Robalzotan hydrochloride (Synonyms: NAD-299 hydrochloride)

Cat. No.: HY-10351A Purity: 99.5%: FAQs
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Robalzotan hydrochloride (NAD-299 hydrochloride) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan hydrochloride increases the firing rate of 5-HT cells. Robalzotan hydrochloride induces 5-HT1A receptor occupancy. Robalzotan hydrochloride has the potential for the research of a cholinergic deficit in the central -nervous system.

For research use only. We do not sell to patients.

Robalzotan hydrochloride Chemical Structure

CAS No. : 184674-99-5

Size	Price	Stock
5 mg	USD 315	Ask For Quote & Lead Time
10 mg	USD 504	Ask For Quote & Lead Time

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Other Forms of Robalzotan hydrochloride:

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5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

5-HT_1A Receptor

In Vivo

Robalzotan hydrochloride (1-100 µg/kg; i.v.) significantly increases the activity of such neurons at 5 µg/kg in rats, and reverses the acute inhibitory effect of citalopram (HY-121203) (300 µg/kg i.v.) or paroxetine (HY-122272) (100 µg/kg, i.v.) on the activity of 5-HT neurons in the dorsal raphe nucleus in rats^[1].
Robalzotan hydrochloride (5, 50 µg/kg; i.v.) increases the firing rate of the 5-HT cells^[1].
Robalzotan hydrochloride (2-100 µg/kg; i.v.) occupies 5-HT1A receptors in a dose-dependent in monkeys^[2].
Robalzotan hydrochloride (0.3; 1 and 3 µmol/kg s.c) causes a dose-dependent increase of extracellular ACh levels in the rat FC^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	300-600 g, male Sprague-Dawley rats (5-HT cells)^[1]
Dosage:	1, 5, 12.5, 25, 50, 100 µg/kg
Administration:	I.v.
Result:	Significantly increased the activity of such neurons at 5 µg/kg, increasing doses of robalzotan 5-100 µg/kg or 50-400 mg/kg did not further affect the firing rate of 5-HT neurons.

Animal Model:	3-4 kg, cynomolgus monkeys^[2]
Dosage:	2, 10, 20, 100 µg/kg
Administration:	I.v.
Result:	Occupied 5-HT1A receptors in a dose-dependent and saturable manner and he highest 5-HT1A receptor occupancy (70-80%) was attained after 100 μg/kg.

Molecular Weight

354.85

Formula

C₁₈H₂₄ClFN₂O₂

CAS No.

184674-99-5

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C2C[C@@H](N(C3CCC3)C4CCC4)COC2=C(F)C=C1)N.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (281.81 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8181 mL	14.0905 mL	28.1809 mL
5 mM	0.5636 mL	2.8181 mL	5.6362 mL
10 mM	0.2818 mL	1.4090 mL	2.8181 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.5%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (253 KB) Elemental Analysis Report (111 KB)

Handling Instructions (2659 KB)

References

[1]. Arborelius L, et al. The 5-HT(1A) receptor antagonist robalzotan completely reverses citalopram-induced inhibition of serotonergic cell firing. Eur J Pharmacol. 1999 Oct 8;382(2):133-8. [Content Brief]

[2]. Farde L, et al. PET-Determination of robalzotan (NAD-299) induced 5-HT(1A) receptor occupancy in the monkey brain. Neuropsychopharmacology. 2000 Apr;22(4):422-9. [Content Brief]

[3]. Hu, Xiao Jing, et al. Modulation of acetylcholine release by serotonergic 5-HT1A and 5-HT1B receptors : a microdialysis study in the awake rat. 2007.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8181 mL	14.0905 mL	28.1809 mL	70.4523 mL
	5 mM	0.5636 mL	2.8181 mL	5.6362 mL	14.0905 mL
	10 mM	0.2818 mL	1.4090 mL	2.8181 mL	7.0452 mL
	15 mM	0.1879 mL	0.9394 mL	1.8787 mL	4.6968 mL
	20 mM	0.1409 mL	0.7045 mL	1.4090 mL	3.5226 mL
	25 mM	0.1127 mL	0.5636 mL	1.1272 mL	2.8181 mL
	30 mM	0.0939 mL	0.4697 mL	0.9394 mL	2.3484 mL
	40 mM	0.0705 mL	0.3523 mL	0.7045 mL	1.7613 mL
	50 mM	0.0564 mL	0.2818 mL	0.5636 mL	1.4090 mL
	60 mM	0.0470 mL	0.2348 mL	0.4697 mL	1.1742 mL
	80 mM	0.0352 mL	0.1761 mL	0.3523 mL	0.8807 mL
	100 mM	0.0282 mL	0.1409 mL	0.2818 mL	0.7045 mL

Robalzotan hydrochloride Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Robalzotan184674-99-5NAD-2995-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorfiring rateneurons5-HT cellsACh levelscholinergic deficitInhibitorinhibitorinhibit

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