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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. [1] In rat spinal cord, BMY 7378 is a weak partial agonist at the hippocampal 5-HT1A receptors. [2] 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. [3] In ligand-binding assay, BMY 7378 displays a 10-fold selectivity for α2C adrenergic receptors over other α2 adrenergic receptors. [4]

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.) [5]

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