1: Fedotova IuO, Pivina SG, Akulova VK, Ordian NÉ. [Pecularities for action of combined administration of NAN-190 and ketanserine with low dose of 17β-estradiol on depression-like behavior in prenatally stressed ovariectomized rats]. Ross Fiziol Zh Im I M Sechenova. 2015 Jan;101(1):35-43. Russian. PMID: 25868324. 2: Fedotova IuO, Sapronov NS. [Co-administration of NAN-190 with low dose of testosterone propionate improves passive avoidance performance in rats with androgen deficiency]. Eksp Klin Farmakol. 2013;76(12):15-9. Russian. PMID: 24605422. 3: Fedotova IuO, Pivina SG, Ordian NÉ. [Analysis of 8-OH-DPAT and NAN-190 effects in young prenatally stressed rats under experimental estrogen deficiency conditions]. Eksp Klin Farmakol. 2012;75(7):11-4. Russian. PMID: 23025046. 4: Kowalski P, Jaśkowska J. An efficient synthesis of aripiprazole, buspirone and NAN-190 by the reductive alkylation of amines procedure. Arch Pharm (Weinheim). 2012 Jan;345(1):81-5. doi: 10.1002/ardp.201100112. Epub 2011 Oct 5. PMID: 22234973. 5: Fedotova YO, Ordyan NE. Effects of 8-OH-DPAT and NAN-190 on anxious- depressive-like behavior of female rats during the estrous cycle. Bull Exp Biol Med. 2010 Dec;150(2):165-7. English, Russian. doi: 10.1007/s10517-010-1094-x. PMID: 21246079. 6: Foong JP, Bornstein JC. 5-HT antagonists NAN-190 and SB 269970 block alpha2-adrenoceptors in the guinea pig. Neuroreport. 2009 Feb 18;20(3):325-30. doi: 10.1097/WNR.0b013e3283232caa. PMID: 19190523. 7: Kessler EJ, Sprouse J, Harrington ME. NAN-190 potentiates the circadian response to light and speeds re-entrainment to advanced light cycles. Neuroscience. 2008 Jul 17;154(4):1187-94. doi: 10.1016/j.neuroscience.2008.04.054. Epub 2008 May 6. PMID: 18538936; PMCID: PMC2637398. 8: Sterniczuk R, Stepkowski A, Jones M, Antle MC. Enhancement of photic shifts with the 5-HT1A mixed agonist/antagonist NAN-190: intra-suprachiasmatic nucleus pathway. Neuroscience. 2008 May 15;153(3):571-80. doi: 10.1016/j.neuroscience.2008.02.062. Epub 2008 Mar 6. PMID: 18406538. 9: Schneider AM, Simson PE. NAN-190 potentiates the impairment of retention produced by swim stress. Pharmacol Biochem Behav. 2007 May;87(1):73-80. doi: 10.1016/j.pbb.2007.04.002. Epub 2007 Apr 11. PMID: 17490739. 10: Sapronov NS, Fedotova YO, Losev NA. Combined administration of NAN-190 and 17beta-estradiol abolishes the amnesic effect of scopolamine in middle-aged ovariectomized rats. Bull Exp Biol Med. 2006 Jul;142(1):80-2. English, Russian. doi: 10.1007/s10517-006-0297-7. PMID: 17369909. 11: Paluchowska MH, Bugno R, Charakchieva-Minol S, Bojarski AJ, Tatarczyńska E, Chojnacka-Wójcik E. Conformational restriction in novel NAN-190 and MP3022 analogs and their 5-HT(1A) receptor activity. Arch Pharm (Weinheim). 2006 Sep;339(9):498-506. doi: 10.1002/ardp.200600009. PMID: 16941730. 12: Djavadian RL, Wielkopolska E, Turlejski K. Postnatal treatment with NAN-190 but not with 5-HT1A receptor agonists retards growth of the rat brain. Int J Dev Neurosci. 2005 Aug;23(5):485-93. doi: 10.1016/j.ijdevneu.2005.02.001. PMID: 16026684. 