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In Vitro Characterization of AR-A000002, a Novel 5-hydroxytryptamine(1B) Autoreceptor Antagonist

In Vitro Characterization of AR-A000002, a Novel 5-hydroxytryptamine(1B) Autoreceptor Antagonist

Charlotte Ahlgren, Anders Eriksson, Pernilla Tellefors, Svante B Ross, Carina Stenfors, Asa Malmberg

Eur J Pharmacol. 2004 Sep 19;499(1-2):67-75.

PMID: 15363952

Abstract:

The in vitro pharmacological properties of AR-A000002 ((R)-N-[5-methyl-8-(4-methylpiperazin-1-yl)-1,2,3,4-tetrahydro-2-naphthyl]-4-morpholinobenzamide), a novel 5-hydroxytryptamine (5-HT)(1B) receptor antagonist, were studied. AR-A000002 bound with high affinity to guinea pig cortex and recombinant guinea pig 5-HT(1B) receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to 5-HT(1D) receptors. The compound displayed weak or no affinity for 63 other binding sites tested. In [35S]GTPgammaS assays AR-A000002 showed 50% efficacy and inhibited 5-HT stimulation with 66% and a pA2 value of 8.9. In slices of guinea pig cortex, AR-A000002 enhanced the outflow of [3H]5-HT upon electrical stimulation. The compound blocked sumatriptan-evoked contraction of rabbit saphenous veins without inducing any contraction itself. Thus, in these two systems AR-A000002 behaved as a 5-HT(1B) receptor antagonist. It is concluded that AR-A000002 is a selective high affinity 5HT(1B) receptor ligand that shows partial agonist activity in recombinant systems. In native tissues AR-A000002 behaves as a 5-HT(1B) receptor antagonist.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP151272901	CP-135807		151272-90-1	Price

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