Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride,introducing its new discovery., category: quinuclidine
Varying Chirality Across Nicotinic Acetylcholine Receptor Subtypes: Selective Binding of Quinuclidine Triazole Compounds
The novel quinuclidine anti-1,2,3-triazole derivatives T1-T6 were designed based on the structure of QND8. The binding studies revealed that the stereochemistry at the C3 position of the quinuclidine scaffold plays an important role in the nAChR subtype selectivity. Whereas the (R)-enantiomers are selective to alpha7 over alpha4beta2 (by factors of 44-225) and to a smaller degree over alpha3beta4 (3-33), their (S)-counterparts prefer alpha3beta4 over alpha4beta2 (62-237) as well as over alpha7 (5-294). The (R)-derivatives were highly selective to alpha7 over alpha3beta4 subtypes compared to (RS)- and (R)-QND8. The (S)-enantiomers are 5-10 times more selective to alpha4beta2 than their (R) forms. The overall strongest affinity is observed for the (S)-enantiomer binding to alpha3beta4 (Ki, 2.25-19.5 nM) followed by their (R)-counterpart binding to alpha7 (Ki, 22.5-117 nM), with a significantly weaker (S)-enantiomer binding to alpha4beta2 (Ki, 414-1980 nM) still above the very weak respective (R)-analogue affinity (Ki, 5059-10436 nM).
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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H154N | ChemSpider