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aRS 79948 hydrochloride
Other Information:
Sold with the permission of Roche Bioscience
Chemical Name:(8aR,12aS,13aS)-5,8,8a,9,10,11,12,12a,13,13a-dechydro-3
-methoxy-12-(ethylsulfonyl)-6H-isoquino[2,1-g][1,6]naph
thyridine hydrochloride
Biological Activity:
This analogue of the highly potent and selective α2-adrenoreceptor
antagonist RS 15385, differs only by having an ethyl instead of a methyl group
at position 12, and has essentially the same pharmacological properties.
Clark et al(1989)
(8aα,12aα,13aα)-5,8,8a,9,10,11,12,12a,13,13a-Decahydro-3-methoxy-12-(ethylsulphonyl)-6H-isoquino[2,1-g][1,6]-naphthyridine,
a potent and highly selective α2-adrenoceptor antagonist.
J. Med. Chem. 32 2034. MacKinnon et al (1992) [3H]-RS-15385-197,
a selective and high affinity radioligand for α2-adrenoceptors:
implications for receptor classification. Br.J. Pharmacol. 106
1011. Humeet al (1996) Evaluation in rat of RS-79948-197 as a
potential PET ligand for central α2-adrenoceptors.
Eur.J.Pharmacol. 317 67. Uhlen et al(1998)[3H]RS79948-197 binding to rat, guinea pig and pig α2A-, α2B and α2C-adrenoceptors.
Comparison with MK912, RX821002, rauwolscine and yohimbine.Eur.J.Pharmacol. 343 93.
