If someone wanted to slice and dice meds for the mood and anxiety disorders, they’d have to understand 5-HT1A receptor partial agonists. That may call for a subject change. But they’re really important to know about, so we’re going there…
Activation of 5-HT1A receptors decreases blood pressure, heart rate, and body temperature…
But before we go anywhere, it’s important to point out that 5-HT (5-hydroxytryptamine) is the chemical designation for the neurotransmitter serotonin. Of course, its role in the mood and anxiety disorders is huge.
Receptors & Agonists
For the purposes of our discussion, receptor refers to a neurotransmitter receptor. You’ll see one on the receiving neuron at the bottom of the image.
Receptors are present on both postsynaptic and presynaptic neurons – the former being used to receive neurotransmitters, the latter for the purpose of preventing further release of a given neurotransmitter.
Each neurotransmitter has its own receptors. And it’s all about efficient electrical signaling.
An agonist is any chemical that binds to a receptor and triggers a response by that cell. A chemical with the opposite action is known as an antagonist.
Oh, partial agonist. Let’s not sweat that detail this go-round.
A 5-HT1A receptor is a subtype of a 5-HT (serotonin) receptor. In fact, it’s the most widespread of the 5-HT receptors.
Among other locations, 5-HT1A receptors are found in high densities in the cerebral cortex, hippocampus, and amygdala – all heavily involved in the mood and anxiety disorders.
Activation of 5-HT1A receptors decreases blood pressure, heart rate, and body temperature. Other activation effects include decreased aggression or an increase in calm behavior, increased sociability, inhibition of addictive behavior, and the facilitation of sexual behavior and arousal.
On the other side of the coin, activation of 5-HT1A receptors generates increased impulsivity, inhibition of penile erection, and the impairment of cognition, learning, and memory.
5-HT1A Receptor Partial Agonists
So, let’s put the pieces together. You may already be familiar with 5-HT1A receptor partial agonists and not even know it. How ’bout these…
aripiprazole (Abilify), buspirone (BuSpar), clozapine (Clozaril), nefazodone (Serzone), trazodone (Desyrel), vilazodone (Viibryd), ziprasidone (Geodon), LSD, psilocybin, yohimbine
5-HT1A receptor partial agonists have traditionally been used in the treatment of mood and anxiety woes. For instance, buspirone (BuSpar) has been a popular anxiety med for a long time.
You’ll notice two atypical antipsychotics (Abilify and Geodon) in our list of 5-HT1A receptor partial agonists. Don’t know about you, but I’ve seen advertisements for Abilify as an augmentation agent for antidepressants for several years now.
Heavily involved here is overcoming a characteristic of serotonin-impacting antidepressants (like the SSRIs). It’s called therapeutic lag. Simply, it can take some time for them to work.
So, an antidepressant regimen that can somehow pick-up 5-HT1A receptor partial agonistic properties brings faster relief and greater overall efficacy.
That’ll Do It
Alrighty, then. A nice thumbnail on 5-HT1A receptor partial agonists. The info may come off like so much bio-babble, but it’s really important to have in your back pocket. I mean, why wouldn’t you want to know the action of a med you’re counting on – and paid for?
Be sure to check-out all of the Chipur articles. Just hit the titles.