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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