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Chemical Compound Review

PT-141     (3R,6S,9S,12S,23S)-15-[[(2S)- 2...

Synonyms: PT 141, AC1O52UR, 189691-06-3, UNII-6Y24O4F92S, Bremelanotide PT 141
 
 
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Psychiatry related information on PT-141

 

High impact information on PT-141

  • A new MTII analog, PT-141 (Palatin Technologies) has initial phase I/II trials and is scheduled to enter pivotal stage III clinical trials leading to commercialization [3].
  • Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction [4].
  • Evaluation of the safety, pharmacokinetics and pharmacodynamic effects of subcutaneously administered PT-141, a melanocortin receptor agonist, in healthy male subjects and in patients with an inadequate response to Viagra [5].
  • The erectogenic potential of PT-141, its tolerability profile and its ability to cause significant erections in patients who do not have an adequate response to a PDE5 inhibitor suggest that PT-141 may provide an alternative treatment for ED with a potentially broad patient base [5].
  • PT-141, a synthetic peptide analogue of alpha-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R, which are expressed primarily in the central nervous system [1].
 

Chemical compound and disease context of PT-141

  • OBJECTIVES: To evaluate the safety and pharmacodynamic effect of co-administration of subtherapeutic doses of PT-141, a cyclic heptapeptide melanocortin analogue, and sildenafil to patients with erectile dysfunction [6].
 

Biological context of PT-141

 

Anatomical context of PT-141

  • Systemic administration of PT-141 to rats activates neurons in the hypothalamus as shown by an increase in c-Fos immunoreactivity [1].
 

Gene context of PT-141

  • CONCLUSIONS: Co-administration of intranasal PT-141 and a phosphodiesterase type 5 inhibitor may constitute a treatment alternative for patients in whom higher doses of a single therapy are not effective or well tolerated [6].
 

Analytical, diagnostic and therapeutic context of PT-141

References

  1. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Molinoff, P.B., Shadiack, A.M., Earle, D., Diamond, L.E., Quon, C.Y. Ann. N. Y. Acad. Sci. (2003) [Pubmed]
  2. An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist. Diamond, L.E., Earle, D.C., Heiman, J.R., Rosen, R.C., Perelman, M.A., Harning, R. The journal of sexual medicine. (2006) [Pubmed]
  3. Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization. Hadley, M.E., Dorr, R.T. Peptides (2006) [Pubmed]
  4. Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction. Diamond, L.E., Earle, D.C., Rosen, R.C., Willett, M.S., Molinoff, P.B. Int. J. Impot. Res. (2004) [Pubmed]
  5. Evaluation of the safety, pharmacokinetics and pharmacodynamic effects of subcutaneously administered PT-141, a melanocortin receptor agonist, in healthy male subjects and in patients with an inadequate response to Viagra. Rosen, R.C., Diamond, L.E., Earle, D.C., Shadiack, A.M., Molinoff, P.B. Int. J. Impot. Res. (2004) [Pubmed]
  6. Co-administration of low doses of intranasal PT-141, a melanocortin receptor agonist, and sildenafil to men with erectile dysfunction results in an enhanced erectile response. Diamond, L.E., Earle, D.C., Garcia, W.D., Spana, C. Urology (2005) [Pubmed]
 
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