Acetylcarnitine

Các tên gọi khác (3) :

acetyl-L-carnitine
O-acetyl-L-carnitine
O-Acetylcarnitine

Vitamin

Thuốc Gốc

Small Molecule

CAS: 3040-38-8

ATC: N06BX12

CTHH: C₉H₁₈NO₄

PTK: 204.2435

Acetylcarnitine is an investigational drug in the United states, Italy, United Kingdom, China, Israel, and Norway, and it is approved in Italy, Portugal, Argentina, Chile, Philippines, Australia, and India. Acetylcarnitine can be synthesized, but it is also naturally found in adequate amounts in healthy humans. In human plasma and tissues, acetylcarnitine is the most predominant acylated ester of carnitine, which is an amino acid derivative that is made in the kidney, liver, and brain from lysine and methionine. The main role of acetylcarnitine is to help transport fatty acids into the mitochondrial matrix where fatty acid metabolism occurs.

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₉H₁₈NO₄

Phân tử khối

204.2435

Monoisotopic mass

204.123583069

InChI

InChI=1/C9H17NO4/c1-7(11)14-8(5-9(12)13)6-10(2,3)4/h8H,5-6H2,1-4H3/p+1/t8-/s2

InChI Key

InChIKey=RDHQFKQIGNGIED-SVGMAFHSNA-O

IUPAC Name

[(2R)-2-(acetyloxy)-3-carboxypropyl]trimethylazanium

Traditional IUPAC Name

O-acetylcarnitinium

SMILES

CC(=O)O[C@H](CC(O)=O)C[N+](C)(C)C

Độ tan chảy

145°C

Độ hòa tan

Very soluble in water and alcohol.

logP

-4.4

logS

-2.8

pKa (strongest acidic)

4.09

pKa (Strongest Basic)

-7

PSA

63.6 Å²

Refractivity

61.8 m³·mol^-1

Polarizability

21.19 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Rule of Five

true

Dược Lực Học : The complete physiological effects of acetycarnitine are still being studied. What has been discovered so far is that acetylcarinitine has positive effects on mental fatigue, neurodegenerative disorders, cognitive functions, peripheral neuropathy, and sperm motility. Specifically, in one study involving patients with HIV, patients on acetylcarnitine supplementation had increased CD4 cells, decreased lymphocyte apoptosis, improved polyneuropathy and cardiovascular damage, and decreased triglyceride and TNF alpha levels in the blood. Another study showed that acetylcarnitine increased glucose disposal in type 2 diabetic patients through possibly increasing the activity of glycogen synthase.

Cơ Chế Tác Dụng : Acetylcarnitine is an investigational drug in the United states, Italy, United Kingdom, China, Israel, and Norway, and it is approved in Italy, Portugal, Argentina, Chile, Philippines, Australia, and India. Acetylcarnitine can be synthesized, but it is also naturally found in adequate amounts in healthy humans. In human plasma and tissues, acetylcarnitine is the most predominant acylated ester of carnitine, which is an amino acid derivative that is made in the kidney, liver, and brain from lysine and methionine. The main role of acetylcarnitine is to help transport fatty acids into the mitochondrial matrix where fatty acid metabolism occurs. The mechanisms of action of acetylcarnitine have not been fully elucidated, but it seems that the main role of acetylcarnitine is to donate an acetyl group during fatty acid metabolism to help transport fatty acids, such as acetyl CoA, into the mitochondrial matrix where fatty acid metabolism occurs. Additionally several studies have found that separate from its metabolic role, acetylcarnitine has neuromodulatory, neurotrophic, and neuroprotective effects that most likely are involved in its positive effects in neurological diseases. In its role in treating male infertility, acetylcarnitine increases the active movement of sperm cells. One study has also mentioned a role for acetylcarnitine as an antioxidant. The study found that through the receptor, tyrosine kinase A, acetylcarnitine was able to decrease the production of free radicals, peroxidation of lipids, and oxidation of proteins as well as decrease glutathione levels and increase thioredoxin.

