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A 4 th G eneration A ntipsychotic and S exual E ntactogenic D rug ( M arketing B rief). A N ew W ay in E motional D isorders and S ex ual T herapy Authors: Simon, Lehel & Répási, József Main scientific source and expert: Dr. Molnár, László.
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A 4thGeneration Antipsychotic and Sexual Entactogenic Drug (Marketing Brief) A New Way in Emotional Disorders and Sexual Therapy Authors: Simon, Lehel& Répási, József Main scientific source and expert: Dr. Molnár, László
The Starting Point of the Medicine: The Expected Hit • V1/V3 antagonist Manning- peptide: • X=D-Tyr-Phe-Val-Asn-Arg-Pro-Arg-Arg-NH2 • http://endo.endojournals.org/content/138/10/4109.full.pdf • It is a free source molecule, what we would like to test pharmacodinamically. Our aim to develope a PET tracer with Fluor18 dervative of this peptide. In this way we could test the receptoraffinity, so it is possible a research with other analogues molecules of AVP
The API • Our molecule is relatively simple peptide • It could be produced in standard peptide labs or manufacturing facilities • The molecule is derived from a free source (see attached file),YOU CAN OPEN IT IN OUTLOOK • http://books.google.hu/books?id=3VH5kb1DEGUC&pg=PA153&lpg=PA153&dq=D-Tyr-Phe-Val-Asn-Arg-Pro-Arg-Arg-NH2&source=bl&ots=-2vrDltgyx&sig=JV_0C1Sz_4yyofv_Yoy5QtRHhy8&hl=hu&ei=T6QdTayWIcaD5Abggd2GAg&sa=X&oi=book_result&ct=result&sqi=2&redir_esc=y#v=onepage&q=D-Tyr-Phe-Val-Asn-Arg-Pro-Arg-Arg- • NH2&f=false • but the therapeutic use could be patented
Is it a Hormone? • It is similar to hormones, but it doesn't have hormonal effects like steroids, because it does not have any effects on V2 renal receptors. Other researchers determined the receptoraffinities - see attached links • http://joe.endocrinology-journals.org/content/141/3/383.abstract • http://www.ncbi.nlm.nih.gov/pubmed/8071638 • This is analogue to a hormone AVP • and expectedto act mainly in the brain
Potential Applications of the Medicine • It is a fairlystablepeptide and could be usedinintravenousinjection or as a transdermal patch Primary suggested usage: therapy ofnegativism (autisms and adults’ negativisticdisorders) Other major application: sextherapy Thesearevalidinallmammals, see http://www.ncbi.nlm.nih.gov/pubmed/9951561 http://www.ncbi.nlm.nih.gov/pubmed/22141469 http://www.ncbi.nlm.nih.gov/pubmed/18655893
Cost and Value • The market value of this drug is huge, because only micrograms are needed from the drug, and it can be produced from very cheap ingredients using standard peptide synthesis procedures.It verified our thesis, that far less receptors are in the brain, than in the kidney; and the V2 (renal) vasopressin-agonist desmopressin’s dose is 0, 1-0,6 mg
Cost and Value • It is very economical: the expected manufacturing cost in industrial scale would be tens of thousand USD/kg • In comparison rats received from the concurrent complicated polycyclic • The expected dose is 10-100 μg/kg • SSR vaptans are used in 10-30 mg/kgdose
Experimental Introduction • We would like the experimental introduction of this molecule from other direct researches: • http://www.ncbi.nlm.nih.gov/pubmed/8071638http://joe.endocrinology-journals.org/cgi/content/abstract/141/3/383 • The estimated cost of proof of concept workexpected to bein the range of 1 - 1,5 million dollars plus the experimental cost - see attached file