38152-22-6Relevant academic research and scientific papers
Modifications to the tetracaine scaffold produce cyclic nucleotide-gated channel blockers with widely varying efficacies
Strassmaier, Timothy,Uma, Ramalinga,Ghatpande, Ambarish S.,Bandyopadhyay, Tapasree,Schaffer, Michelle,Witte, John,McDougal, Patrick G.,Brown, R. Lane,Karpen, Jeffrey W.
, p. 5805 - 5812 (2005)
Five new tetracaine analogues were synthesized and evaluated for potency of blockade of cyclic nucleotide-gated channels relative to a multiply charged tetracaine analogue described previously (4). Increased positive charge at the tertiary amine end of tetracaine results in higher potency and voltage dependence of block. Modifications that reduce the hydrophobic character at the butyl tail are deleterious to block. The tetracaine analogues described here have apparent affinities for CNGA1 channels that vary over nearly 8 orders of magnitude.
Preparation method of tetracaine hydrochloride
-
Paragraph 0012-0013, (2017/04/22)
The invention relates to the technical field of preparation method of tetracaine hydrochloride. The preparation method comprises the preparation steps: carrying out a reaction of p-nitrobenzoyl chloride (2) and 2-dimethylamino-1-ethanol (3) to generate p-nitrobenzoic acid-2-dimethylamino ethyl (4), reducing the compound (3) to obtain p-aminobenzoic acid-2-dimethylamino ethyl (4), generating pontocaine (7) from a compound (5) and 1-bromobutane (6) under alkaline conditions, and finally carrying out a reaction of the pontocaine (7) with HCl to generate tetracaine hydrochloride (1).
