| Description | Vadocaine (Vadocaina) is a novel analgesic compound for local anaesthesia and can be used to study the central nervous system and cardiovascular system. |
| In vivo | 在豚鼠身上，vadocaine通过口服2.5 mg/kg的剂量，能将由硫磺二氧化物或氨诱导的咳嗽发作次数减少约70%，相较于磷酸可待因，其效果更为显著。在猫咪中，vadocaine（3 mg/kg，静脉注射）通过机械刺激气管引发的咳嗽反射，在约10分钟内抑制了大约80%。当vadocaine通过椎动脉给药时，其活性比经静脉给药路径高出约10倍。可待因的活性是vadocaine的3倍，无论通过哪种给药途径。这一结果表明vadocaine抗咳动作中有一个重要的中枢成分。在另一个猫的模型中，vadocaine的5 mg/kg剂量比可待因的1 mg/kg剂量在通过电刺激喉神经引发的咳嗽抑制上略显弱效（Domenjoz方法）。在狗狗身上，vadocaine和可待因分别以6 mg/kg口服和静脉注射的剂量，以及2 mg/kg的可待因剂量，在抑制通过电刺激气管引起的咳嗽上，抑制率达60-80%，表现出大致相同的效力。vadocaine在口服给药期间，血清浓度约为1微克/ml。通过两种途径，抗咳活性（抑制50%以上的咳嗽）至少持续2小时。vadocaine在0.25%和0.5%的浓度下，对豚鼠皮肤风团的局部麻醉作用，以及在0.5%浓度下对豚鼠角膜的局部麻醉作用，其麻醉持续时间均长于利多卡因。vadocaine对豚鼠气管条的实验没有产生影响。 |
| Synonyms | Vadocaina, Vadocainum |
| molecular weight | 304.43 |
| Molecular formula | C18H28N2O2 |
| CAS | 72005-58-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (197.09 mM) |
| References | 1. Männistö PT, et al. Antitussive action of the new anilide derivative vadocaine hydrochloride compared with codeine phosphate in four animal models. Arzneimittelforschung. 1988 Apr;38(4A):598-604. 2. Paakkari I, et al. Cardiovascular and ventilator effects of vadocaine hydrochloride in urethane-anaesthetized rats and guinea-pigs. Arzneimittelforschung. 1988 Apr;38(4A):617-9.2. 3. Karttunen P, et al. Studies on the nonspecific central nervous system effects of the novel antitussive compound vadocaine hydrochloride. Arzneimittelforschung. 1988 Apr;38(4A):605-8. 4. Silvasti M, et al. The single dose and steady-state pharmacokinetics of a vadocaine tablet in healthy human volunteers. Int J Clin Pharmacol Ther Toxicol. 1989 Nov;27(11):558-63. |