2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. Methocinnamox

Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor (KOR) (Ki = 4.9 nM) and delta-opioid receptor (DOR) (Ki = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Methocinnamox

Methocinnamox 構造式

CAS 番号 : 117339-76-1

容量 在庫状況
50 mg   お問い合わせ  
100 mg   お問い合わせ  
250 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

Methocinnamox 関連抗体

Top Publications Citing Use of Products

Opioid Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor (KOR) (Ki = 4.9 nM) and delta-opioid receptor (DOR) (Ki = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction[1][2][3].

IC50 & Target[3]

μ Opioid Receptor/MOR

0.6 nM (Ki)

κ Opioid Receptor/KOR

4.9 nM (Ki)

δ Opioid Receptor/DOR

2.2 nM (Ki)

体外実験

Methocinnamox binds very tightly to the μ receptor in the mouse brain tissue and has an extremely slow dissociation rate, but it has no effect on the binding sites of the δ and κ receptors[3].
Methocinnamox insurmountable and pseudoirreversible blocks the inhibitory effects of DAMGO (HY-P0210), psychoactive compound and morphine on the accumulation of cAMP in HEK293 cells that have been transfected with human μ-opioid receptor[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Methocinnamox 関連抗体
体内実験

Methocinnamox (10 mg/kg, s.c., single dose) effectively counteracts a variety of effects mediated by morphine (analgesia, respiratory depression, gastrointestinal inhibition, and changes in body temperature) in rats, and the antagonistic effect persists for more than two weeks after a single administration [1].
Methocinnamox (0.0001-10 mg/kg, i.v. or 10 mg/kg, i.v. and s.c, single dose) effectively reverses and protects the respiratory depression caused by psychoactive compound in rats[2].
Methocinnamox (0.32 mg/kg, s.c., single dose, or once every 12 days for 5 doses; 0.032 mg/kg, once daily for 21 days) reduces the self-administration behavior of opioids, but it has no effect on the self-administration of the response to food in rhesus monkeys[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Paw inflammation and mechanical sensitivity, gastrointestinal transit and physical dependence and withdrawal model established in male Sprague-Dawley rats[1]
Dosage: 10 mg/kg
Administration: Subcutaneous injection (s.c.), single dose
Result: Significantly reduced the analgesic effect of morphine on paw inflammation and this antagonistic effect persisted for at least 15 days.
Blocked the increase in body temperature caused by morphine, with the effect lasting for more than 15 days.
Completely blocked the inhibitory effect of morphine on gastrointestinal peristalsis until 21 days.
Did not result in a longer or more severe withdrawal syndrome.
Animal Model: Reversal of psychoactive compound assay established in adult male Sprague-Dawley rats[2]
Dosage: 0.0001, 0.001, 0.01, 0.1, 1, 10 mg/kg (i.v.) and 10 mg/kg (i.v.) and (s.c)
Administration: Intravenous injection (i.v.) and subcutaneous injection (s.c.), single dose
Result: Dose-dependently rapidly reversed severe respiratory depression.
Provide long-lasting protection and effectively prevent the "re-anesthesia" phenomenon that occurs after rescue.
Exhibited a significantly longer duration of action when administered subcutaneously (s.c.) compared to intravenous (i.v.) administration at the same dose.
Animal Model: Self-Administration model established in rhesus monkeys[3]
Dosage: 0.032 mg/kg and 0.32 mg/kg
Administration: Subcutaneous injection (s.c.), single dose, or once every 12 days for 5 doses (0.32 mg/kg); once daily for 21 days (0.032 mg/kg)
Result: Effectively and selectively blocked the reinforcing effects (euphoria) of opioid agent.
Reduced the relative reinforcing value of opioid drugs, making non-drug rewards (such as food) more attractive.
Did not impair advanced cognitive functions such as working memory or attention.
had no significant effect on the cardiovascular system and body temperature regulation at 3.2 mg/kg.
分子量

484.59

分子式

C30H32N2O4
CAS 番号
SMILES

O=C(CC1)[C@]([C@@](C2=C(C[C@H]3N4CC5CC5)C=C6)(CC4)[C@@]13NC(/C=C/C7=CC=C(C)C=C7)=O)([H])OC2=C6O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Methocinnamox Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Methocinnamox117339-76-1M-CAMOpioid ReceptorBehavioral pharmacologymethocinnamoxopioid use disorderopioidsoverdoseInhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

  

カスタマ需要量 *

お名前 *

 

タイトル

メールアドレス *

 

電話番号 *

デパートメント

 

組纖名 *

市区町村

都道府県

国或いは地域 *

      

必ず会社名を記載ください。個人への返信は行いません。

備考

バルクお問い合わせ

Inquiry Information

製品名:
Methocinnamox
製品番号:
HY-135698
数量:
MCE 日本正規代理店:

カスタマーレビュー

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

製品名

  

Lot #

お名前 *

 

メールアドレス *

電話番号 *

 

部門 *

組纖名 *

 

国或いは地域 *

備考

Request for HNMR Report

We have received your request and will respond to you as soon as possible.