AHR-1709 is an experimental antipsychotic of the tryptamine family which was never marketed. It is a cyclized tryptamine, more specifically an analogue of pip-tryptamine.
Pharmacology Pharmacodynamics AHR-1709 shows high affinity for the serotonin 5-HT1A and 5-HT2A receptors (Ki = 27–44nM and 4.8nM, respectively) and for the dopamine D2 receptor (Ki = 81nM). It may act as a serotonin 5-HT1A receptor antagonist. The drug also shows high affinity for ketanserin-labeled serotonin 5-HT2A receptors (Ki = 9.33–12.6nM) and is a potent antagonist of these receptors (A2 = 24.6–120nM).
The drug produces antipsychotic-like effects in rodents, including reversal of hyperlocomotion but without induction of catalepsy, antagonism of stereotypy, or elevation of prolactin levels. AHR-1709 also produces antiemetic effects in rodents.
It is a derivative of the dopaminergic neurotoxin MPTP and is a weak dopamine reuptake inhibitor similarly but with 23-fold higher potency ( = 4,200nM and 95,200nM, respectively). However, unlike MPTP, AHR-1709 did not produce dopaminergic neurotoxicity in rodents.
Chemistry A number of derivatives of AHR-1709 have been described. An analogue of AHR-1709 with an elongated side chain is EMD-23448. AHR-1709 is also structurally similar to pertines like oxypertine.
History AHR-1709 was first described in the scientific literature by 1978.
See also Cyclized tryptamine pip-Tryptamine
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