Fourteen tropane and related alkaloids were analyzed for their affinity for nicotinic and/or muscarinic acetylcholine receptors. The biogenetic intermediates littorine, 6 beta-hydroxyhyoscyamine, 7 beta-hydroxyhyoscyamine exhibit similar affinities at the muscarinic receptor as scopolamine and atropine. The quarternary derivatives N-methylatropine and N-methylscopolamine show the highest binding with IC50 values of less than 100 pM and 300 pM, respectively. The tropane alkaloids (including cocaine) also bind to the nicotinic acetylcholine receptor, albeit with much lower affinities.
机构:
Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Copenhagen, Denmark
NeuroSearch AS, Ballerup, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Copenhagen, Denmark
Olsen, Jeppe A.
论文数: 引用数:
h-index:
机构:
Balle, Thomas
Gajhede, Michael
论文数: 0引用数: 0
h-index: 0
机构:
Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Copenhagen, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Copenhagen, Denmark
Gajhede, Michael
Ahring, Philip K.
论文数: 0引用数: 0
h-index: 0
机构:
Univ Sydney, Fac Pharm, Sydney, NSW 2006, Australia
Aniona ApS, Ballerup, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Copenhagen, Denmark
Ahring, Philip K.
Kastrup, Jette S.
论文数: 0引用数: 0
h-index: 0
机构:
Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Copenhagen, DenmarkUniv Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, Copenhagen, Denmark