Absorption, Distribution and Excretion
All metabolites exhibit high renal clearance, indicating that they are primarily excreted via active renal secretion. Metabolism/Metabolite Rapidly converted to its major active metabolite, which is subsequently further converted to two secondary metabolites. Biological Half-Life The average plasma half-life of averine is 0.8 hours, while the average plasma half-life of its major active metabolite is 5.7 hours.

:Br J Pharmacol, 2007. 152(8): p. 1228-38.

Alverine is a tertiary amine with an ethyl group and two 3-phenylpropyl-1-yl groups attached to its nitrogen atom. It is an antispasmodic that acts directly on the smooth muscle of the intestines and uterus, and is commonly used to treat irritable bowel syndrome (IBS), especially citrate. It is an antispasmodic and the conjugate base of Alverine (1+). Alverine is a smooth muscle relaxant used to relieve gastrointestinal spasms or cramps. Therefore, it can be used to treat irritable bowel syndrome (IBS) and similar conditions. It can also be used to relieve dysmenorrhea.

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Drug Indications
Used to relieve gastrointestinal spasms or cramps. It can also be used to treat irritable bowel syndrome (IBS) and similar conditions. It can also be used to relieve dysmenorrhea. Alverine citrate is currently under investigation to enhance the cytotoxic effects of the proteasome inhibitor MG132 on breast cancer cells.

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Therapeutic Uses
Parasympathetic Blocker
Used to treat gastrointestinal disorders with hypermotility or spasms…and genitourinary spasms, such as spasms caused by stone passage, urinary tract infection, or benign prostatic hyperplasia. …Also used to treat certain primary dysmenorrhea and as an adjunct to various endoscopic examinations. /Citrate/
Alverine gum, with or without the smooth muscle relaxant, showed similar benefits in constipation and shortened intestinal transit time in two groups of 10 patients with diverticulosis.
Anticholinergic Drug
Drug Warnings
Use with caution in elderly patients, patients with arteriosclerosis, and patients with angina. /Citrate/
Pharmacodynamics
Alverine is a smooth muscle relaxant. Smooth muscle is a type of muscle that is not controlled by voluntary muscle and is found in areas such as the intestines and uterus. Alverine acts directly on the intestinal muscles, causing them to relax. This can prevent intestinal muscle spasms caused by conditions such as irritable bowel syndrome and diverticulosis.
Diverticulosis is a condition where small pouches form along the lining of the intestines. These pouches trap food residue, leading to inflammation and pain. Irritable bowel syndrome (IBS) patients experience a loss of normal intestinal muscle activity. Muscle spasms can cause symptoms such as heartburn, abdominal pain, bloating, constipation, or diarrhea. Alverine citrate relieves these symptoms by relaxing intestinal muscles. Alverine can also relax uterine smooth muscle. Therefore, it is also used to treat dysmenorrhea (painful menstruation) caused by uterine muscle spasms.

C20H27N

281.214

150-59-4

5560-59-8 (citrate);5982-87-6 (HCl);3686-59-7 (tartrate);

3678

LIQUID

1.0±0.1 g/cm3

358.8±0.0 °C at 760 mmHg

< 25 °C

174.4±21.7 °C

0.0±0.8 mmHg at 25°C

1.548

5.93

0

1

9

21

214

0

CCN(CCCC1=CC=CC=C1)CCCC2=CC=CC=C2

ZPFXAOWNKLFJDN-UHFFFAOYSA-N

InChI=1S/C20H27N/c1-2-21(17-9-15-19-11-5-3-6-12-19)18-10-16-20-13-7-4-8-14-20/h3-8,11-14H,2,9-10,15-18H2,1H3

Benzenepropanamine, N-ethyl-N-(3-phenylpropyl)-

NSC 35459 NSC-35459 NSC35459

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)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)