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具有甜味的局部麻醉剂和血管收缩剂离子共轭物。

Sweet-Tasting Ionic Conjugates of Local Anesthetics and Vasoconstrictors.

机构信息

Department of Orthodontics, College of Dentistry, University of Florida, Gainesville, FL 32610, USA.

EigenChem Technologies Inc., Alachua, FL 32615, USA.

出版信息

Molecules. 2021 Feb 12;26(4):983. doi: 10.3390/molecules26040983.

DOI:10.3390/molecules26040983
PMID:33673320
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7918242/
Abstract

Local anesthetics are widely utilized in dentistry, cosmetology, and medicine. Local anesthesia is essential to providing a pain-free experience during dental and local surgeries as well as cosmetic procedures. However, the injection itself may produce discomfort and be a source of aversion. A novel approach toward the taste modulation of local anesthetics is proposed, in which the anesthetics of the "-caine" family serve as cations and are coupled with anionic sweeteners such as saccharinate and acesulfamate. Ionic conjugates of vasoconstrictor epinephrine such as epinephrine saccharinate and epinephrine acesulfamate have also been synthesized. Novel ionic conjugates were developed using anion exchange techniques. Reported compounds are sweet-tasting and are safe to use both topically and as injections.

摘要

局部麻醉剂在牙科、美容和医学领域得到广泛应用。局部麻醉对于在牙科和局部手术以及美容程序中提供无痛体验至关重要。然而,注射本身可能会引起不适,并成为人们反感的原因。本文提出了一种局部麻醉剂味觉调制的新方法,其中“-caine”家族的麻醉剂作为阳离子与 saccharinate 和 acesulfamate 等阴离子甜味剂结合。也已经合成了血管收缩剂肾上腺素的离子共轭物,如肾上腺素 saccharinate 和肾上腺素 acesulfamate。新型离子共轭物是使用阴离子交换技术开发的。报道的化合物具有甜味,可以安全地用于局部和注射。

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Sweet-Tasting Ionic Conjugates of Local Anesthetics and Vasoconstrictors.具有甜味的局部麻醉剂和血管收缩剂离子共轭物。
Molecules. 2021 Feb 12;26(4):983. doi: 10.3390/molecules26040983.
2
Ionic conjugates of lidocaine and sweeteners as better tasting local anesthetics for dentistry.利多卡因与甜味剂的离子共轭物作为口感更佳的牙科局部麻醉剂。
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本文引用的文献

1
Ionic conjugates of lidocaine and sweeteners as better tasting local anesthetics for dentistry.利多卡因与甜味剂的离子共轭物作为口感更佳的牙科局部麻醉剂。
J Mater Chem B. 2015 Nov 21;3(43):8492-8498. doi: 10.1039/c5tb00674k. Epub 2015 Sep 29.
2
Warmed and buffered lidocaine for pain relief during bone marrow aspiration and biopsy. A randomized and controlled trial.用于骨髓穿刺和活检时缓解疼痛的温热缓冲利多卡因。一项随机对照试验。
Scand J Pain. 2014 Jan 1;5(1):43-47. doi: 10.1016/j.sjpain.2013.10.003.
3
The Effect of Oral Dexmedetomidine Premedication on Preoperative Cooperation and Emergence Delirium in Children Undergoing Dental Procedures.
口腔右美托咪定用药对行牙科治疗患儿术前配合和苏醒期谵妄的影响。
Biomed Res Int. 2017;2017:6742183. doi: 10.1155/2017/6742183. Epub 2017 Aug 20.
4
A Review of Local Anesthetics: Minimizing Risk and Side Effects in Cutaneous Surgery.局部麻醉药综述:降低皮肤外科手术中的风险和副作用
Dermatol Surg. 2017 Feb;43(2):173-187. doi: 10.1097/DSS.0000000000000887.
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Development and Clinical Evaluation of New Topical Anesthetic Formulations for Dental Care.
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Dental anxiety among adults: an epidemiological study in South India.成人牙科焦虑症:印度南部的一项流行病学研究。
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Masking the bitter taste of injectable lidocaine HCl formulation for dental procedures.掩盖用于牙科手术的盐酸利多卡因注射剂的苦味。
AAPS PharmSciTech. 2015 Apr;16(2):455-65. doi: 10.1208/s12249-014-0239-z. Epub 2014 Nov 1.
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Minimizing the pain of local anesthesia injection.尽量减轻局部麻醉注射的疼痛。
Plast Reconstr Surg. 2013 Sep;132(3):675-684. doi: 10.1097/PRS.0b013e31829ad1e2.
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Use of the Operant Orofacial Pain Assessment Device (OPAD) to measure changes in nociceptive behavior.使用操作性口面部疼痛评估装置(OPAD)测量伤害感受性行为的变化。
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10
The cytotoxicity of bupivacaine, ropivacaine, and mepivacaine on human chondrocytes and cartilage.布比卡因、罗哌卡因和甲哌卡因对人软骨细胞和软骨的细胞毒性。
Anesth Analg. 2013 Aug;117(2):514-22. doi: 10.1213/ANE.0b013e31829481ed. Epub 2013 Jun 7.