Wednesday, November 30, 2011

Top 8 Worst Stimulants of All Time

1. Halostachine

2. N-Methyltyramine

3. Tyramine
  • Pros: None
  • Cons: Minimal bioavailability in the presence of gut lumen MAO; Converts to a false neurotransmitter (receptor antagonism) - sympatholytic with chronic supplementation; Strong pressor effect with acute supplementation; Short half life (30 minutes); Depletes vesicular catecholamines; Competitively inhibits catecholamine beta-hydroxylase; No CNS penetration

4. Para-Synephrine ("Synephrine")

5. 3,3'-Diiodo-L-Thyronine

6. 3,5-Diiodo-L-Thyronine
  • Pros: Can help manage hyperthyroidism
  • Cons: Goitrogenic (Directly suppresses the thyroid gland); Less than 3% of the calorigenic activity of T4; No increase in BMR en vivo; Decreases circulating levels of TSH
  • References:
  • (1)  http://endo.endojournals.org/cgi/content/abstract/64/1/62 
  • (2) 3,5-Diiodo-L-thyronine (T2) has selective thyromimetic effects in vivo and in vitro. Journal of Molecular Endocrinolog (1997) 19, 137-147

7. Hordenine
  • Pros: Weak competitive inhibition of MAO-B
  • Cons: Minimal bioavailability; Elimination half-life of 20-30 minutes; No CNS penetration

8. Phenylethylamine
  • Pros: Transient high
  • Cons: Rapidly metabolised (Half-life of 5-10 minutes); No direct receptor agonism; Sympatholytic with chronic supplementation; Competitive inhibitor of beta-hydroxylase