SB-699551 is a drug which was the first compound developed to act as a selective
antagonist for the
serotonin receptor
5-HT5A, with selectivity of around 100x over other serotonin receptor subtypes.[1] Multiple therapeutic roles have been suggested for 5-HT5A ligands due to the presence of this receptor in several areas of the brain, but research is still at an early stage,[2] In animal studies, SB-699551 was found to block cue-mediated responding to
LSD, again suggesting an antipsychotic type of activity.[3] It also reduces the viability of certain types of
cancer cells in vitro, suggesting the 5-HT5A receptor as a possible target for novel chemotherapy drugs.[4][5]
References
^Thomas DR, Soffin EM, Roberts C, Kew JN, de la Flor RM, Dawson LA, et al. (September 2006). "SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain". Neuropharmacology. 51 (3): 566–577.
doi:
10.1016/j.neuropharm.2006.04.019.
PMID16846620.
S2CID543423.
^Nikiforuk A, Hołuj M, Kos T, Popik P (June 2016). "The effects of a 5-HT5A receptor antagonist in a ketamine-based rat model of cognitive dysfunction and the negative symptoms of schizophrenia". Neuropharmacology. 105: 351–360.
doi:
10.1016/j.neuropharm.2016.01.035.
PMID26826431.
S2CID31557477.
^Popik P, Krawczyk M, Kuziak A, Bugno R, Hogendorf A, Staroń J, Nikiforuk A (November 2019). "Serotonin type 5A receptor antagonists inhibit D-lysergic acid diethylamide discriminatory cue in rats". Journal of Psychopharmacology. 33 (11): 1447–1455.
doi:
10.1177/0269881119867603.
PMID31452444.
S2CID201733534.
SB-699551 is a drug which was the first compound developed to act as a selective
antagonist for the
serotonin receptor
5-HT5A, with selectivity of around 100x over other serotonin receptor subtypes.[1] Multiple therapeutic roles have been suggested for 5-HT5A ligands due to the presence of this receptor in several areas of the brain, but research is still at an early stage,[2] In animal studies, SB-699551 was found to block cue-mediated responding to
LSD, again suggesting an antipsychotic type of activity.[3] It also reduces the viability of certain types of
cancer cells in vitro, suggesting the 5-HT5A receptor as a possible target for novel chemotherapy drugs.[4][5]
References
^Thomas DR, Soffin EM, Roberts C, Kew JN, de la Flor RM, Dawson LA, et al. (September 2006). "SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain". Neuropharmacology. 51 (3): 566–577.
doi:
10.1016/j.neuropharm.2006.04.019.
PMID16846620.
S2CID543423.
^Nikiforuk A, Hołuj M, Kos T, Popik P (June 2016). "The effects of a 5-HT5A receptor antagonist in a ketamine-based rat model of cognitive dysfunction and the negative symptoms of schizophrenia". Neuropharmacology. 105: 351–360.
doi:
10.1016/j.neuropharm.2016.01.035.
PMID26826431.
S2CID31557477.
^Popik P, Krawczyk M, Kuziak A, Bugno R, Hogendorf A, Staroń J, Nikiforuk A (November 2019). "Serotonin type 5A receptor antagonists inhibit D-lysergic acid diethylamide discriminatory cue in rats". Journal of Psychopharmacology. 33 (11): 1447–1455.
doi:
10.1177/0269881119867603.
PMID31452444.
S2CID201733534.