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A 4th Generation 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-ArgNH2 X O 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 receptor affinity, 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&d q=D-Tyr-Phe-Val-Asn-Arg-Pro-Arg-Arg-NH2&source=bl&ots=2vrDltgyx&sig=JV_0C1Sz_4yyofv_Yoy5QtRHhy8&hl=hu&ei=T6QdTayWIc aD5Abggd2GAg&sa=X&oi=book_result&ct=result&sqi=2&redir_esc=y#v= onepage&q=D-Tyr-Phe-Val-Asn-Arg-Pro-Arg-ArgNH2&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 receptor affinities - 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 expected to act mainly in the brain Potential Applications of the Medicine It is a fairly stable peptide and could be used in intravenous injection or as a transdermal patch Primary suggested usage: therapy of negativism (autisms and adults’ negativistic disorders) Other major application: sextherapy These are valid in all mammals, 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/kg dose Experimental Introduction • We would like the experimental introduction of this molecule from other direct researches: • http://www.ncbi.nlm.nih.gov/pubmed/8071638 http://joe.endocrinology-journals.org/cgi/content/abstract/141/3/383 • The estimated cost of proof of concept work expected to be in the range of 1 - 1,5 million dollars plus the experimental cost - see attached file