Electric Literature of 63006-93-9, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 63006-93-9, Name is (1,2,3,4-Tetrahydroisoquinolin-3-yl)methanol, molecular formula is C10H13NO. In a Article£¬once mentioned of 63006-93-9
3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N- methyltransferase versus the alpha2-adrenoceptor(1a)
3-Hydroxymethyl-1,2,3,4-tetrahydroisoquinoline (4) is a more selective inhibitor (PNMT K(i) = 1.1 muM, alpha2 K(i) = 6.6 muM, selectivity (alpha2 K(i)/PNMT K(i)) = 6.0) of phenylethanolamine N-methyltransferase (PNMT, EC 2.1.1.28), with respect to its alpha2-adrenoceptor affinity, than is 3-methyl- 1,2,3,4-tetrahydroisoquinoline (2; PNMT K(i) = 2.1muM, alpha2 K(i) = 0.76 muM, selectivity = 0.36) or 1,2,3,4-tetrahydroisoquinoline (1, THIQ; PNMT K(i) = 9.7 muM, alpha2 K(i) = 0.35 muM, selectivity = 0.036). Evaluation of the O- methyl ether derivative of 4 suggested that the 3-hydroxymethyl substituent might be involved in a hydrogen-bond donor-type of interaction at a sterically compact region in the PNMT active site. The directionality of the steric bulk tolerance at both the PNMT active site and the alpha2-adrenoceptor appears to be the same. Since the presence of a hydrophilic electron- withdrawing substituent (such as NO2, SO2CH3, or SO2NH2) at the 7- position of THIQ reduced the binding affinity toward the alpha2-adrenoceptor, we investigated the combination of both a hydrophilic electron-withdrawing 7- substituent and a 3-alkyl substituent on a THIQ nucleus. A synergistic effect in increasing the PNMT-inhibitory potency of the THIQ nucleus and reducing the affinity toward the alpha2-adrenoceptor was observed with this 3,7- disubstitution. Remarkably, 7-aminosulfonyl-3-hydroxymethyl-THIQ (12; PNMT K(i) = 0.34 muM, alpha2 K(i) = 1400 muM, selectivity = 4100) displayed a 23- 680-fold enhanced selectivity over the parent compounds 27 (SK and F 29661; PNMT K(i) = 0.55 muM, alpha2 K(i) = 100 muM, selectivity = 180) and 4 selectivity = 6.0) and is thus the most selective PNMT inhibitor yet reported.
Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Electric Literature of 63006-93-9. In my other articles, you can also check out more blogs about 63006-93-9
Reference£º
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem