1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor


Cat. No.: HY-103102
Handling Instructions

TCB2 is an agonist of serotonin 5-HT2A receptor.

For research use only. We do not sell to patients.

TCB2 Chemical Structure

TCB2 Chemical Structure

CAS No. : 912342-28-0

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


TCB2 is an agonist of serotonin 5-HT2A receptor.

IC50 & Target

5-HT2A Receptor


In Vitro

The selective 5-HT2A agonist TCB2 at 30 nM produces a marked shift to the right in the competition curve obtained with the 5-HT1A receptor agonist ipsapirone from [3H]-8-OHDPAT binding sites in both areas of the brain. A significant increase in the mean Ki value is obtained with TCB2, demonstrating a reduction in the affinity of the high-affinity 5-HT1A agonist binding sites by the 5-HT2A agonist in both regions. In the case of hippocampus, there are also indications for antagonistic effects of ketanserin[2].

In Vivo

In an initial dose-response study, TCB2 (0.5, 1.0, and 2.5 mg/kg) and DOI (0.5, 1.0, 2.5, and 5.0 mg/kg) induce head twitches in C57BL/6J mice in a dose-dependent manner compared to vehicle. Head twitches induced by TCB2 and DOI are similar across the doses, with the exception that at the highest dose (5.0 mg/kg), TCB2 induces half as many head twitches as does DOI (p=0.021). Confirming 5-HT2A mediation of the head twitch response, in two separate studies, pretreatment with the selective 5-HT2A antagonist MDL 11,939 (1.0 mg/kg) block head twitches induced by DOI (2.5 mg/kg) and by TCB2 (2.5 mg/kg; p<0.0001). Compared to vehicle, corticosterone levels are increased following TCB2 (5.0 mg/kg, p=0.01; 10.0, p=0.012; with a trend following 2.5 mg/kg, p=0.079) and DOI (10.0 mg/kg, p=0.035)[1].

Solvent & Solubility
In Vitro: 

10 mM in H2O

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8325 mL 14.1623 mL 28.3246 mL
5 mM 0.5665 mL 2.8325 mL 5.6649 mL
10 mM 0.2832 mL 1.4162 mL 2.8325 mL
*Please refer to the solubility information to select the appropriate solvent.
Animal Administration

Male C57BL/6J mice and SERT+/+ (+/−, −/−) mice (25-30 g) are used. TCB2 is dissolved in distilled water, MDL 11,939 is dissolved in a few drops of acetic acid and prepared in distilled water, and DOI is dissolved in saline. All drugs and their vehicles are administered via intraperitoneal injection at a volume of 10 ml/kg. Following 15 min of habituation in a plexiglass container, mice are administered the test drug. Head twitches were recorded for five 1-min periods over a 30-min period; the scores from the five 1-min periods are summed together. In two separate experiments, mice are pretreated with the selective 5-HT2A antagonist MDL 11,939 (1.0 mg/kg) or its vehicle 30 min prior to administration of DOI or TCB2 (2.5 mg/kg). Finally, head twitches are assessed in SERT+/+ (+/−, −/−) mice administered TCB2. C57BL/6J mice are injected with vehicle, TCB2 (1.0 or 2.5 mg/kg) or DOI (1.0 or 2.5 mg/kg). Following administration of vehicle, TCB2 (1.0, 2.5, or 5.0 mg/kg) or DOI (1.0, 2.5, or 5.0 mg/kg), mice are placed in the test cage. In a final feeding study, mice are pretreated with vehicle or MDL 11,939 (1.0 mg/kg) followed 30 min later by an intermediate dose of TCB2 (3.75 mg/kg)[1].

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

Molecular Weight









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


Room temperature in continental US; may vary elsewhere

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Cat. No.: HY-103102