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(Z)-5-tetradecen-1-ol, Potential female sex attractant
(Z)-5-Tetradecen-1-ol, mw 212.37, formula C14H20O CAS 40642-42-0
Odorant receptors, present on nasal sensory neurons, perceive volatile compounds and regulate animal behavior such as reproduction. The nature of the ligands interacting with these receptors is, however, largely unknown.
Keiichi Yoshikawa and colleagues, University of Tokyo, Japan, shed new light on this issue. The researchers demonstrated that, in mice, preputial gland cells generate and secrete into the urine the unsaturated aliphatic alcohol (Z)-5-tetradecen-1-ol (pictured). This compound is regulated by the male hormone testosterone and acts as a natural agonist of the mouse odorant receptor Olfr288, affecting attractiveness to female mice. The urine of males lacking (Z)-5-tetradecen-1-ol, in fact, failed to attract females.
By identifying a novel receptor-ligand interaction in the mouse olfactory system, this study offers new insights into the complex chemistry regulating reproductive behavior.
- An unsaturated aliphatic alcohol as a natural ligand for a mouse odorant receptor,
K. Yoshikawa, H. Nakagawa, N. Mori, H. Watanabe, K. Touhara,
Nature Chem. Biol. 2013.
DOI: 10.1038/nchembio.1164 - Ohloff, G. et al. 1977. Helv. Chim. Acta. 60:1161-1174.
- http://www.cas-msds.com/40642-42-0
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Bestmann, H.J., Brosche, T., Koschatzky, K.H., Michaelis, K., Platz, H., Vostrowsky, O., and Knauf, W. 1980. Pheromone XXX. Identifizierung eines neuartigen pheromonkomplexes aus der graseule Scotia exclamationis. Tetrahedron Lett. 21:747-750. Kelkar, S.V., Reddy, G.B., and Kulkarni, G.H. 1989. Indian J. Chem. Sect. B. 28:980-981. Ohloff, G., Vial, C., Näf, F., and Pawlak, M. 1977. Stereoselective syntheses of the isomeric 5, 10-pentadecadienals. Helv. Chim. Acta. 60:1161-1174.
DR ANTHONY MELVIN CRASTO Ph.D
ARTEMISININ AN ACE ANTIMALARIAL
Artemisinin
by ANTHONY MELVIN CRASTO Ph.D on Jan 20, 2012
- 956 views as on 12 may2013
Anthony Melvin Crasto presents Artemisinin, Glenmark scientist helping millions
amcrasto@gmail.com
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Brazilian scientists have created a synthetic protein that could one day lead to a vaccination against poisonous spider venom.
Brazilian scientists have created a synthetic protein that could one day lead to a vaccination against poisonous spider venom.
Biotie Announces Start of Clinical Study With Nepicastat (SYN117) in Cocaine Dependence
NEPICASTAT
TURKU, FINLAND–BIOTIE THERAPIES CORP. STOCK EXCHANGE RELEASE 10 May 2013 at 9.00 a.m.
Biotie announces start of clinical study with nepicastat (SYN117) in cocaine dependence
Biotie Therapies today announced the start of a Phase 2 clinical study evaluating nepicastat (SYN117) in cocaine dependence. The National Institute on Drug Abuse (NIDA) at the US National Institutes of Health is funding the conduct of the study under a Collaborative Research and Development Agreement (CRADA) signed in December 2011.
The study is a randomized, double-blind placebo-controlled 11-week trial and is expected to enroll about 180 treatment-seeking cocaine-dependent subjects. The study will be conducted at approximately 12 US clinics specializing in the treatment of drug dependence.
The trial is expected to take approximately two years to complete.
ABOUT NEPICASTAT (SYN117)
Nepicastat is an orally administered, potent and selective inhibitor of the enzyme dopamine beta-hydroxylase (DBH) which converts dopamine into norepinephrine. Like many other addictions, cocaine dependence is driven by dysregulation in the dopamine-reward system. Inhibition of DBH by nepicastat increases levels of dopamine, which may reduce craving for cocaine, and reduces the levels of norepinephrine, which may decrease the pleasurable responses to cocaine and the potential for stress-induced relapse following withdrawal. Biotie has previously conducted a placebo-controlled Phase 2a study in non-treatment seeking cocaine addicts. The study showed that nepicastat had a favourable safety profile and was well tolerated when administered with cocaine.
