HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Gastric pentadecapeptide BPC 157 effective against serotonin syndrome in rats.

Abstract
Serotonin syndrome commonly follows irreversible monoamine oxidase (MAO)-inhibition and subsequent serotonin (5-HT) substrate (in rats with fore paw treading, hind limbs abduction, wet dog shake, hypothermia followed by hyperthermia). A stable gastric pentadecapeptide BPC 157 with very safe profile (inflammatory bowel disease clinical phase II, PL-10, PLD-116, PL-14736, Pliva) reduced the duration of immobility to a greater extent than imipramine, and, given peripherally, has region specific influence on brain 5-HT synthesis (alpha-[14C]methyl-L-tryptophan autoradiographic measurements) in rats, different from any other serotonergic drug. Thereby, we investigate this peptide (10 microg, 10 ng, 10 pg/kg i.p.) in (i) full serotonin syndrome in rat combining pargyline (irreversible MAO-inhibition; 75 mg/kg i.p.) and subsequent L-tryptophan (5-HT precursor; 100 mg/kg i.p.; BPC 157 as a co-treatment), or (ii, iii) using pargyline or L-tryptophan given separately, as a serotonin-substrate with (ii) pargyline (BPC 157 as a 15-min posttreatment) or as a potential serotonin syndrome inductor with (iii) L-tryptophan (BPC 157 as a 15 min-pretreatment). In all experiments, gastric pentadecapeptide BPC 157 contrasts with serotonin-syndrome either (i) presentation (i.e., particularly counteracted) or (ii) initiation (i.e., neither a serotonin substrate (counteraction of pargyline), nor an inductor for serotonin syndrome (no influence on L-tryptophan challenge)). Indicatively, severe serotonin syndrome in pargyline + L-tryptophan rats is considerably inhibited even by lower pentadecapeptide BPC 157 doses regimens (particularly disturbances such as hyperthermia and wet dog shake thought to be related to stimulation of 5-HT2A receptors), while the highest pentadecapeptide dose counteracts mild disturbances present in pargyline rats (mild hypothermia, feeble hind limbs abduction). Thereby, in severe serotonin syndrome, gastric pentadecapeptide BPC 157 (alone, no behavioral or temperature effect) has a beneficial activity, which is likely, particular, and mostly related to a rather specific counteraction of 5-HT2A receptors phenomena.
AuthorsAlenka Boban Blagaic, Vladimir Blagaic, Mirela Mirt, Nikola Jelovac, Goran Dodig, Rudolf Rucman, Marijan Petek, Branko Turkovic, Tomislav Anic, Miroslav Dubovecak, Mario Staresinic, Sven Seiwerth, Predrag Sikiric
JournalEuropean journal of pharmacology (Eur J Pharmacol) Vol. 512 Issue 2-3 Pg. 173-9 (Apr 11 2005) ISSN: 0014-2999 [Print] Netherlands
PMID15840402 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Anti-Ulcer Agents
  • Antidepressive Agents, Second-Generation
  • Monoamine Oxidase Inhibitors
  • Peptide Fragments
  • Proteins
  • Tryptophan
  • BPC 157
  • Pargyline
Topics
  • Animals
  • Anti-Ulcer Agents (pharmacology, therapeutic use)
  • Antidepressive Agents, Second-Generation (pharmacology, therapeutic use)
  • Behavior, Animal (drug effects)
  • Body Temperature (drug effects)
  • Dose-Response Relationship, Drug
  • Drug Therapy, Combination
  • Male
  • Monoamine Oxidase Inhibitors (pharmacology, therapeutic use)
  • Pargyline (pharmacology, therapeutic use)
  • Peptide Fragments (pharmacology, therapeutic use)
  • Proteins (pharmacology, therapeutic use)
  • Rats
  • Rats, Wistar
  • Serotonin Syndrome (pathology, prevention & control)
  • Time Factors
  • Treatment Outcome
  • Tryptophan (pharmacology, therapeutic use)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: