5-HT1A partial agonist and α1D adrenoceptor antagonist
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||21102-95-4||SDF||Download SDF|
|Solubility||Soluble in DMSO > 10 mM||Storage||Store at -20°C|
BMY 7378 is a α2C and α1D adrenergic receptors inhibitor (pKi= 6.54 and 8.2, respectively) and a mixed agonist and antagonist for 5-HT1A receptors.
Adrenergic α1 and α2 receptors are G protein-coupled receptors that are located in CNS and periphery. It plays a role in regulating neurotransmission, smooth muscle contraction and thermogegualtion. 5-HT receptor is a G-protein coupled receptor for 5-hydroxytryptamine (serotonin) that found in nerve systems. It also functions as receptor for various alkaloids and psychoactive substances.
BMY 7378 blocks the inhibition on forskolin-stimulated adenylate cyclase activity in rat hippocampus induced by the 5-HT1A agonist, 8-OHh-DPAT.  In rat spinal cord, BMY 7378 is a weak partial agonist at the hippocampal 5-HT1A receptors.  BMY 7378 is also the first α1D adrenergic receptors subtype selective ligand that has high affinity and had a clear pharmacological distinction between the α1B and α1D adrenergic receptors subtypes.  In ligand-binding assay, BMY 7378 displays a 10-fold selectivity for α2C adrenergic receptors over other α2 adrenergic receptors. 
BMY 7378 not only shows 5-HT1A antagonist activity in the rat behavioral experiments, but also exerts a marked decrease of 5-HT release in ventral hippocampus of the anaesthetized rat in a dose-dependent manner (0.01-1.0 mg/kg s.c.) 
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