Ketanserin (Vulketan Gel) is specific 5-HT2A serotonin receptor antagonist with a Ki of 2.5 nM for rat and human 5-HT2A. Ketanserin (Vulketan Gel) is a compound with affinity for multiple G protein-coupled receptors. Ketanserin ( Vulketan Gel) inhibits rat and human 5-HT2C with Ki of 50 and100 nM, respectively and has higher affinity binding for alpha-1 adrenergic (Ki = ~ 40 nM) and Histamine H1 (Ki = 2 nM). Ketanserin (Vulketan Gel) can also be used to discriminate between 5-HT1D and 5-HT1B receptor subtypes. Ketanserin (Vulketan Gel) has antihypertensive properties. Ketanserin (Vulketan Gel) also reduces platelet aggregation produced by serotonin. Ketanserin also has high affinity for alpha-1 adrenergic receptors, and very high affinity for histamine H1 receptors. Ketanserin (Vulketan Gel) was shown to reduce the severity and frequency of the vasospasm in Raynaud’s phenomenon.
| Molecular Weight | 395.43 |
| Formula | C22H22FN3O3 |
| CAS Number | 74050-98-9 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] J Pope, et al. Ketanserin for Raynaud's phenomenon in progressive systemic sclerosis
[3] A Breckenridge. Ageing, serotonin and ketanserin
[5] B Persson, et al. Clinical pharmacokinetics of ketanserin
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