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.
Structural Formula
Spiramide
Solubility
DMSO : 20 mg/mL(52.16 mM;Need ultrasonic)
Source
Plants >Rosaceae > Spiraea japonica
Storage
-20℃, stored under nitrogen
IC50 & Target
Human Endogenous Metabolite
Shipping
Room temperature in continental US; may vary elsewhere.
SMILES
O=C1NCN(C2=CC=CC=C2)C13CCN(CCCOC4=CC=C(F)C=C4)CC3
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.AMI-193 (0.003-0.01 mg/kg; i.m.) attenuates the discriminative-stimulus effects of cocaine in drug-discrimination experiments.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).
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).
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Datasheet 