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Cap 11 - Recettori della serotonina e farmaci attivi sulla neurotrasmissione serotoninergica
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Synthesis and pharmacological evaluation of some thiolupinine derivatives
No full textA small set of 9-(lupinylthio)xanthene, -thioxanthenes and α-(lupinylthio)diphenylmethanes was prepared and found to inhibit
the angiotensin II-induced contractions of guinea pig ileum. Some of these compounds were also moderately active in vitro as
tracheal relaxants and one compound was more active than aspirin against arachidonic acid-induced platelet aggregation
N-Homolupinanoyl and N-(ω-lupinylthio)alkanoyl derivatives of some tricyclic systems as ligands for muscarinic M1 and M2 receptor subtypes
No full textA set of N-homolupinanoyl- and N-(v-lupinylthio)alkanoyl derivatives of tricyclic systems (as phenothiazine, iminodibenzyl and
dihydropyridobenzodiazepinone) has been prepared and tested for affinity for rat muscarinic M1 and M2 receptor subtypes labeled
with [3H]pirenzepine and [3H]AF-DX 384. Good affinity for both M1 and M2 subtypes was displayed by most compounds, often
with nanomolar Ki values, which for lupinylthiopropionyl- and lupinylthiobutyryl-phenothiazines (13/16) were comparable to
those of pirenzepine and methoctramine, respectively. However, only moderate selectivity for one or the other subtype was seen
Cytisine derivatives as ligands for neuronal nicotine receptors and with various pharmacological activities
No full textNeuronal nicotinic acetylcholine receptors (nAChRs) form a family of ACh-gated cation channels made up of different subtypes.
They are widely distributed in peripheral and central nervous systems and are involved in complex cerebral processes as learning,
memory, nociception, movement, etc. The possibility that subtype-selective ligands be used in the treatment of CNS disorders
promoted the synthesis of a large number of structural analogues of nicotine and epibatidine, two very potent nAChR agonists.
Pursuing our long standing research on the structural modification of quinolizidine alkaloids, we devoted our attention to cytisine,
another very potent ligand for many nAChR subtypes. Thus a systematic structural modification of cytisine was undertaken in
order to obtain compounds of potential therapeutic interest at peripheral as well as central level, with a particular concern for
achieving nAChR subtype selective ligands. Up to the present more than 80 cytisine derivatives, mainly of N-substitution and a few
by modifying the pyridone ring, have been prepared. The biological results, which concern so far about an half of the prepared
compounds, indicate that the introduction of a nitro group in position 3 of the pyridone nucleus further enhances the high affinity of
cytisine, while the introduction of substituents on the basic nitrogen, though reducing in different degrees the affinity, gives rise to
compounds with a higher selectivity for central (α4β2) versus gangliar (α3-containing) receptor subtype. On the other hand, the analgesic, antihypertensive and inotropic activities found in some N-substituted cytisines, represent an attractive starting point for the development of more active compounds
(+)-Laburnamine, a natural selective ligand and partial agonist for the α4β2 nicotinic receptor subtype
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