Drugs online research references
Acta Psychiatr Scand Suppl. 1981;290:277-88.
Sedative/anxiolytic effects of antidepressants in animals.
Ogren SO, Cott JM, Hall H.
The sedative effects of several different structural types of antidepressants were investigated in mice. Six different models of sedation were used and the results were averaged. The rank order of sedative potency was: amitriptyline greater than mianserin greater than maprotiline greater than imipramine greater than desipramine greater than clomipramine greater than alaproclate greater than zimelidine greater than norzimelidine. Sedative potency of the antidepressants was found to be significantly correlated with their affinity for four different brain amine receptors. The rank order of correlation of sedation with receptor affinity was: histamine (H1) greater than serotonergic greater than muscarinic greater than alpha 1-adrenergic. These findings appear to be associated with clinical side effects observed during treatment with antidepressants. While scant literature is available concerning specific anxiolytic effects of antidepressants, pharmacological evidence for the role of central 5-HT systems in the anxiolytic effect is plentiful. Our preliminary findings show a marked antagonism of isolation-induced aggression by low doses of the specific 5-HT uptake inhibitor, zimelidine, and the 5-HT releasing agent, p-chloramphetamine, thus supporting the hypothetical importance of 5-HT in the pharmacology of anxiolytic agents.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6111897&dopt=Abstract
Life Sci. 1983 Jul 11;33(2):181-8.
Functional supersensitivity of CNS alpha 1-adrenoceptors following chronic antidepressant treatment.
Menkes DB, Kehne JH, Gallager DW, Aghajanian GK, Davis M.
Chronic but not acute administration (21 days) of desipramine (10 mg/kg), amitriptyline (10 mg/kg) or iprindole (5 mg/kg) enhanced the stimulatory effect of the alpha 1-adrenergic agonist phenylephrine on the acoustic startle reflex when phenylephrine was infused into the subarachnoid space of the spinal cord. Comparable supersensitivity to phenylephrine also occurred 1 week after selective depletion of norepinephrine in the spinal cord via intrathecal administration of 6-hydroxydopamine. Behavioral supersensitivity to phenylephrine was associated with an increase in the number of 3H-prazosin binding sites following denervation but not following chronic antidepressant treatments. The results indicate that chronic antidepressant treatments may enhance functional alpha 1-adrenergic transmission through mechanisms different than those following denervation.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6306376&dopt=Abstract
Life Sci. 1983 Oct 24;33(17):1727-30.
Amitriptyline sensitization of a serotonin-mediated behavior depends on the passage of time and not repeated treatment.
Antelman SM, DeGiovanni LA, Kocan D, Perel JM, Chiodo LA.
Daily treatment for 10 days with either amitriptyline or the tricyclic muscle relaxant, cyclobenzaprine, increased the incidence of head-twitch behavior in response to 5-hydroxytryptophan (5-HTP) when this was examined two days later. Only one day of amitriptyline treatment followed by an 11-day hiatus before administration of 5-HTP also sensitized the head-twitch response whereas similar amitriptyline treatment followed by 5-HTP one hour later failed to do so. These data provide the first evidence for time-dependent sensitization of brain serotonin systems.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6605468&dopt=Abstract
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