PD-168077 maleate | CAS#630117-19-0 | D4 agonist

MedKoo Cat#: 555683 | Name: PD-168077 maleate

Featured

Description:

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

PD168077 is a potent D4 dopamine receptor agonist (Ki = 8.7 nM) with > 400-fold selectivity over D2 and > 300-fold selectivity versus D3 subtypes respectively. PD-168077 induces synaptic translocation of CaMK II to postsynaptic sites in cultured prefrontal cortical neurons. Centrally active in vivo.

Chemical Structure

PD-168077 maleate

CAS#630117-19-0 (maleate)

Theoretical Analysis

MedKoo Cat#: 555683

Name: PD-168077 maleate

CAS#: 630117-19-0 (maleate)

Chemical Formula: C24H26N4O5

Exact Mass: 0.0000

Molecular Weight: 450.50

Elemental Analysis: C, 63.99; H, 5.82; N, 12.44; O, 17.76

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 550.00
50mg	USD 1,175.00

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

190383-31-4 (free base) 630117-19-0 (maleate)

Synonym

PD168077; PD-168077; PD 168077; PD-168,077; PD 168,077; PD168,077; PD-168077 maleate;

IUPAC/Chemical Name

N-((4-(2-cyanophenyl)piperazin-1-yl)methyl)-3-methylbenzamide maleate

InChi Key

NAEUGRPISCANHO-BTJKTKAUSA-N

InChi Code

InChI=1S/C20H22N4O.C4H4O4/c1-16-5-4-7-17(13-16)20(25)22-15-23-9-11-24(12-10-23)19-8-3-2-6-18(19)14-21;5-3(6)1-2-4(7)8/h2-8,13H,9-12,15H2,1H3,(H,22,25);1-2H,(H,5,6)(H,7,8)/b;2-1-

SMILES Code

OC(=O)\C=C/C(O)=O.CC1=CC(=CC=C1)C(=O)NCN1CCN(CC1)C1=C(C=CC=C1)C#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:

PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.

In vitro activity:

The present study established a cell model of hyperglycemia-induced endothelial dysfunction by treating human umbilical vein endothelial cells (HUVEC) with high glucose. Pre-treatment with PD168077, a specific D4 receptor agonist, greatly improved endothelial cell viability and decreased apoptosis. Reference: Biochem Biophys Res Commun. 2019 Oct 20;518(3):554-559. https://pubmed.ncbi.nlm.nih.gov/31447121/

In vivo activity:

NKA activity, nitric oxide (NO) and cyclic guanosine monophosphate (cGMP) levels were measured in RPT cells treated with the D4 receptor agonist PD168077 and/or the D4 receptor antagonist L745870, the NO synthase inhibitor NG-nitro-L-arginine-methyl ester (L-NAME) or the soluble guanylyl cyclase inhibitor 1H-[1,2,4] oxadiazolo-[4,3-a] quinoxalin-1-one (ODQ). Total D4 receptor expression and its expression in the plasma membrane were investigated by immunoblotting in RPT cells from Wistar-Kyoto (WKY) rats and spontaneously hypertensive rats (SHRs). Activation of D4 receptors with PD168077, inhibited NKA activity in RPT cells from WKY rats in a concentration- and time-dependent manner. Reference: Cardiol Discov. 2023 Mar;3(1):24-29. https://pubmed.ncbi.nlm.nih.gov/36969984/

	Solvent	mg/mL	mM
Solubility
	DMSO	97.5	216.48

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 450.50 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. Wang H, Yao Y, Liu J, Cao Y, Si C, Zheng R, Zeng C, Guan H, Li L. Dopamine D4 receptor protected against hyperglycemia-induced endothelial dysfunction via PI3K /eNOS pathway. Biochem Biophys Res Commun. 2019 Oct 20;518(3):554-559. doi: 10.1016/j.bbrc.2019.08.080. Epub 2019 Aug 22. PMID: 31447121. 2. Guo F, Zhao J, Zhao D, Wang J, Wang X, Feng Z, Vreugdenhil M, Lu C. Dopamine D4 receptor activation restores CA1 LTP in hippocampal slices from aged mice. Aging Cell. 2017 Dec;16(6):1323-1333. doi: 10.1111/acel.12666. Epub 2017 Oct 3. PMID: 28975698; PMCID: PMC5676052. 3. He D, Ren H, Wang H, Jose PA, Zeng C, Xia T, Yang J. Effect of D4 Dopamine Receptor on Na+-K+-ATPase Activity in Renal Proximal Tubule Cells. Cardiol Discov. 2023 Mar;3(1):24-29. doi: 10.1097/CD9.0000000000000076. Epub 2022 Oct 14. PMID: 36969984; PMCID: PMC10030170.

