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My CartCAS：99291-25-5
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 99291-25-5 |
| Name | Levodropropizine |
| Molecular Formula | C13H20N2O2 |
| Molecular Weight | 236.31 |
| Solubility | Soluble in Water/DMSO(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00866852 |
| SMILES | C1CN(CCN1CC(CO)O)C2=CC=CC=C2 |
| InChIKey | PTVWPYVOOKLBCG-ZDUSSCGKSA-N |
| InChI | InChI=1S/C13H20N2O2/c16-11-13(17)10-14-6-8-15(9-7-14)12-4-2-1-3-5-12/h1-5，13，16-17H，6-11H2/t13-/m0/s1 |
| PubChem CID | 65859 |
| Target Point | Histamine Receptor |
| Passage | GPCR & G Protein;Neuronal Signaling;Immunology & Inflammation |
| Background | Levodropropizine inhibits histamine receptors and reduces cough by interfering with stimulatory activation of peripheral sensory nerve endings and modulating neuropeptides involved in the cough reflex. |
| Biological Activity | Levodropropizine 可以抗过敏并抑制组胺受体，通过干扰外围感觉神经末端的刺激活化作用以及调节参与咳嗽反射的神经肽来减轻咳嗽。[1-5] |
| In Vivo | 静脉注射或腹腔注射左羟丙哌嗪不会对心血管和呼吸系统产生任何明显影响，对 H1 组胺受体和α-肾上腺素能受体具有亲和力。[1]静脉注射左羟丙哌嗪(LVDP)能显著降低迷走 C 纤维对化学刺激的反应，缩短呼吸暂停的持续时间，并降低 C 纤维对 PBG 的反应，C 纤维的放电率降低。LVDP 对 C 纤维对 PBG 反应的抑制作用在肺纤维中平均为 50%，在非肺纤维中平均为 25%。[2]静脉注射后，左羟丙哌嗪对兔子和豚鼠机械和电击引起的咳嗽的活性是可待因的 1/10 至 1/20，与它的衍生物滴罗匹嗪相当。豚鼠口服左羟丙哌嗪后，在刺激性气溶胶引起的咳嗽方面，镇咳活性与滴罗匹嗪和可待因相当。[3]左旋多巴嗪的外周作用部位与感觉神经肽有关。豚鼠咳嗽模型脑室内注射左羟丙哌嗪(40 微克/50 微升 i.c.v.)并不能阻止电引起的咳嗽。在辣椒素诱发的咳嗽中，口服后，可待因的药效大约是左羟丙哌嗪的两到三倍。在气雾剂给药后，这两种化合物的药效相当。[4]左羟丙哌嗪(10、50 和 200 毫克/千克)以剂量依赖的方式减少了辣椒素诱发的大鼠气管中神经源性血浆外渗。[5] |
| Data Literature Source | [1]. Melillo G，et al. General pharmacology of the new antitussive levodropropizine. Arzneimittelforschung. 1988 Aug;38(8):1144-50. [2]. Shams H，et al. Effects of levodropropizine on vagal afferent C-fibres in the cat. Br J Pharmacol. 1996 Mar;117(5):853-8. [3]. Malandrino S，et al. Antitussive properties of levodropropizine. Arzneimittelforschung. 1988 Aug;38(8):1141-3. [4]. Lavezzo A，et al. Peripheral site of action of levodropropizine in experimentally-induced cough: role of sensory neuropeptides. Pulm Pharmacol. 1992 Jun;5(2):143-7. [5]. Yamawaki I，et al. Levodropropizine reduces capsaicin- and substance P-induced plasma extravasation in the rat trachea. Eur J Pharmacol. 1993 Oct 12;243(1):1-6. |
| Unit | Bottle |
| Specification | 50mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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