12H,8-11,13H2,(H,20,21);1H

SMILES Code

GFFJYISJZJIKAF-UHFFFAOYSA-N

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist.

In vitro activity:

The D(3) selective antagonist S33084 and D(4)-selective antagonist L-745870 were highly selective for D(3) and D(4) receptors with K(b) of 0.7 and 0.1 nM, respectively. Reference: Biochem Pharmacol. 2004 Aug 15;68(4):761-72. https://pubmed.ncbi.nlm.nih.gov/15276084/

In vivo activity:

In another experiment where male rats were given full access to a receptive female, a D(4) (L-745870) but not D(2) or D(3) antagonist (L-741626; nafadotride) inhibited penile erection (intromission), and this was correlated with SON magnocellular oxytocin neuron activation. Reference: Eur J Neurosci. 2009 Dec 3;30(11):2151-64. https://pubmed.ncbi.nlm.nih.gov/20128851/

Preparing Stock Solutions

The following data is based on the product molecular weight 363.29 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Moreland RB, Nakane M, Donnelly-Roberts DL, Miller LN, Chang R, Uchic ME, Terranova MA, Gubbins EJ, Helfrich RJ, Namovic MT, El-Kouhen OF, Masters JN, Brioni JD. Comparative pharmacology of human dopamine D(2)-like receptor stable cell lines coupled to calcium flux through Galpha(qo5). Biochem Pharmacol. 2004 Aug 15;68(4):761-72. doi: 10.1016/j.bcp.2004.05.019. PMID: 15276084. 2. Baskerville TA, Allard J, Wayman C, Douglas AJ. Dopamine-oxytocin interactions in penile erection. Eur J Neurosci. 2009 Dec 3;30(11):2151-64. doi: 10.1111/j.1460-9568.2009.06999.x. Epub 2009 Nov 25. PMID: 20128851. 3. Jackson CR, Chaurasia SS, Zhou H, Haque R, Storm DR, Iuvone PM. Essential roles of dopamine D4 receptors and the type 1 adenylyl cyclase in photic control of cyclic AMP in photoreceptor cells. J Neurochem. 2009 Apr;109(1):148-57. doi: 10.1111/j.1471-4159.2009.05920.x. Epub 2009 Jan 22. PMID: 19166506; PMCID: PMC2727872.

In vitro protocol:

In vivo protocol:

1. Baskerville TA, Allard J, Wayman C, Douglas AJ. Dopamine-oxytocin interactions in penile erection. Eur J Neurosci. 2009 Dec 3;30(11):2151-64. doi: 10.1111/j.1460-9568.2009.06999.x. Epub 2009 Nov 25. PMID: 20128851. 2. Jackson CR, Chaurasia SS, Zhou H, Haque R, Storm DR, Iuvone PM. Essential roles of dopamine D4 receptors and the type 1 adenylyl cyclase in photic control of cyclic AMP in photoreceptor cells. J Neurochem. 2009 Apr;109(1):148-57. doi: 10.1111/j.1471-4159.2009.05920.x. Epub 2009 Jan 22. PMID: 19166506; PMCID: PMC2727872.

1: Bristow LJ, Kramer MS, Kulagowski J, Patel S, Ragan CI, Seabrook GR. Schizophrenia and L-745,870, a novel dopamine D4 receptor antagonist. Trends Pharmacol Sci. 1997;18(6):186‐188. doi:10.1016/s0165-6147(97)01066-3. 2: Patel S, Freedman S, Chapman KL, et al. Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor. J Pharmacol Exp Ther. 1997;283(2):636‐647. 3: Kulagowski JJ, Broughton HB, Curtis NR, 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;39(10):1941‐1942. doi:10.1021/jm9600712.