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A-315456: A Selective alpha(1D)-adrenoceptor Antagonist With Minimal Dopamine D(2) and 5-HT(1A) Receptor Affinity

A-315456: A Selective alpha(1D)-adrenoceptor Antagonist With Minimal Dopamine D(2) and 5-HT(1A) Receptor Affinity

S A Buckner, I Milicic, A Daza, J J Lynch 3rd, T Kolasa, M Nakane, J P Sullivan, J D Brioni

Eur J Pharmacol. 2001 Dec 14;433(1):123-7.

PMID: 11755142

Abstract:

In functional assays, A-315456, N-[3-(cyclohexylidene-(1H-imidazol-4-ylmethyl))phenyl]ethanesulfonamide, behaved as an alpha(1D)-adrenoceptor subtype selective antagonist (pA(2)=8.34) in the rat aorta. It was 83-fold less potent at the alpha(1B)-adrenoceptor subtype expressed in the rat spleen, and was inactive at the alpha(1A)-adrenoceptor subtype expressed in the rat vas deferens. Radioligand binding assays also revealed high affinity (pK(i)=8.71) for the alpha(1D)-adrenoceptor subtype and weaker affinities at the alpha(1A)-adrenoceptor (pK(i)=6.23) and alpha(1B)-adrenoceptor (pK(i)=7.86). In comparison to its potent affinity at the alpha(1D)-adrenoceptor subtype, A-315456 was 3020-, 794- and 38-fold weaker at the dopamine D(2)-, 5-HT(1A)-, and alpha(2a)-adrenoceptors, respectively. These studies indicate that A-315456 is a potent and selective alpha(1D)-antagonist that may serve as a useful pharmacological ligand to probe the physiological role of the alpha(1D)-adrenoceptor subtype in normal and disease states.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
IAR4241415	A-315456			Price

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