JNJ-18038683 citrate
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MedKoo CAT#: 555803

CAS#: 851376-05-1 (citrate)

Description: JNJ-18038683 is a 5-HT7 receptor antagonist which has been shown to be effective in models of depression and to increase the latency to rapid eye movement (REM) sleep and decrease REM duration. JNJ-18038683 enhanced serotonin transmission, antidepressant-like behavior, and REM sleep suppression induced by citalopram in rodents.


Chemical Structure

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JNJ-18038683 citrate
CAS# 851376-05-1 (citrate)

Theoretical Analysis

MedKoo Cat#: 555803
Name: JNJ-18038683 citrate
CAS#: 851376-05-1 (citrate)
Chemical Formula: C26H28ClN3O7
Exact Mass:
Molecular Weight: 529.974
Elemental Analysis: C, 58.92; H, 5.33; Cl, 6.69; N, 7.93; O, 21.13

Price and Availability

Size Price Availability Quantity
5.0mg USD 95.0 Ready to ship
10.0mg USD 170.0 Ready to ship
25.0mg USD 350.0 Ready to ship
50.0mg USD 550.0 Ready to ship
100.0mg USD 950.0 Ready to ship
200.0mg USD 1650.0 Ready to ship
500.0mg USD 2950.0 Ready to ship
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Related CAS #: 851376-05-1 (citrate)   851373-91-6 (free base)    

Synonym: JNJ-18038683 citrate; JNJ-18038683; JNJ 18038683; JNJ18038683.

IUPAC/Chemical Name: 3-(4-chlorophenyl)-1-(phenylmethyl)-5,6,7,8-tetrahydro-4H-pyrazolo[5,4-d]azepine citrate

InChi Key: DIQZMBPDLFAJLK-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H20ClN3.C6H8O7/c21-17-8-6-16(7-9-17)20-18-10-12-22-13-11-19(18)24(23-20)14-15-4-2-1-3-5-15;7-3(8)1-6(13,5(11)12)2-4(9)10/h1-9,22H,10-14H2;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)

SMILES Code: ClC1=CC=C(C2=NN(CC3=CC=CC=C3)C4=C2CCNCC4)C=C1.OC(C(O)=O)(CC(O)=O)CC(O)=O

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: JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist.
In vitro activity: TBD
In vivo activity: This study then tested whether the 5-HT7 receptor antagonist JNJ-18038683 would attenuate the phase advance of wheel running locomotor activity elicited by the 5-HT1A/7 receptor agonist 8-OH-DPAT. Administration of the vehicle for JNJ-18038683 followed by 8-OH-DPAT resulted in a robust phase advance of the onset of locomotor activity during constant dark conditions (37.0 ± 6.3 min, F(3,58) = 18.49 p < 0.0001, one-way ANOVA, Tukey’s post hoc analysis) when compared to the other three treatment groups (Vehicle + Vehicle: −5.4 ± 4.1 min, JNJ-18038683 + Vehicle −0.9 ± 3.6 min, JNJ-18038683 + 8-OH-DPAT: −2.7 ± 3.0 min) (Figure 1). Comparable to what had been measured during the generation of the phase response curve, the administration of JNJ-18038683 in conjunction with the vehicle for 8-OH-DPAT did not produce any phase shift at CT 6. The administration of the 5-HT7 receptor antagonist JNJ-18038683 completely blocked the phase advance produced by 8-OH-DPAT (Figure 1). Reference: Front Behav Neurosci. 2014; 8: 453. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4295543/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 200.0 377.38

Preparing Stock Solutions

The following data is based on the product molecular weight 529.974 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.

Recalculate based on batch purity %
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. Shelton J, Yun S, Losee Olson S, Turek F, Bonaventure P, Dvorak C, Lovenberg T, Dugovic C. Selective pharmacological blockade of the 5-HT7 receptor attenuates light and 8-OH-DPAT induced phase shifts of mouse circadian wheel running activity. Front Behav Neurosci. 2015 Jan 15;8:453. doi: 10.3389/fnbeh.2014.00453. PMID: 25642174; PMCID: PMC4295543.
In vitro protocol: TBD
In vivo protocol: 1. Shelton J, Yun S, Losee Olson S, Turek F, Bonaventure P, Dvorak C, Lovenberg T, Dugovic C. Selective pharmacological blockade of the 5-HT7 receptor attenuates light and 8-OH-DPAT induced phase shifts of mouse circadian wheel running activity. Front Behav Neurosci. 2015 Jan 15;8:453. doi: 10.3389/fnbeh.2014.00453. PMID: 25642174; PMCID: PMC4295543.

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1: Shelton J, Yun S, Losee Olson S, Turek F, Bonaventure P, Dvorak C, Lovenberg T, Dugovic C. Selective pharmacological blockade of the 5-HT7 receptor attenuates light and 8-OH-DPAT induced phase shifts of mouse circadian wheel running activity. Front Behav Neurosci. 2015 Jan 15;8:453. doi: 10.3389/fnbeh.2014.00453. PMID: 25642174; PMCID: PMC4295543.

2: Bonaventure P, Dugovic C, Kramer M, De Boer P, Singh J, Wilson S, Bertelsen K, Di J, Shelton J, Aluisio L, Dvorak L, Fraser I, Lord B, Nepomuceno D, Ahnaou A, Drinkenburg W, Chai W, Dvorak C, Sands S, Carruthers N, Lovenberg TW. Translational evaluation of JNJ-18038683, a 5-hydroxytryptamine type 7 receptor antagonist, on rapid eye movement sleep and in major depressive disorder. J Pharmacol Exp Ther. 2012 Aug;342(2):429-40. doi: 10.1124/jpet.112.193995. Epub 2012 May 8. PMID: 22570363.



Additional Information

Recent reports have illustrated a reciprocal relationship between circadian rhythm disruption and mood disorders. The 5-HT7 receptor may provide a crucial link between the two sides of this equation since the receptor plays a critical role in sleep, depression, and circadian rhythm regulation.