Nepicastat has also been evaluated as a potential treatment for post-traumatic stress disorder (PTSD). In December 2012, Biotie announced top-line data from an investigator-initiated Phase 2 study in PTSD. In this study, nepicastat was generally well tolerated but was not effective in relieving PTSD-associated symptoms when compared to placebo. Biotie is evaluating data from this study in further detail and will then decide on next steps with nepicastat in PTSD
Biotie holds full rights to nepicastat and will be able to use data from studies conducted with NIDA to support future potential regulatory submissions.
ABOUT BIOTIE
Biotie is a specialized drug development company focused on the development of drugs for neurodegenerative and psychiatric disorders (e.g. Parkinson’s disease, Alzheimer’s disease and other cognitive disorders, alcohol and drug dependence (addiction) and post-traumatic stress disorder), and inflammatory and fibrotic liver disease. The company has a strong and balanced development portfolio with several innovative small molecule and biological drug candidates at different stages of clinical development. Biotie’s products address diseases with high unmet medical need and significant market potential.
Biotie’s most advanced product, Selincro (nalmefene), licensed to H. Lundbeck A/S, has on 28 February 2013 received European marketing authorization for the reduction of alcohol consumption in adult patients with alcohol dependence who have a high level of alcohol consumption. In addition, Biotie has a strategic collaboration with UCB Pharma S.A. covering tozadenant which is transitioning into Phase 3 development for Parkinson’s disease. Biotie shares are listed on NASDAQ OMX Helsinki Ltd.
Nepicastat (INN, codenamed SYN117, RS-25560-197) is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.[1]
It has been studied as a possible treatment for congestive heart failure, and appears to be well tolerated as such.[2] As of 2012, clinical trials to assess nepicastat as a treatment forpost-traumatic stress disorder (PTSD) and cocaine dependence have been completed.[3][4]
Synthesis
- Stanley WC, Li B, Bonhaus DW, et al. (August 1997). “Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase”. Br J Pharmacol 121 (8): 1803–9. doi:10.1038/sj.bjp.0701315.PMC 1564872. PMID 9283721.
- Hegde SS, Friday KF (December 1998). “Dopamine-beta-hydroxylase inhibition: a novel sympatho-modulatory approach for the treatment of congestive heart failure”. Current pharmaceutical design 4 (6): 469–79. PMID 10197057.
- “Pharmacogenetic Clinical Trial of Nepicastat for Post Traumatic Stress Disorder (PTSD)”. ClinicalTrials.gov. U.S. National Institutes of Health. June 4, 2008. Retrieved on February 1, 2012.
- “Study of Safety and Potential Efficacy of SYN117 in Cocaine Dependent Volunteers”. ClinicalTrials.gov. U.S. National Institutes of Health. August 15, 2008. Retrieved on February 1, 2012.
Hutchison Chi-Med in Partner Talks for Cancer Drug
WO-2011060746 Compound, certain novel forms thereof, pharmaceutical compositions thereof and methods for preparation and use
may give you the structure
May 9, 2013
Hutchison Chi-Med expects to license global rights to fruqintinib, one of its novel small-cell cancer drugs, before year-end, according to CEO Christian Hogg.
The company has been in due diligence discussions with potential partners, he added. Because the drug is a promising treatment for solid tumors,
Chi-Med will conduct simultaneous clinical trials against several types of cancer, and the company wants a partner to help shoulder the financial burden
Hutchison China MediTech Ltd. (HCM), the drugmaker controlled by Hong Kong billionaire Li Ka-shing, is in talks to license a cancer treatment based on traditional Chinese medicines, Chief Executive Officer Christian Hogg said.
The Hong Kong-based company, known as Chi-Med, completed due diligence with potential partners and will probably reach an agreement on fruquintinib by year-end, Hogg said yesterday in an interview in London, where the shares trade. The medicine may be used to treat colorectal, lung, breast and gastric cancers, he said.
