Gene Encoding the 5HT2C Receptor

The gene encoding the 5-HT2C receptor is extraordinarily complex, which explains why it has taken quite some time to obtain the full sequence (see reference Lubbert et al. 1987). There are three splice variants of the 5-HT2C receptor: the full length receptor and two severely truncated forms (Canton et al. 1996), thought to be inactive. In addition, it has become clear that the primary transcript undergoes RNA editing (Burns et al. 1997), something that is unheard of on the GPCR field but was described for ionotropic glutamate receptors of the AMPA type. In rodents there are four editing sites within the coding region, whereas in humans a fifth editing site is present; together they may produce up to 32 different mRNAs and 24 different proteins. The 5-HT2C receptor is characterized by constitutive activity, the level of which decreases as editing increases (Herrick-Davis et al. 1999). Editing also leads to a loss of the active state of the receptor (Niswender et al. 1999) and a delay in agonist-stimulated calcium release in the fully edited isoforms (Price and SandersBush 2000). The fully edited receptor couples to both Gq/11 and G13, whereas editing reduces or eliminates coupling to G13 (Price et al. 2001). Thus, editing may serve to stop constitutive activity by reducing coupling to G proteins.

Defeat Drugs and Live Free

Defeat Drugs and Live Free

Being addicted to drugs is a complicated matter condition that's been specified as a disorder that evidences in the obsessional thinking about and utilization of drugs. It's a matter that might continue to get worse and become disastrous and deadly if left untreated.

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