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
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
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.
Biological target:
JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist.
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/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
200.0 |
377.38 |
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
529.97
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. 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 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.
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.