“A deal on fruquintinib is a pretty important priority,” Hogg said. “What we want to do is partner and take on in parallel clinical programs in all of those tumor types.”
A licensing agreement on fruquintinib, which has completed early-stage testing, would follow a joint venture with Nestle SA (NESN), which last month said it has started late-stage trials of HMPL-004 for ulcerative colitis. Chi-Med is aiming to be the first drugmaker to bring to market pharmaceutical products from traditional Chinese botanicals.
Fruquintinib will probably be the last product for which Chi-Med will grant global marketing rights to a partner, with subsequent agreements giving Chi-Med the rights to China, Hogg said. China’s pharmaceutical market is expected to grow as much as 18 percent a year to $165 billion by 2016, making it the world’s second-largest market after the U.S., according to consultancy IMS Health Inc.
PTC Therapeutics’ large-scale multinational trial of ataluren for nonsense-mutation Duchenne or Becker MD has opened its first site in Cincinnati, Ohio
ATALUREN
A large-scale, multinational, phase 3 trial of the experimental drug ataluren has opened its first trial site, in Cincinnati, Ohio.
The trial is recruiting boys with Duchenne muscular dystrophy (DMD) or Becker muscular dystrophy (BMD) caused by anonsense mutation — also known as a premature stop codon — in the dystrophin gene. This type of mutation causes cells to stop synthesizing a protein before the process is complete, resulting in a short, nonfunctional protein. Nonsense mutations are believed to cause DMD or BMD in approximately 10 to 15 percent of boys with these disorders.
Ataluren — sometimes referred to as a stop codon read-through drug — has the potential to overcome the effects of a nonsense mutation and allow functional dystrophin — the muscle protein that’s missing in Duchenne MD and deficient in Becker MD — to be produced.
The orally delivered drug is being developed by PTC Therapeutics, a South Plainfield, N.J., biotechnology company, to whichMDA gave a $1.5 million grant in 2005.
Ataluren, formerly known as PTC124, is a novel small-molecular agent designed to makeribosomes become less sensitive to, or possibly ignore premature stop codons. This may be particularly beneficial in genetic disorders where the mRNA contains a mutation causing premature stop codon or nonsense codon. However, it is not equally effective with every stop codon, working best on the sequence ‘UGA’.
PTC124 has been tested on healthy humans and humans carrying genetic disorderscaused by nonsense mutations,such as some people with cystic fibrosis andDuchenne muscular dystrophy. Clinical trials are proceeding for several genetic disorders, in the subset of affected people who have nonsense mutations (typically <10% of those with the disorder). PTC Therapeutics released preliminary results of its phase 2b clinical trial for Duchenne muscular dystrophy, with participants not showing a significant improvement in the six minute walk distance after the 48 weeks of the trial.However, phase 2 clinical trials were successful for cystic fibrosis in Israel, France and Belgium.Multicountry phase 3 clinical trials are currently in progress for cystic fibrosis in Europe and the USA.
PTC124 has been developed by PTC Therapeutics.
SILDENAFIL, VIAGRA REVIEW
Sildenafil by Anthony Crasto
by ANTHONY MELVIN CRASTO Ph.D on May 11, 2013
- FRESHLY LOADED ON SLIDESHARE
Sildenafil by DR ANTHONY CRASTO, WORLDDRUGTRACKER
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COLCHININE
Anthony crasto colchinine
by ANTHONY MELVIN CRASTO Ph.D on Apr 06, 2012
- 468 views
Anthony crasto presents colchinine review
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Drug Design:Discovery, Development and Delivery
Drug Design:Discovery, Development and Delivery
by Dr. Basavaraj Nanjwade
http://www.slideshare.net/bknanjwade/drug-designdiscovery-development-and-delivery
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HERBAL AND DRUG DESIGN TECHNOLOGY
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an introduction to drug discovery ON SLIDESHARE
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DR ANTHONY MELVIN CRASTO
ORGANIC SPECTROSCOPY
New Drug Approvals 