A dopamine receptor antagonist and 5-HT1A partial agonist; binds to dopamine D1

(–)-Stepholidine – 500 µg

Brand:
Cayman
CAS:
16562-13-3
Storage:
-20
UN-No:
Non-Hazardous - /

(–)-Stepholidine is a dopamine receptor antagonist and a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A.{45111,45112,45113} (–)-Stepholidine binds to dopamine D1, D2, D3, D4, and D5 receptors (Kis = 5.1, 11.6, 24, 1,450, and 5.8 nM, respectively) as well as 5-HT1A, 5-HT2B, α2C-adrenergic receptors (α2C-ARs), and sigma-2 (σ2) receptors in a radioligand binding assay (Kis = 143, 226, 215, and 53 nM, respectively).{45111} It inhibits dopamine-induced cAMP accumulation in HEK293 cells expressing dopamine D1, D2, and D5 receptors with IC50 values of 20.5, 128, and 27 nM, respectively. (–)-Stepholidine inhibits forskolin-induced cAMP production in CHO cells expressing rat 5-HT1A receptors (EC50 = 1.2 μM).{45112} In vivo, (–)-stepholidine (1 mg/kg, i.v.) increases dopamine neuron firing rates, the number of spikes in bursts, and the amplitude of slow oscillations by 20, 155, and 126%, respectively, in the rat ventral tegmental area (VTA), effects that can be blocked by the 5-HT1A antagonist WAY-100635 (Item No. 14599).{45113} Pretreatment with (–)-stepholidine inhibits amphetamine- and phencyclidine-induced locomotor activity in rats (ED50s = 2.4 and 6.5 mg/kg, respectively).{45114}  

 

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Description

A dopamine receptor antagonist and 5-HT1A partial agonist; binds to dopamine D1, D2, D3, D4, and D5 receptors (Kis = 5.1, 11.6, 24, 1,450, and 5.8 nM, respectively) as well as 5-HT1A, 5-HT2B, α2C-ARs, and σ2 receptors in a radioligand binding assay (Kis = 143, 226, 215, and 53 nM, respectively); inhibits dopamine-induced cAMP accumulation in HEK293 cells expressing dopamine D1, D2, and D5 receptors (IC50 = 20.5, 128, and 27 nM, respectively); inhibits forskolin-induced cAMP production in CHO cells expressing rat 5-HT1A receptors (EC50 = 1.2 μM); increases dopamine neuron firing rates, the number of spikes in bursts, and the amplitude of slow oscillations in the rat VTA at 1 mg/kg; inhibits amphetamine- and phencyclidine-induced locomotor activity in rats (ED50s = 2.4 and 6.5 mg/kg, respectively)

Formal name: (13aS)-5,8,13,13a-tetrahydro-3,9-dimethoxy-6H-dibenzo[a,g]quinolizine-2,10-diol

Synonyms: 

Molecular weight: 327.4

CAS: 16562-13-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience

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