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Alpha series of novel 3,6-diazabicyclo[3.1.1]heptane derivatives 4a-f was synthesized and their affinity and selectivity towards alpha4beta2 and alpha7 nAChR subtypes were evaluated. The results of the current study revealed a number of compounds (4a, 4b and 4c) having a very high affinity for alpha4beta2 (Ki at alpha4beta2 ranging from 0.023 to 0.056 nM) versus alpha7 nAChR subtypes; among these compounds, the 3-(6-bromopyridin-3-yl)-3,6-diazabicyclo[3.1.1]heptane 4c was found to be the most alpha7alpha4beta2 selective term in receptor binding assays (alpha7alpha4beta2 = 1295). Moreover, compound 4d also had high affinity for the alpha4beta2 nAChR subtype (Ki = 1.2 nM) with considerably high selectivity (alpha7/alpha4beta2 = 23300).
Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.Read on for other articles about 141-30-0Related Products of 141-30-0
Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1831 – PubChem