Zimelidine 

Zimelidine is an orally active selective serotonin reuptake inhibitor. Zimelidine competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine is used for the study of depressive disorders and analgesic tolerance^[1][2][3][4].

Zimelidine potently and selectively inhibits serotonin uptake in rat hypothalamic synaptosomes, mouse cerebral cortical slices, and mouse striatal slices, with IC₅₀ values of 0.33 μmol/L, 3.3 μmol/L, and 9.1 μmol/L respectively, and shows far weaker inhibition of noradrenaline and dopamine uptake^[2].
Zimelidine inhibits serotonin uptake into human platelets in vitro with an IC₅₀ of 2.6 μmol/L^[2].
Zimelidine has low affinity for postsynaptic serotonin, α-noradrenergic, β-noradrenergic, and dopamine receptors in vitro^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Zimelidine (5 mg/kg; i.p.; daily; 14 days) enhances the efficacy of 5-HT neurotransmission in the hippocampus via a presynaptic mechanism without altering postsynaptic neuronal responsiveness to direct 5-HT or GABA application^[1].
Zimelidine (5 mg/kg; i.p.; daily; 2-14 days) causes an initial reduction in 5-HT neuron activity followed by gradual restoration of normal activity and desensitization of 5-HT autoreceptors after 14 days of treatment^[1].
Zimelidine (i.p.) inhibits H75/12- and PCA-induced 5-HT depletion in rat brain with ED₅₀ values of 4 mg/kg (H75/12) and 1.5 mg/kg (PCA)^[1].

Zimelidine (i.p.; p.o.) potentiates 5-HTP-induced head twitches in mice, with an ED₅₀ of 3.2 μmol/kg (p.o.) and 8.6 μmol/kg (i.p.)^[2].
Zimelidine reduces serotonin's inhibitory effects on visual cortex responses in rabbits following chronic treatment^[2].
Zimelidine (15 mg/kg; i.p.; single dose) significantly attenuates the development of induced antinociceptive tolerance in rats^[3].
Zimelidine (0.2-20 nmol/100 nL; bilateral medial amygdaloid nucleus microinjection; single dose) administered via bilateral MeA microinjection produces a dose-dependent hypophagic effect in fasted male Wistar rats^[4].
Zimelidine (2 nmol/100 nL; bilateral medial amygdaloid nucleus microinjection; single dose; administered 15 minutes after SB-242084 (HY-13409) or vehicle pretreatment) (2 nmol via bilateral MeA microinjection) in fasted male Wistar rats is mediated by MeA 5-HT₂C receptors^[4].
Zimelidine (20 mg/kg; intraperitoneal injection; single dose; administered 15 minutes after SB-242084 or vehicle pretreatment) in fasted male Wistar rats is mediated by MeA 5-HT₂C receptors^[4].
Zimelidine (2 nmol/100 nL; bilateral medial amygdaloid nucleus microinjection; single dose; administered 15 minutes after WAY-100635 (HY-10349) or vehicle pretreatment) (2 nmol via bilateral MeA microinjection) in fasted male Wistar rats is not mediated by MeA 5-HT₁A receptors^[4].
Zimelidine (2 nmol/100 nL; bilateral medial amygdaloid nucleus microinjection; single dose; administered 15 minutes after SB-216641 or vehicle pretreatment) (2 nmol via bilateral MeA microinjection) in fasted male Wistar rats is not mediated by MeA 5-HT₁B receptors^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

317.22

C₁₆H₁₇BrN₂

56775-88-3

CN(C/C=C(C1=CC=CN=C1)/C2=CC=C(C=C2)Br)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Blier P, et al. Electrophysiological investigations on the effect of repeated zimelidine administration on serotonergic neurotransmission in the rat. J Neurosci. 1983 Jun;3(6):1270-8.  [Content Brief]

  [2]. Heel RC, et al. Zimelidine: a review of its pharmacological properties and therapeutic efficacy in depressive illness. Drugs. 1982 Sep;24(3):169-206.  [Content Brief]

  [3]. Ozdemir E, et al. Zimelidine attenuates the development of tolerance to morphine-induced antinociception. Indian J Pharmacol. 2012 Mar;44(2):215-8.  [Content Brief]

  [4]. Scopinho AA, et al. Medial amygdaloid nucleus 5-HT₂c receptors are involved in the hypophagic effect caused by zimelidine in rats. Neuropharmacology. 2012 Aug;63(2):301-9.  [Content Brief]