5-CT acts as a
non-selective,
high-affinityfull agonist 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.[1][2][3] It has negligible affinity for the
5-HT1E and
5-HT1F receptors.[4] 5-CT binds most strongly to the 5-HT1A receptor and it was once thought to be selective for this site.[5][6] Recently, a close derivative of 5-CT,
AH-494 has been shown to function as an agonist of
5-HT7, although being more selective over
5-HT1A.[7] Structural study indicated residue Ser5x43 might play critical roles in the selectivity of 5-CT across the serotonin receptor family.[8]
^Yamada J, Sugimoto Y, Noma T, Yoshikawa T (October 1998). "Effects of the non-selective 5-HT receptor agonist, 5-carboxamidotryptamine, on plasma glucose levels in rats". European Journal of Pharmacology. 359 (1): 81–86.
doi:
10.1016/S0014-2999(98)00617-7.
PMID9831297.
^Glennon RA, Dukat M, Westkaemper RB (2000-01-01).
"Serotonin Receptor Subtypes and Ligands". American College of Neurophyscopharmacology.
Archived from the original on 21 April 2008. Retrieved 2008-04-11.
^Stanton JA, Middlemiss DN, Beer MS (February 1996). "Autoradiographic localization of 5-CT-insensitive 5-HT1-like recognition sites in guinea pig and rat brain". Neuropharmacology. 35 (2): 223–229.
doi:
10.1016/0028-3908(95)00178-6.
PMID8734492.
S2CID27188133.
^Saxena PR, Lawang A (October 1985). "A comparison of cardiovascular and smooth muscle effects of 5-hydroxytryptamine and 5-carboxamidotryptamine, a selective agonist of 5-HT1 receptors". Archives Internationales de Pharmacodynamie et de Therapie. 277 (2): 235–252.
PMID2933009.
5-CT acts as a
non-selective,
high-affinityfull agonist 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.[1][2][3] It has negligible affinity for the
5-HT1E and
5-HT1F receptors.[4] 5-CT binds most strongly to the 5-HT1A receptor and it was once thought to be selective for this site.[5][6] Recently, a close derivative of 5-CT,
AH-494 has been shown to function as an agonist of
5-HT7, although being more selective over
5-HT1A.[7] Structural study indicated residue Ser5x43 might play critical roles in the selectivity of 5-CT across the serotonin receptor family.[8]
^Yamada J, Sugimoto Y, Noma T, Yoshikawa T (October 1998). "Effects of the non-selective 5-HT receptor agonist, 5-carboxamidotryptamine, on plasma glucose levels in rats". European Journal of Pharmacology. 359 (1): 81–86.
doi:
10.1016/S0014-2999(98)00617-7.
PMID9831297.
^Glennon RA, Dukat M, Westkaemper RB (2000-01-01).
"Serotonin Receptor Subtypes and Ligands". American College of Neurophyscopharmacology.
Archived from the original on 21 April 2008. Retrieved 2008-04-11.
^Stanton JA, Middlemiss DN, Beer MS (February 1996). "Autoradiographic localization of 5-CT-insensitive 5-HT1-like recognition sites in guinea pig and rat brain". Neuropharmacology. 35 (2): 223–229.
doi:
10.1016/0028-3908(95)00178-6.
PMID8734492.
S2CID27188133.
^Saxena PR, Lawang A (October 1985). "A comparison of cardiovascular and smooth muscle effects of 5-hydroxytryptamine and 5-carboxamidotryptamine, a selective agonist of 5-HT1 receptors". Archives Internationales de Pharmacodynamie et de Therapie. 277 (2): 235–252.
PMID2933009.