1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
    Dopamine Receptor
  3. Spiramide

Spiramide (Synonyms: AMI-193)

Cat. No.: HY-100971 Purity: 98.81%
Handling Instructions

Spiramide (AMI-193) is a potent and selective antagonist of 5-HT2 and dopamine D2 receptor, with Kis of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT2 versus 5-HT1C (Ki=4300 nM) receptors. Spiramide exhibits antipsychotic activity.

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

Spiramide Chemical Structure

Spiramide Chemical Structure

CAS No. : 510-74-7

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100 mg USD 750 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Spiramide (AMI-193) is a potent and selective antagonist of 5-HT2 and dopamine D2 receptor, with Kis of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT2 versus 5-HT1C (Ki=4300 nM) receptors. Spiramide exhibits antipsychotic activity[1][2][3].

IC50 & Target[1]

5-HT2 Receptor

2 nM (Ki)

D2 Receptor

3 nM (Ki)

5-HT1A Receptor

50 nM (Ki)

D1 Receptor

2530 nM (Ki)

5-HT1C Receptor

4300 nM (Ki)

In Vitro

Spiramide retains affinity for 5-HT1A sites (Ki=50 nM) and also binds at dopamine D2 sites (Ki=3 nM), but possesses low affinity for dopamine D1 sites (Ki=2530 nM)[1].

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

In Vivo

AMI-193 (0.003-0.01 mg/kg; i.m.) dose-dependently decreases response rate in monkeys under a fixed-interval (FI) schedule of stimulus termination[2].
AMI-193 (0.003-0.01 mg/kg; i.m.) attenuates the discriminative-stimulus effects of cocaine in drug-discrimination experiments[2].
AMI-193 (0.003-0.01 mg/kg; i.m.) reduces response rate under a second-order schedule of i.v. self-administration of cocaine (0.1 mg/infusion)[2].

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

Animal Model: Adult male squirrel monkeys (850-1300 g)[2]
Dosage: 0.003, 0.01 mg/kg
Administration: I.m. on Tuesday, Wednesday, and Thursday the following week
Result: Decreased the response rate.
The rate-decreasing effects were reversed by cocaine.
Molecular Weight

383.46

Formula

C₂₂H₂₆FN₃O₂

CAS No.

510-74-7

SMILES

O=C1NCN(C2=CC=CC=C2)C13CCN(CCCOC4=CC=C(F)C=C4)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (52.16 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6078 mL 13.0392 mL 26.0783 mL
5 mM 0.5216 mL 2.6078 mL 5.2157 mL
10 mM 0.2608 mL 1.3039 mL 2.6078 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2 mg/mL (5.22 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2 mg/mL (5.22 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Keywords:

SpiramideAMI-193AMI193AMI 1935-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2dopamineD2antipsychoticInhibitorinhibitorinhibit

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Spiramide
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