8-hydroxy DPAT (hydrobromide)

8-Hydroxy DPAT (8-OH-DPAT) is an agonist of serotonin (5-HT) receptor subtype 5-HT_1A (EC₅₀ = 12 nM in rat hippocampal membranes).¹ It mimics the effect of serotonin (Item No. 14332) on reducing excitatory post-synaptic potentials (EPSPs) in the entorhinal cortex layers II and III when used at concentrations of 10 and 50 µM.² In rhesus monkeys, it enhances the behavioral effects of Δ⁹-tetrahydrocannabinol (Δ⁹-THC; Item Nos. 12068 | ISO60157) in a discriminant stimulus-shock test when administered at a dose of 0.178 mg/kg.³ In mice, 8-OH-DPAT reduces the number of attack bites when administered directly to the dorsal raphe nucleus in a baclofen-induced model of aggressiveness and impairs contextual fear when administered prior to training at a dose of 0.5 mg/kg.^4,5 It also reduces the incidence of apnea and improves respiratory regularity in a methyl-CpG-binding protein 2-deficient mouse model of Rett syndrome when administered at a dose of 50 µg/kg.⁶ In a rat model of diabetes, 8-OH-DPAT enhances bradycardia in response to vagal electrical stimulation.⁷

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1. Meller, E., Li, H., Carr, K.D., et al. 5-hydroxytryptamine1A receptor-stimulated [35S]GTPγS binding in rat brain: Absence of regional differences in coupling efficiency. J. Pharmacol. Exp. Ther. 292(2), 684-691 (2000).

2. Schmitz, D.A., Gloveli, T., Empson, R.M., et al. Serotonin reduces synaptic excitation in the superficial medial entorhinal cortex of the rat via a presynaptic mechanism. J. Physiol. 508(Pt 1), 119-129 (1998).

3. McMahon, L.R. Enhanced discriminative stimulus effects of Δ9-THC in the presence of cannabidiol and 8-OH-DPAT in rhesus monkeys. Drug Alcohol Depend. 165, 87-93 (2016).

4. Takahashi, A., Shimamoto, A., Boyson, C.O., et al. GABAB receptor modulation of serotonin neurons in the dorsal raphé nucleus and escalation of aggression in mice. J. Neurosci. 30(35), 11771-11780 (2010).

5. Stiedl, O., Misane, I., Spiess, J., et al. Involvement of the 5-HT_1A receptors in classical fear conditioning in C57BL/6J mice. J. Neurosci. 20922), 8515-8527 (2000).

6. Abdala, A.P.L., Dutschmann, M., Bissonnette, J.M., et al. Correction of respiratory disorders in a mouse model of Rett syndrome. Proc. Natl. Acad. Sci. USA 107(42), 18208-18213 (2010).

7. Restrepo, B., Martín, M.L., San Román, L., et al. Peripheral 5-HT_1A and 5-HT₇ serotonergic receptors modulate parasympathetic neurotransmission in long-term diabetic rats. Exp. Diabetes Res. 686734 (2010).