Dược Động Học :

▧ Absorption :
Acetylcarnitine supplements are absorbed in a similar manner to L-carnitine.
▧ Route of Elimination :
Acetylcarnitine is eliminated in a similar manner as L-carnitine. Both of which are eliminated by the kidneys and involve tubular secretion.

Chỉ Định : Acetylcarnitine is not approved for any indication in the United states and Canada, but it is approved and indicated in Italy for cerebrovascular disorders, mental function disorders, peripheral nerve disorders, diabetic neuropathy, and nutritional supplementation; Portugal for mental function disorders; Argentina for cerebral vasculopathy, nutritional supplementation, and peripheral neuropathy; Chile for dementia; Philippines for cerebrovascular disorders and mental function disorders; Australia for nutritional supplementation; and India for nutritional supplementation to increase sperm count. Acetylcarnitine also has several potential therapeutic indications for which it is still being investigated: in Norway, acetylcarnitine is in a phase IV trial for prophylactic treatment of migraines; in Italy acetylcarnitine is in a phase II trial for use in patients with type 2 Diabetes Mellitus, a phase III trial for alleviating fatigue in patients with chronic hepatitis C, and for use in patients with Minimal Hepatic Encephalopathy; in the United States acetylcarnitine is in a phase II trial for the neurodegenerative disorder Progressive Supranuclear Palsy, a phase II and III trial for reducing peripheral neuropathy in cancer patients as an adjunct to chemotherapy, a phase I and II trial for treating patients in septic shock, a phase II trial for bipolar depression, a phase II trial to reduce oxidative stress in patients with Sickle Cell disease, a phase I and II trial for chronic fatigue syndrome, and a study for preventing nerve damage in HIV patients; in China acetylcarnitine is in a phase III trial for reducing peripheral neuropathy in cancer patients as an adjunct to chemotherapy; in the United Kingdom acetylcarnitine is being investigated for preventing nerve damage in HIV patients; and in Israel acetylcarnitine is being studied for the treatment of male infertility.

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty : IFI (Italy)

Sản phẩm biệt dược : Acilen
Công ty : Bago (Chile)

Sản phẩm biệt dược : Actigeron
Công ty : Sigma-Tau (Italy)

Sản phẩm biệt dược : Branigen
Công ty : OFF (Italy)

Sản phẩm biệt dược : Branitil
Công ty : IRBI (Italy)

Sản phẩm biệt dược : Ceredor
Công ty : Fortbenton (Argentina)

Sản phẩm biệt dược : Fertilix
Công ty : Pentafarma (Portugal)

Sản phẩm biệt dược : Lacetilina
Công ty : Lafedar (Argentina)

Sản phẩm biệt dược : Laremide
Công ty : Korea United (Philippines)

Sản phẩm biệt dược : Levocetile
Công ty : Sun (India)

Sản phẩm biệt dược : Maxoza
Công ty : Gruppo Medica (Philippines)

Sản phẩm biệt dược : Memorx IQ Plus
Công ty : Euro-Pharma (Italy)

Sản phẩm biệt dược : Memovigor
Công ty : Beta (Argentina)

Sản phẩm biệt dược : Neurex
Công ty : Bago (Argentina)

Sản phẩm biệt dược : Neuroactil
Công ty : Sigma-Tau (Italy)

Sản phẩm biệt dược : Nicetile
Công ty : Medosan (Italy)

Sản phẩm biệt dược : Normobren
Công ty : Tubilux (Italy)

Sản phẩm biệt dược : Phototrop
Công ty : Sigma-Tau (Italy)

Sản phẩm biệt dược : Zibren

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB08842

KEGG Compound

http://www.genome.jp/dbget-bin/www_bget?cpd:C02571

Wikipedia

http://en.wikipedia.org/wiki/Acetylcarnitine

RxList

http://www.rxlist.com/acetyl-l-carnitine/supplements.htm

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