Selective serotonin receptor agonists

Sumatriptan (Imitrex), subcutaneous, a selective serotonin receptor agonist. 

An opioid analgesic should be given only if ergot alkaloids or selective serotonin receptor agonist medications (migraine-specific medications) are not effective in treating the pain. 

The patient reports mild to moderate pain. A migraine-specific drug, such as a selective serotonin receptor agonist,... 

Sumatriptan (Imitrex) [Antimigraine Agent/Selective 5-HTi Receptor Agonist] Uses Rx acute migraine Action Vascular serotonin receptor agonist Dose Adults. SQ 6 mg SQ as a single dose PRN repeat PRN in 1 h to a max of 12 mg/24 h PO 25 mg, repeat in 2 h, PRN, 100 mg/d max PO dose max 300 mg/d Nasal spray 1 spray into 1 nostril, repeat in 2 h to 40 mg/24 h... 

Mechanism of Action A serotonin receptor agonist that binds selectively to vascular receptors, producing a vasoconstrictive effect on cranial blood vessels. Therapeutic Effect Produces relief of migraine headache. 

BMY 7378, initially described as a serotonin receptor agonist with selectivity for the 5-HT,a subtype [25, 26], has recently been suggested to be selective for the oi,-AR subtype as well [11]. We tested this compound for its selectivity at the expressed human aj-AR clones. In fH]tamsuIosin binding inhibition curves, BMY 7378 potently inhibited binding at the a, subtype with a ten-fold selectivity over the ,b-AR subtype and one hundred-fold selectivity over the oi,-AR subtype (see Fig. 3). 

Beginning in the 1960s, ben2odia2epiae anxiolytics and hypnotics rapidly became the standard prescription dmg treatment. In the 1980s, buspkone [36505-84-7] (3), which acts as a partial agonist at the serotonin [50-67-9] (5-hydroxytryptamine, 5-HT) type lA receptor, was approved as treatment for generali2ed anxiety. More recently, selective serotonin reuptake inhibitors (SSRIs) have been approved for therapy of panic disorder and obsessive—compulsive behavior. 

The enantiomerically pure 3-arylglutaric ester are precursors for the synthesis of (—)-paroxetine [10], a selective serotonin reuptake inhibitor used in the treatment of depression, obsessive compulsive disorder, and panic, and (i )-Baclofen [11], a GABAb receptor agonist, which is used cHnically in the treatment of spasticity (Chart 5.1). 

Titeler. M. Lyon, R.A. Davis, K.A. and Glennon, R.A. Selectivity of serotonergic drugs for multiple brain serotonin receptors The role of H-DOB, a 5-HT2 agonist radioligand. Biochem Pharmacol 36 3265-3271,... 

Opioids, benzodiazepines, barbiturates, corticosteroids, dopamine agonists (e.g., amantadine, bromocriptine, levodopa, pergolide, pramipexole, ropinirole), H2-receptor antagonists, anticholinergics (e.g., diphenhydramine, trihexylphenidyl), P-adrenergic blockers, clonidine, methyldopa, carbamazepine, phenytoin, baclofen, cyclobenzaprine, lithium, antidepressants (e.g., tricyclic antidepressants, selective serotonin reuptake inhibitors), and interleukin-2... 

FDA, Combined Use of 5-Hydroxytryptamine Receptor Agonists (Triptans), Selective Serotonin Reuptake Inhibitors (SSRIs) or Selective Serotonin/Norepinephrine Reuptake Inhibitors (SNRIs) May Result in Life-Threatening Serotonin Syndrome , FDA Public Health Advisory (2006) http //www.fda.gov/Cder/Drug/advisory/ S SRI S S200607.htm... 

Monti, J. M. Jantos, H. (2006b). Effects of the serotonin 5-HT2a/2c receptor agonist DOI and of the selective 5-HT2a or 5-HT2c receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat. Eur. J. Pharmacol. 553, 163-70. 

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