In vitro protocol:

In vivo protocol:

1. He D, Ren H, Wang H, Jose PA, Zeng C, Xia T, Yang J. Effect of D4 Dopamine Receptor on Na+-K+-ATPase Activity in Renal Proximal Tubule Cells. Cardiol Discov. 2023 Mar;3(1):24-29. doi: 10.1097/CD9.0000000000000076. Epub 2022 Oct 14. PMID: 36969984; PMCID: PMC10030170.

1: Navakkode S, Chew KCM, Tay SJN, Lin Q, Behnisch T, Soong TW. Bidirectional modulation of hippocampal synaptic plasticity by Dopaminergic D4-receptors in the CA1 area of hippocampus. Sci Rep. 2017 Nov 14;7(1):15571. doi: 10.1038/s41598-017-15917-1. PubMed PMID: 29138490; PubMed Central PMCID: PMC5686203. 2: Guo F, Zhao J, Zhao D, Wang J, Wang X, Feng Z, Vreugdenhil M, Lu C. Dopamine D4 receptor activation restores CA1 LTP in hippocampal slices from aged mice. Aging Cell. 2017 Dec;16(6):1323-1333. doi: 10.1111/acel.12666. Epub 2017 Oct 3. PubMed PMID: 28975698; PubMed Central PMCID: PMC5676052. 3: Wang YL, Wang JG, Guo FL, Gao XH, Zhao DD, Zhang L, Wang JZ, Lu CB. Selective dopamine receptor 4 activation mediates the hippocampal neuronal calcium response via IP(3) and ryanodine receptors. Brain Res. 2017 Sep 1;1670:1-5. doi: 10.1016/j.brainres.2017.05.012. Epub 2017 May 12. PubMed PMID: 28506554. 4: Miyauchi M, Neugebauer NM, Meltzer HY. Dopamine D(4) receptor stimulation contributes to novel object recognition: Relevance to cognitive impairment in schizophrenia. J Psychopharmacol. 2017 Apr;31(4):442-452. doi: 10.1177/0269881117693746. Epub 2017 Feb 1. PubMed PMID: 28347261. 5: Cocker PJ, Lin MY, Barrus MM, Le Foll B, Winstanley CA. The agranular and granular insula differentially contribute to gambling-like behavior on a rat slot machine task: effects of inactivation and local infusion of a dopamine D4 agonist on reward expectancy. Psychopharmacology (Berl). 2016 Sep;233(17):3135-47. doi: 10.1007/s00213-016-4355-1. Epub 2016 Jul 14. PubMed PMID: 27417550. 6: Cocker PJ, Vonder Haar C, Winstanley CA. Elucidating the role of D4 receptors in mediating attributions of salience to incentive stimuli on Pavlovian conditioned approach and conditioned reinforcement paradigms. Behav Brain Res. 2016 Oct 1;312:55-63. doi: 10.1016/j.bbr.2016.06.007. Epub 2016 Jun 6. PubMed PMID: 27275521. 7: Rivera A, Gago B, Suárez-Boomgaard D, Yoshitake T, Roales-Buján R, Valderrama-Carvajal A, Bilbao A, Medina-Luque J, Díaz-Cabiale Z, Craenenbroeck KV, Borroto-Escuela DO, Kehr J, Rodríguez de Fonseca F, Santín L, de la Calle A, Fuxe K. Dopamine D(4) receptor stimulation prevents nigrostriatal dopamine pathway activation by morphine: relevance for drug addiction. Addict Biol. 2017 Sep;22(5):1232-1245. doi: 10.1111/adb.12407. Epub 2016 May 22. PubMed PMID: 27212105. 8: Zhang Y, Ren H, Lu X, He D, Han Y, Wang H, Zeng C, Shi W. Inhibition of D4 Dopamine Receptors on Insulin Receptor Expression and Effect in Renal Proximal Tubule Cells. J Am Heart Assoc. 2016 Apr 22;5(4). pii: e002448. doi: 10.1161/JAHA.115.002448. PubMed PMID: 27107134; PubMed Central PMCID: PMC4843542. 9: Cocker PJ, Hosking JG, Murch WS, Clark L, Winstanley CA. Activation of dopamine D4 receptors within the anterior cingulate cortex enhances the erroneous expectation of reward on a rat slot machine task. Neuropharmacology. 2016 Jun;105:186-195. doi: 10.1016/j.neuropharm.2016.01.019. Epub 2016 Jan 15. PubMed PMID: 26775821. 