13: Ginawi OT, Al-Majed AA, Al-Suwailem AK. NAN-190, a possible specific antagonist for methamphetamine. Regul Toxicol Pharmacol. 2005 Mar;41(2):122-7. doi: 10.1016/j.yrtph.2004.10.005. Epub 2004 Dec 19. PMID: 15698535. 14: Wesołowska A, Borycz J, Paluchowska MH, Chojnacka-Wójcik E. Pharmacological analysis of the hypothermic effects of NAN-190 and its analogs, postsynaptic 5-HT1A receptor antagonists, in mice. Pol J Pharmacol. 2002 Jul-Aug;54(4):391-9. PMID: 12523493. 15: Paluchowska MH, Mokrosz MJ, Bojarski A, Wesołowska A, Borycz J, Charakchieva-Minol S, Chojnacka-Wójcik E. On the bioactive conformation of NAN-190 (1) and MP3022 (2), 5-HT(1A) receptor antagonists. J Med Chem. 1999 Dec 2;42(24):4952-60. doi: 10.1021/jm991045h. PMID: 10585205. 16: Cao BJ, Rodgers RJ. Influence of 5-HT1A receptor antagonism on plus-maze behaviour in mice. II. WAY 100635, SDZ 216-525 and NAN-190. Pharmacol Biochem Behav. 1997 Oct;58(2):593-603. doi: 10.1016/s0091-3057(97)00279-7. PMID: 9300624. 17: Belcheva I, Belcheva S, Petkov VV, Hadjiivanova C, Petkov VD. Behavorial responses to the 5-HT1A receptor antagonist NAN190 injected into rat CA1 hippocampal area. Gen Pharmacol. 1997 Mar;28(3):435-41. doi: 10.1016/s0306-3623(96)00185-1. PMID: 9068987. 18: Sharp T, Umbers V, Hjorth S. The role of 5-HT1A autoreceptors and alpha 1-adrenoceptors in the inhibition of 5-HT release--II NAN-190 and SDZ 216-525. Neuropharmacology. 1996 Jun;35(6):735-41. doi: 10.1016/0028-3908(96)84645-4. PMID: 8887982. 19: Dalpiaz A, Ferretti V, Gilli P, Bertolasi V. Stereochemistry of serotonin receptor ligands from crystallographic data. Crystal structures of NAN-190.HBr, 1-phenylbiguanide, MDL 72222 and mianserin.HCl and selectivity criteria towards 5-HT1, 5-HT2, and 5-HT3 receptor subtypes. Acta Crystallogr B. 1996 Jun 1;52 ( Pt 3):509-18. doi: 10.1107/s0108768195014765. PMID: 8767764. 20: Neckelmann D, Bjørkum AA, Bjorvatn B, Ursin R. Sleep and EEG power spectrum effects of the 5-HT1A antagonist NAN-190 alone and in combination with citalopram. Behav Brain Res. 1996 Feb;75(1-2):159-68. doi: 10.1016/0166-4328(96)00204-5. PMID: 8800653.

C23H27N3O3

393.487

393.21

C, 70.21; H, 6.92; N, 10.68; O, 12.20

102392-05-2

NAN-190 hydrobromide;115338-32-4

O=C1N(C(C2=C1C=CC=C2)=O)CCCCN3CCN(CC3)C4=CC=CC=C4OC

SJDOMIRMMUGQQK-UHFFFAOYSA-N

1S/C23H27N3O3/c1-29-21-11-5-4-10-20(21)25-16-14-24(15-17-25)12-6-7-13-26-22(27)18-8-2-3-9-19(18)23(26)28/h2-5,8-11H,6-7,12-17H2,1H3

1H-Isoindole-1,3(2H)-dione, 2-(4-(4-(2-methoxyphenyl)-1-piperazinyl)butyl)-

NAN190 free base; NAN-190; NAN 190; NAN190

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

---

Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

View More

Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

---

Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

View More

Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

---

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

---

 (Please use freshly prepared in vivo formulations for optimal results.)