1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor 5-HT Receptor
  3. Spiroxatrine

Spiroxatrine  (Synonyms: R 5188)

Cat. No.: HY-12706 Purity: 99.18%
COA Handling Instructions

Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α, 5-HT1β and 5-HT2, respectively. Spiroxatrine (R 5188) has a sedative effect.

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

Spiroxatrine Chemical Structure

Spiroxatrine Chemical Structure

CAS No. : 1054-88-2

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Based on 1 publication(s) in Google Scholar

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Description

Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α, 5-HT1β and 5-HT2, respectively. Spiroxatrine (R 5188) has a sedative effect[1][2][3][4].

IC50 & Target

α2-adrenergic receptor

 

5-HT1A Receptor

3.94 nM (Ki)

5-HT1B/D Receptor

224000 nM (Ki)

5-HT2 Receptor

118.5 nM (Ki)

In Vitro

Spiroxatrine (0.01-0.1 μM, 15 mins) increases contraction in vas deferenstissues from α2A/D-adrenoceptor knockout mice[2].

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

In Vivo

Spiroxatrine (1-25 ug for i.p., 5 days) increases hindpaw withdrawal latencies to thermal and mechanical stimulation in the nerve injury rat and Carrageenan (HY-125474)-induced rat inflammation model[3].
Spiroxatrine (4 mg/kg/day for i.p., 5 mins) increases the voluntary oral ethanol intake induced by Fluoxetine (HY-B0102) in the selectively bred alcohol-preferring P line of rats [4].

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

Animal Model: The nerve injury rat model and Carrageenan (HY-125474)-induced rat inflammation model[3]
Dosage: 1, 10, 25 ug, 5 days
Administration: Intraperitoneal injection (i.p.)
Result: Increased hindpaw withdrawal latencies to thermal and mechanical stimulation.
Animal Model: Fluoxetine (HY-B0102) -induced reduction of ethanol Intake by the P Line of rats[4]
Dosage: 4 mg/kg/day, 5 mins
Administration: Intraperitoneal injection (i.p.)
Result: Increased the voluntary oral ethanol intake induced by Fluoxetine (HY-B0102) in the selectively bred alcohol-preferring P line of rats.
Molecular Weight

379.45

Formula

C22H25N3O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NCN(C2=CC=CC=C2)C13CCN(CC4OC5=CC=CC=C5OC4)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 1.92 mg/mL (5.06 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6354 mL 13.1770 mL 26.3539 mL
5 mM 0.5271 mL 2.6354 mL 5.2708 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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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.

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Product Name:
Spiroxatrine
Cat. No.:
HY-12706
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