186 research outputs found
Thiol-reactive analogues of galanthamine, codeine and morphine as potential probes to interrogate allosteric binding within nAChRs
Alkaloids including galanthamine (1) and codeine (2) are reported to be positive allosteric modulators of nicotinic acetylcholine receptors (nAChRs) but the binding sites responsible for this activity are not known with certainty. Analogues of galanthamine (1), codeine (2) and morphine (3) with reactivity towards cysteine thiols were synthesised including conjugated enone derivatives of the three alkaloids 4-6 and two chloro-alkane derivatives of codeine 7 and 8. The stability of the enones was deemed sufficient for use in buffered aqueous solutions and their reactivity towards thiols was assessed by determining the kinetics of reaction with a cysteine derivative. All three enone derivatives were of sufficient reactivity and stability to be used in covalent trapping, an extension of the substituted cysteine accessibility method (SCAM), to elucidate the allosteric binding sites of galanthamine and codeine at nAChRs
New binding site in the nicotinic acetylcholine receptors:hope for new treatment of e.g. ADHD and Alzheimer's disease
Anlægsrapport - F414/FP412 benved (<em>Euonymus europaeus</em>) - fremavl af træer og buske til landskabsformål 2001-2010
Anlægsrapport - F412/FP418 fjeldribs (<em>Ribes alpinum</em>) - fremavl af træer og buske til landskabsformål 2001-2010
Anlægsrapport - F410/FP403 dunet gedeblad (<em>Lonicera xylosteum</em>) - fremavl af træer og buske til landskabsformål 2001-2010
Anlægsrapport - F411/FP424 kvalkved (<em>Viburnum opulus</em>) - fremavl af træer og buske til landskabsformål 2001-2010
Anlægsrapport - F413/FP294 dunbirk (<em>Betula pubescens)</em> - fremavl af træer og buske til landskabsformål 2001-2010
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