5-Carboxamidotryptamine (5-CT) is a
tryptamine
Tryptamine is an indolamine metabolite of the essential amino acid, tryptophan. The chemical structure is defined by an indole ─ a fused benzene and pyrrole ring, and a 2-aminoethyl group at the second carbon (third aromatic atom, with the f ...
derivative
In mathematics, the derivative of a function of a real variable measures the sensitivity to change of the function value (output value) with respect to a change in its argument (input value). Derivatives are a fundamental tool of calculus. ...
closely related to the
neurotransmitter serotonin.
5-CT acts as a
non-selective,
high-affinity full agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the a ...
at the
5-HT1A,
5-HT1B,
5-HT1D,
5-HT5A, and
5-HT7 receptors, as well as at the
5-HT2,
5-HT3,
5-HT6 receptors with lower affinity.
It has negligible affinity for the
5-HT1E and
5-HT1F receptors.
5-CT binds most strongly to the 5-HT
1A receptor and it was once thought to be selective for this site. Recently, a close derivative of 5-CT,
AH-494
AH-494 is a potent and selective, water-soluble full agonist at the 5HT7 serotonin receptor. It is a close derivative of the known chemical probe 5-Carboxamidotryptamine, as well as of the more lipophilic indole-imidazoles: AGH-107 and AGH-192 ...
has been shown to function as an agonist of
5-HT7, although being more selective over
5-HT1A
The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptor, or 5-HT receptor, that binds serotonin, also known as 5-HT, a neurotransmitter. 5-HT1A is expressed in the brain, spleen, and neonatal kidney. It is a G protein-c ...
.
Structural study indicated residue Ser5x43 might play critical roles in the selectivity of 5-CT across the serotonin receptor family.
See also
*
2-Methyl-5-hydroxytryptamine
2-Methyl-5-hydroxytryptamine (2-Methylserotonin, 2-Methyl-5-HT) is a tryptamine derivative closely related to the neurotransmitter serotonin which acts as a moderately selective full agonist at the 5-HT3 receptor.
See also
* 5-Carboxamidotry ...
*
5-Benzyloxytryptamine
*
5-Methoxytryptamine
*
α-Methyl-5-hydroxytryptamine
*
Frovatriptan
Frovatriptan, sold under the brand name Frova, is a triptan drug developed by Vernalis for the treatment of migraine headaches and for short term prevention of menstrual migraine. The product is licensed to Endo Pharmaceuticals in North Americ ...
*
AH-494
AH-494 is a potent and selective, water-soluble full agonist at the 5HT7 serotonin receptor. It is a close derivative of the known chemical probe 5-Carboxamidotryptamine, as well as of the more lipophilic indole-imidazoles: AGH-107 and AGH-192 ...
*
Acetryptine
Acetryptine (INN) (developmental code name W-2965-A), also known as 5-acetyltryptamine (5-AT), is a drug described as an antihypertensive agent which was never marketed. Structurally, acetryptine is a substituted tryptamine, and is closely relat ...
*
Sumatriptan
References
Serotonin receptor agonists
Tryptamines
Carboxamides
Serotonin releasing agents
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