Wednesday, December 4, 2013

Melanotan 2 info



MOLECULAR FORMULA : C50H69N15O9 MOLECULAR WEIGHT : 1024.2 CAS NO. : 121062-08-6

SEQUENCE: AC-NLE-ASP-HIS-D-PHE-ARG-TRP-LYS-NH2(CYCLIC 2-7)

DEVELOPED AT THE UNIVERSITY OF ARIZONA. FOR RESEARCH PURPOSES ONLY.

A PILOT PHASE I CLINICAL TRIAL CONDUCTED ON THREE MALES USING MT-2 BY THE COLLEGE OF MEDICINE, PHARMACOLOGY DEPARTMENT, UNIVERSITY OF ARIZONA IN TUCSON, ARIZONA PUBLISHED IN 1996 REPORTED THAT, "MT-2" HAS TANNING ACTIVITY IN HUMANS GIVEN ONLY 5 LOW DOSES EVERY OTHER DAY BY SUBCUTANEOUS INJECTION. ((MILD SIDE EFFECTS REPORTED INCLUDED SLIGHT NAUSEA AND INCREASED SPONTANEOUS PENILE ERECTIONS.
THE DEPARTMENT OF PHARMACOLOGY, UNIVERSITY OF ARIZONA COLLEGE OF MEDICINE PUBLISHED A STUDY IN 1998 THAT INVOLVED TEN MEN WHO SUFFERED FROM PSYCHOGENIC ERECTILE DYSFUNCTION. THEIR TRIAL CONCLUDED THAT, "MELANOTAN-II IS A POTENT INITIATOR OF ERECTIONS IN MEN WITH PSYCHOGENIC ERECTILE DYSFUNCTION AND HAS MANAGEABLE SIDE EFFECTS AT A DOSE OF 0.025 MG./KG." [14]
A CLINICAL STUDY PUBLISHED IN 2000 OF 20 MEN WITH PSYCHOGENIC AND ORGANIC ERECTILE DYSFUNCTION CONDUCTED AT THE SECTION OF UROLOGY OF THE UNIVERSITY OF ARIZONA COLLEGE OF MEDICINE CONCLUDED, "THAT MELANOTAN II IS A POTENT INITIATOR OF PENILE ERECTION IN MEN WITH ERECTILE DYSFUNCTION." [15]

AFTER SYNTHESIZING AND SCREENING HUNDREDS OF MOLECULES, THE RESEARCHERS HEADED BY DR. VICTOR HRUBY, FOUND A PEPTIDE THAT AFTER TRIALS AND TESTING SEEMED TO NOT ONLY BE SAFE BUT ALSO APPROXIMATELY 1,000 TIMES MORE POTENT THAN NATURAL Α-MSH. THEY DUBBED THIS NEW PEPTIDE MELANOTAN-II (MT-2). SINCE THEIR DISCOVERY, NUMEROUS STUDIES DATING BACK TO THE MID-1980S HAVE SHOWN NO OBVIOUS TOXIC EFFECTS OF MELANOTAN-2. BECAUSE SKIN CANCER (MELANOMA) TODAY IS A MAJOR HEALTH CONCERN, MELANOTAN II (MT-2) IS EXPECTED TO BE USED AS A DRUG TO COMBAT IT. MT-2 WILL DO THIS BY STIMULATING THE BODY'S NATURAL TANNING MECHANISM TO CREATE A TAN WITHOUT FIRST NEEDING EXPOSURE TO HARMFUL LEVELS OF UV RADIATION. THIS IN TURN WILL REDUCE THE POTENTIAL FOR SKIN DAMAGE THAT CAN EVENTUALLY LEAD TO SKIN CANCER.

MELANOTAN-II (MT-2) IS A CYCLIC HEPTAPEPTIDE ANALOG OF THE ALPHA-MELANOCYTE STIMULATING HORMONE (A-MSH), WITH THE FOLLOWING MOLECULAR STRUCTURE:

IT HAS BEEN DESCRIBED TO HAVE SUPERPOTENT MELANOTROPIC ACTIVITY IN VITRO. ITS EFFECT ON TANNING, LIKE THE EFFECT OF ITS SIMILAR PEPTIDE MELANOTAN I, WAS ALSO INVESTIGATED (DORR ET AL. 1996).

