Oti-Adrenoceptor

Lithium (Li) is a common mood stabilizer and it used in the treatment of bipolar disorder. There are numerous evidences that the therapeutic effect of Li is mediated via an inositol triphosphate (IP3) and protein kynase C (PKC)-mediated mechanism (Amsten, 2008). Since the IP3 and PKC are involved the signal transduction pathway of oti -adrenoceptors, it is possible that there receptor are target of Li treatment. Indeed, it has been observed that chronic Li suppress the al-mediated IP3 formation and PKC activation. It has been also observed that chronic Li deregulates al3 a2 and p-adrcnoceptors in the brain (Devaki et al., 2006). 

For the same class of compounds Timmermans determined log Papp values (n-octanol/buffer, pH = 7.4), binding affinities to oti adrenoceptors, ICsoOti (displacement of the oti antagonist prazosin), binding affinities to a2 adrenoceptors, IC5(,a2 (displacement of the 2 agonist clonidine), antihypertensive activities (mediated by a central mechanism) in anesthetized normotensive rats (ED2s%, i v. application), and hypertensive activities (mediated by peripheral a stimulation which, in the absence of central nervous system regulation, causes blood vessel contraction) in... 

Kitazawa T, Hashiba K, Cao J, Unno T, Komori S, Yamada M, Wess J, Taneike T (2007) Functional roles of muscarinic M2 and M3 receptors in mouse stomach motility studies with muscarinic receptor knockout mice. Eur J Pharmacol 554 212-22 Knauber J, Muller WE (2000) Decreased exploratory activity and impaired passive avoidance behaviour in mice deficient for the aiB-adrenoceptor. Eur Neuropsychopharmacol 10 423-7 Koshimizu TA, Tanoue A, Tsujimoto G (2006) Clinical implications from studies of oti adrenergic receptor knockout mice. Biochem Pharmacol. 

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