Posted by Brainbeard on May 28, 2010, at 15:37:58
In reply to 5HT2A-antagonism + 5HT2C-agonism Would Be Ideal, posted by Brainbeard on May 28, 2010, at 15:17:55
Quotes from mentioned article:
'Interactions have also been observed between 5-HT2A and 5-HT2C receptors at a behavioral level. Opposing effects exist for 5-HT2A and 5-HT2C receptors in modulating hyperlocomotion induced in mice by noncompetitive N-methyl-d-aspartate (NMDA) antagonists (Martin et al, 1997). A recent study has found clear evidence supporting opposing effects of 5-HT2A and 5-HT2C receptors in modulating head shakes in rats (Vickers et al, 2001). Activation of 5-HT2A and 5-HT2C receptors also leads to opposing effects on sexual function in rodents (Berendsen et al, 1990), in a manner suggesting that activation of 5-HT2A receptors could be responsible for the sexual side effects of SSRIs. DRL 72-s behavior also appears to involve reciprocal interactions between 5-HT2A and 5-HT2C receptors, since 5-HT2C agonists, similar to 5-HT2A antagonists, exert antidepressant-like actions in rats performing under this operant paradigm (Marek and Seiden, 1988; Martin et al, 1998; Marek et al, 2001a). In a similar vein, blockade of 5-HT2C receptors may attenuate the antidepressant-like effects observed on the DRL 72-s schedule following administration of drugs that block 5-HT2A receptors (Marek and Seiden, 1994).'
.....
'Activation of 5-HT2C receptors appears to cause effects that functionally oppose the effects resulting from activation of 5-HT2A receptors (see above). These two receptors are differentially regulated by antidepressants in a manner that could have clinical relevance (Berendsen and Broekkamp, 1991). Other preclinical work in rodents has found that 5-HT2C agonists have antidepressant-like action in the forced swim test, the olfactory bulbectomy model, and the DRL 72-s schedule (Martin et al, 1998; Cryan and Lucki, 2000). Moreover, a polymorphism for the 5-HT2C receptor has been linked to mood disorders (Lerer et al, 2001). This might result in an alteration of 5-HT2C function independent of receptor abundance. Alterations in RNA editing of 5-HT2C receptors has been reported in suicide victims (Niswender et al, 2001). Thus, simultaneous blockade of 5-HT2A receptors and activation of 5-HT2C receptors could result in an improved therapeutic benefit over either of these actions in isolation.'
Current meds: 10mg melitracene + 0.5mg flupentixol; sertraline 100mg; amitriptyline 25mg; gabapentin (Neurontin) 300mg; melatonin 0.3mg. PRN: diazepam (Valium) 2.5-5mg.
poster:Brainbeard
thread:948688
URL: http://www.dr-bob.org/babble/neuro/20100223/msgs/949281.html