10: Kotani M, Kiyoshi A, Murai T, Nakako T, Matsumoto K, Matsumoto A, Ikejiri M, Ogi Y, Ikeda K. The dopamine D1 receptor agonist SKF-82958 effectively increases eye blinking count in common marmosets. Behav Brain Res. 2016 Mar 1;300:25-30. doi: 10.1016/j.bbr.2015.11.028. Epub 2015 Dec 7. PubMed PMID: 26675887. 11: Yu C, Chen J, Guan W, Han Y, Wang WE, Wang X, Wang H, Jose PA, Zeng C. Activation of the D4 dopamine receptor attenuates proliferation and migration of vascular smooth muscle cells through downregulation of AT1a receptor expression. Hypertens Res. 2015 Sep;38(9):588-96. doi: 10.1038/hr.2015.48. Epub 2015 Apr 2. PubMed PMID: 25832920; PubMed Central PMCID: PMC6400214. 12: Oh JH, Lee DK, Shim YB, Ryu IS, Seo SY, Kim J, Yang JH, Cho HW, Choe ES. Dopamine D4 receptors linked to protein kinase G are required for changes in dopamine release followed by locomotor activity after repeated cocaine administration. Exp Brain Res. 2015 May;233(5):1511-8. doi: 10.1007/s00221-015-4228-6. Epub 2015 Feb 22. PubMed PMID: 25702161. 13: Chiang FK, Cheng RK, Liao RM. Differential effects of dopamine receptor subtype-specific agonists with respect to operant behavior maintained on a differential reinforcement of low-rate responding (DRL) schedule. Pharmacol Biochem Behav. 2015 Mar;130:67-76. doi: 10.1016/j.pbb.2015.01.002. Epub 2015 Jan 10. PubMed PMID: 25584855. 14: Li SB, Du D, Hasan MT, Köhr G. D4 Receptor Activation Differentially Modulates Hippocampal Basal and Apical Dendritic Synapses in Freely Moving Mice. Cereb Cortex. 2016 Feb;26(2):647-55. doi: 10.1093/cercor/bhu229. Epub 2014 Sep 30. PubMed PMID: 25270308. 15: Yu C, Wang Z, Han Y, Liu Y, Wang WE, Chen C, Wang H, Jose PA, Zeng C. Dopamine D₄ receptors inhibit proliferation and migration of vascular smooth muscle cells induced by insulin via down-regulation of insulin receptor expression. Cardiovasc Diabetol. 2014 Jun 2;13:97. doi: 10.1186/1475-2840-13-97. PubMed PMID: 24888351; PubMed Central PMCID: PMC4078019. 16: Tejas-Juárez JG, Cruz-Martínez AM, López-Alonso VE, García-Iglesias B, Mancilla-Díaz JM, Florán-Garduño B, Escartín-Pérez RE. Stimulation of dopamine D4 receptors in the paraventricular nucleus of the hypothalamus of male rats induces hyperphagia: involvement of glutamate. Physiol Behav. 2014 Jun 22;133:272-81. doi: 10.1016/j.physbeh.2014.04.040. Epub 2014 May 5. PubMed PMID: 24805978. 17: Jackson CR, Capozzi M, Dai H, McMahon DG. Circadian perinatal photoperiod has enduring effects on retinal dopamine and visual function. J Neurosci. 2014 Mar 26;34(13):4627-33. doi: 10.1523/JNEUROSCI.4887-13.2014. PubMed PMID: 24672008; PubMed Central PMCID: PMC3965786. 18: Cocker PJ, Le Foll B, Rogers RD, Winstanley CA. A selective role for dopamine D₄ receptors in modulating reward expectancy in a rodent slot machine task. Biol Psychiatry. 2014 May 15;75(10):817-24. doi: 10.1016/j.biopsych.2013.08.026. Epub 2013 Oct 4. PubMed PMID: 24094512. 19: Niijima-Yaoita F, Tsuchiya M, Saito H, Nagasawa Y, Murai S, Arai Y, Nakagawasai O, Nemoto W, Tadano T, Tan-No K. Influence of a long-term powdered diet on the social interaction test and dopaminergic systems in mice. Neurochem Int. 2013 Oct;63(4):309-15. doi: 10.1016/j.neuint.2013.07.004. Epub 2013 Jul 16. PubMed PMID: 23871718. 20: Sanna F, Corda MG, Melis MR, Piludu MA, Löber S, Hübner H, Gmeiner P, Argiolas A, Giorgi O. Dopamine agonist-induced penile erection and yawning: a comparative study in outbred Roman high- and low-avoidance rats. Pharmacol Biochem Behav. 2013 Aug;109:59-66. doi: 10.1016/j.pbb.2013.05.002. Epub 2013 May 8. PubMed PMID: 23664901.