Ki 为 75 nM 时，喷托韦林以竞争性方式与豚鼠脑膜上的 [3H]-喷他佐辛标记位置结合 [4]。

在豚鼠中，喷托韦林（1-5 mg/kg；单次腹腔注射）可减少柠檬酸引起的咳嗽[4]。

Absorption, Distribution and Excretion
In humans, peak plasma concentrations are reached 1.2 hours after oral administration. Pharmacokinetic Data Unavailable Pharmacokinetic Data Unavailable Pharmacokinetic Data Unavailable Metabolism/Metabolites Pharmacokinetic Data Unavailable Biological Half-Life The half-life after oral administration is 2.3 hours.

Protein Binding

No pharmacokinetic data available.

[1]. Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands. J Med Chem. 1994 Jul 22;37(15):2285-91.

[2]. Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br J Pharmacol. 2004 Jan;141(2):233-40.

[3]. Extraction-free spectrophotometric assay of the antitussive drug pentoxyverine citrate using sulfonephthalein dyes. Spectrochim Acta A Mol Biomol Spectrosc. 2019 Nov 5;222:117186.

[4]. Sigma-1 Receptor Agonism Promotes Mechanical Allodynia After Priming the Nociceptive System with Capsaicin. Sci Rep. 2016 Nov 25:6:37835. doi: 10.1038/srep37835.

[5]. In Vivo Evaluation of the Antiasthmatic, Antitussive, and Expectorant Activities and Chemical Components of Three Elaeagnus Leaves. Evid Based Complement Alternat Med. 2015:2015:428208.

1-Phenylacetic acid 2-[2-(diethylamino)ethoxy]ethyl ester belongs to the benzene family of compounds.
Pethylverine (also known as carbetapentane) is a non-opioid centrally acting antitussive with antimuscarinic, anticonvulsant, and local anesthetic effects. It is used in combination with guaifenesin and H1 receptor antagonists and is the active ingredient in many over-the-counter cough medicines. Pethylverine acts on σ-1 receptors as well as κ and μ opioid receptors. The U.S. Food and Drug Administration (FDA) has revoked the approval of all oral gel formulations containing pethylverine citrate. Other forms of pethylverine citrate are still available on the market.
Indications
For the relief of cough caused by the common cold, influenza, bronchitis, and sinusitis.
Mechanism of Action
The mechanism of action of pethylverine's antitussive effect is not fully understood, but it is generally believed to be mediated by σ-1 receptors expressed in the central nervous system. Pentovirine, as a σ receptor agonist, has a Ki value of 75 ± 28 nM, as confirmed in competitive binding assays. The role of σ receptors in antitussive activity is unclear, but these receptors are highly expressed in the nucleus tractus solitarius (NTS) of the brainstem, where afferent fibers first form synapses. Located near the brainstem cough center, the NTS may act as a "gateway" for the cough reflex, allowing σ-1 receptor agonists to modulate the cough reflex before afferent nerves reach the cough center. Studies have shown that highly lipophilic σ-1 receptor agonists may penetrate the central nervous system after systemic administration. When administered as an aerosol, σ-1 receptor agonists may act temporarily peripherally, modulating cough by activating σ receptors expressed in the lungs. However, current evidence regarding the peripheral localization of σ receptor agonists after aerosol administration and the exclusion of systemic exposure is limited. The local anesthetic effect of pentoxifylline may be achieved by inhibiting voltage-gated sodium ion currents. Many drugs are known to reduce cough through their central action, but their exact mechanisms remain not fully understood. /Non-Opioid Antitussives/

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Therapeutic Use
Antussis
...Drugs previously used as centrally acting antitussives include...carbeta-spray...

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Drug Warnings
Other drugs previously used as...antitussives include...carbeta-spray, caramifen, and oxoramine. ...Overall, they have low toxicity, but there is currently a lack of sufficient controlled clinical studies to determine whether they are worthwhile alternatives to more well-studied drugs.
Generally, any centrally acting antitussive should be used with caution in combination with other centrally acting antitussives. /Antussis/

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Pharmacodynamics
Pentanone can cause antitussive effects. Animal studies have shown that intraperitoneal injection of pentanone can inhibit citric acid-induced cough in guinea pigs. Some mouse and rat studies have shown that pentanone may also have anticonvulsant activity and does not provide protection against NMDA receptor-induced lethality. Following intraperitoneal or oral administration, penoxyverine demonstrated a dose-dependent protective effect against maximal electroshock-induced seizures. In hERG-transfected cells, penoxyverine inhibited the outward current of hERG ion channels at a half-maximal inhibitory concentration (IC50) of 3.0 µM. In rats receiving intrathecal injection, penoxyverine exhibited a dose-dependent spinal cord blockade effect, with stronger sensory selectivity than motor blockade. Compared to lidocaine, penoxyverine-induced spinal cord blockade showed stronger sensory/nociceptive selectivity than motor blockade.

C20H31NO3

333.46504

333.23

77-23-6

Pentoxyverine citrate;23142-01-0

2562

White to off-white solid powder

1.0±0.1 g/cm3

435.5±30.0 °C at 760 mmHg

90-95

217.2±24.6 °C

0.0±1.0 mmHg at 25°C

1.517

3.29

38.77

0

4

11

24

356

0

CFJMRBQWBDQYMK-UHFFFAOYSA-N

InChI=1S/C20H31NO3/c1-3-21(4-2)14-15-23-16-17-24-19(22)20(12-8-9-13-20)18-10-6-5-7-11-18/h5-7,10-11H,3-4,8-9,12-17H2,1-2H3

2-[2-(diethylamino)ethoxy]ethyl 1-phenylcyclopentane-1-carboxylate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~250 mg/mL (~749.69 mM)

配方 1 中的溶解度: ≥ 2.08 mg/mL (6.24 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 20.8 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.08 mg/mL (6.24 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.08 mg/mL (6.24 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。