WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 559121
CAS#: 1173023-36-3 (HCl)
Description: L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist. L-745870 hydrochloride has excellent brain penetration.
MedKoo Cat#: 559121
Name: L-745870 hydrochloride
CAS#: 1173023-36-3 (HCl)
Chemical Formula: C18H20Cl2N4
Exact Mass: 362.1065
Molecular Weight: 363.286
Elemental Analysis: C, 59.51; H, 5.55; Cl, 19.52; N, 15.42
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
| 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/ |
The following data is based on the product molecular weight 363.286 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: | 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. |
| 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.
