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Alpha-MSH analog for curing sexual disorder and preparation method

A technology of sexual function and analogs, applied in the field of α-MSH analogs and preparations for the treatment of sexual dysfunction, can solve problems such as unsatisfactory treatment measures, achieve the effects of reducing effective doses, improving biological activity, and avoiding side effects

Inactive Publication Date: 2005-01-12
西南生物工程产业化中试基地有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these treatments are not ideal, and it is urgent to find a new treatment method

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: Synthesis of SEQ ID NO: 1 polypeptide by solid-phase synthesis

[0026] The polypeptide of SEQ ID NO: 1 is synthesized by a standard solid-phase synthesis method, and the polypeptide exists in the form of acetate.

[0027](1) Add 2.0 grams of P-HMPA-AM (0.8 mmol / g) resin (Jill Biochemical Co., Ltd.) Amide washes, 2 minutes each. (2) Add 20 milliliters of dimethylformamide and mechanically shake for 10 minutes, add three times the amount of amino acid derivative Fmoc-Lys(Dnp)-OH (CS Biochemical Company, USA) and 2.1 milliliters of HOBt (Gill Biochemical Co., Ltd. ), shake for 2-3 hours. (3) Ninhydrin test was negative. (4) Wash the product with 4 portions of 20 ml of dimethylformamide for 2 minutes each time. (5) Add 20 ml of 20% piperidine / dimethylformamide and shake for 1 minute, then add 20 ml of 20% piperidine / dimethylformamide and shake for 30 minutes. (6) Wash the product with 20 ml of 4 parts of dimethylformamide, 2 minutes each time. (7) Wash ...

Embodiment 2

[0029] Embodiment 2: The polypeptide of SEQ ID NO:2 is synthesized by solid-phase synthesis

[0030] (1) Add 2.0 grams of P-MBHA resin (0.7 mmol / g) (Gill Biochemical Co., Ltd.) and 20 milliliters of dimethylformamide into the reactor (CS Biochemical Company, CS736 type), mechanically shake for 10 minutes After that, three times of Boc-Lys(2-C1-Z) (Gill Biochemical Co., Ltd.) and the same amount of HOBt were added, and the mixture was shaken mechanically at room temperature for 3 hours. (2) Detection of ninhydrin. If the test result is positive, react for another 1 hour. If it is still positive, use acetic anhydride / pyridine / dichloromethane (1:1:2 V / V) twice as much as the resin, and react for 30 minutes at room temperature to remove excess amino groups. . (3) Ninhydrin test was negative. (4) Wash the product with 2 20 mL portions of dichloromethane for 1 minute each. (5) Cleavage and removal of the protecting group Boc with 30 ml of 50% trifluoroacetic acid / dichloromethane...

Embodiment 3

[0032] Example 3: Effects of α-MSH analogue SEQ ID NO: 1 and its C-terminal derivative SEQ ID NO: 2 on the sexual function of mice.

[0033] The experimental animals are rats. Experimental reagents include SEQ ID NO: 1, α-MSH, Ac-[Nle 4 , D-Phe 7 ]-α-MSH 1-13 NH 2 ,, Ac-[Nle 4 , D-Phe 7 Lys 10 ]-α-MSH 4-10 NH 2 , SEQ ID NO: 2 (synthesized by the method provided in Examples 1 and 2).

[0034] The administration method of the above five reagents is intravenous injection, and the administration dose is 10 μg / kg. Animal experiment There are five groups of rats, 4 rats in each group, and each group of rats is intravenously injected with one of the above five reagents. Observed for 0.5 hours after injection. Rats injected with α-MSH had an erection rate of 5%; injections of Ac-[Nle 4 , D-Phe]-α-MSH 1-13 NH 2 The erection rate of rats was 12%; injection of Ac-[Nle 4 , D-Phe, Lys 10 ]-α-MSH 4-10 NH 2 The erection rate of rats injected with SEQ ID NO: 1 and SEQ ID NO:...

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PUM

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Abstract

The invention discloses an alpha-MSH analogue AC-Nle-cyclo(-Asp-His-D-Phe-Arg-Trg-Lys)-OH(SEQ ID No:1) polypeptide and derivative (SEQ ID No:2) whose C end is umidated for curing sexual dysfunction, and discloses a method for synthesizing the above-mentioned polypeptide, and discloses a medicine composite containing the above-mentioned polypeptide for curing sexual dysfunction and its preparation method, and application of said medicine composite for curing sexual dysfunction diseases, including male sexual dysfunction, for example, erectile dysfunction and female sexual dysfunction.

Description

technical field [0001] The present invention relates to an α-MSH analogue for treating sexual dysfunction, derivatives of the analogue whose C-terminus is amidated and a preparation method of these analogues, and also relates to a drug containing the above-mentioned polypeptide for treating sexual dysfunction combination. Background technique [0002] Sexual dysfunction, including male sexual dysfunction and female sexual dysfunction, is a wide-ranging medical condition. The causes of sexual dysfunction are mental, organic and mixed. Stress, depression, organic diseases such as circulatory system diseases, nervous system damage, arteriosclerosis, diabetes, high blood pressure and high cholesterol can all lead to sexual dysfunction. [0003] In clinical treatment, drug therapy and auxiliary device therapy are mainly adopted according to different etiologies. Now commonly used drugs include sildenafil, vardenafil, etc., and these drugs are all PDE5 inhibitors, which cause c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61P15/08C07K7/06
Inventor 李晓鹏周涛李明
Owner 西南生物工程产业化中试基地有限公司
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