THE EFFECTS OF MELANOTAN II ON THE DIET AND FOOD INTAKE OF THE LABORATORY MICE HAVE ALSO BEEN INVESTIGATED. IT HAS BEEN DEMONSTRATED THAT THE CENTRAL MELANOCORTIN (MC) HAS BEEN ACTIVATED BY MELANOTAN II WHEN FED AND INDUCED IN THE MICE. THE SIX-DAY TREATMENT OF MT-2 HAS SHOWN THAT MELANOTAN II ACTUALLY REDUCED THE BODY WEIGHT AND THE ADIPOSE TISSUE IN THE VISCERA OF THE MICE AND SUPPRESSED THE CALORIC INTAKE OF THE ORGANISM. THIS HAS IMPLICATIONS IN CLINICAL APPLICATIONS OF THE POSSIBLE TREATMENT TO REDUCE CARBOHYDRATE OR CALORIE INTAKE ESPECIALLY FOR THE OVERWEIGHT AND THE OBESE. FURTHERMORE, THE SAME STUDY HAS ALSO DEMONSTRATED THAT THERE WAS A SUSTAINED INCREASE IN THE AVAILABLE OXYGEN CONSUMPTION IN OBESE ANIMALS. MELANOTAN II (MT-2) ALSO HELPED REDUCED THE LEVEL OF SERUM INSULIN AND THE CHOLESTEROL LEVELS WHEN COMPARED WITH THE CONTROL TREATMENTS. FURTHERMORE, IT HAS BEEN SUGGESTED THAT MELANOTAN ACTUALLY LOWERS THE LEVEL OF ACETYLCHOLINE A CABOXYLASE EXPRESSION AND EVEN PREVENTED THE REDUCTION OF CARNITINE AND PALMITOLTRANSFERASE I MRNA IN MUSCLE-TYPE TISSUES BY PAIR-FEEDING IN THE MUSCLES OF THE OBESE RATS. MOREOVER, THE MELANOTAN II ACTUALLY INCREASED THE FAT CATABOLISM IN THE MUSCLES AND EVEN IMPROVED THE CHOLESTEROL METABOLISM (LI ET AL. 2004).

ANOTHER STUDY THAT HAS IMPLICATIONS FOR CLINICAL APPLICATIONS IS THE TREATMENT OF MELANOTAN II (MT-2) AND ITS EFFECT ON SEXUAL STIMULATION AND MOTIVATION ALONG WITH ENHANCED ERECTIONS IN ANIMALS AND HUMANS. IN A STUDY CONDUCTED BY WESSELLS ET AL. (2000), THEY HAVE SHOWN THAT MELANOTAN II (MT-2) ACTUALLY INCREASED SEXUAL DESIRE AND EVEN CONCLUDED THAT MELANOTAN II (MT-2) IS A POTENT INITIATOR OF PENILE ERECTION IN MEN ESPECIALLY WITH THAT OF ERECTILE DYSFUNCTION.
OTHER CHEMICAL ACTIVITIES OF MELANOTAN II (MT-2) WHEN TESTED IN VIVO ARE INHIBITION OF FEEDING, SUPPRESSION OF NPY OREXIGENIC ACTION AND REDUCTION IN BASAL INSULINAEMIA (RAPOSINHO ET AL. 2003). 

MELANOTAN AND MELANOTAN II ARE BOTH ANALOGS OF THE PEPTIDE HORMONE ALPHA-MELANOCYTE STIMULATING HORMONE (Α-MSH) THAT TEND TO INDUCE SKIN TANNING. UNLIKE MELANOTAN THOUGH, MELANOTAN II (MT-2) HAS BEEN SHOWN TO HAVE THE ADDITIONAL EFFECT OF INCREASING LIBIDO. MELANOTAN II (MT-2) HAS BEEN SHOWN TO HAVE APHRODISIAC PROPERTIES.

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