139953-73-4
Chemical Structure
Cyclazosin
- CAS No.: 139953-73-4
- Formula:C23H27N5O4
- Molecular Weight:437.49
InChIKey: XBRXTUGRUXGBPX-DLBZAZTESA-N
SMILES: O=C(C1=CC=CO1)N2[C@]3([H])[C@](CCCC3)([H])N(C4=NC5=C(C=C(C(OC)=C5)OC)C(N)=N4)CC2
Biological Activity: Cyclazosin is an α1D-adrenergic receptor antagonist and a partial agonist of CXCR4/ACKR3. The pKi values of Cyclazosin for cloned human α1D, α1B and α1A adrenergic receptors are 9.28, 9.23 and 8.18, respectively. Cyclazosin induces β-arrestin recruitment in CXCR4 and ACKR3 with EC50 values of 16 μM and 10 μM, respectively, stimulates ERK1/2 phosphorylation, and induces receptor internalization. Cyclazosin potently inhibits CXCL12-induced chemotaxis of primary human aortic vascular smooth muscle cells. Cyclazosin alters MDMA-induced thermoregulatory responses in mice, converting monophasic hyperthermia to a biphasic pattern without affecting resting core body temperature. Cyclazosin can be used for diseases related to tumor metastasis, MDMA-induced hyperthermia and vasoconstriction[1][2][3][4][5][6].
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Cyclazosin | Cyclazosin is an α1D-adrenergic receptor antagonist and a partial agonist of CXCR4/ACKR3. The pKi values of Cyclazosin for cloned human α1D, α1B and α1A adrenergic receptors are 9.28, 9.23 and 8.18, respectively. Cyclazosin induces β-arrestin recruitment in CXCR4 and ACKR3 with EC50 values of 16 μM and 10 μM, respectively, stimulates ERK1/2 phosphorylation, and induces receptor internalization. Cyclazosin potently inhibits CXCL12-induced chemotaxis of primary human aortic vascular smooth muscle cells. Cyclazosin alters MDMA-induced thermoregulatory responses in mice, converting monophasic hyperthermia to a biphasic pattern without affecting resting core body temperature. Cyclazosin can be used for diseases related to tumor metastasis, MDMA-induced hyperthermia and vasoconstriction. | |||||||||||||||||||||
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References
- [1]. Giardinà D, et al. Receptor binding profile of cyclazosin, a new alpha 1B-adrenoceptor antagonist. Eur J Pharmacol. 1995 Dec 4;287(1):13-6. [Content Brief]
- [2]. Gao X, et al. Partial agonist activity of α1-adrenergic receptor antagonists for chemokine (C-X-C motif) receptor 4 and atypical chemokine receptor 3. PLoS One. 2018 Sep 24;13(9):e0204041. [Content Brief]
- [3]. Bexis S, et al. Role of alpha1-adrenoceptor subtypes in the effects of methylenedioxy methamphetamine (MDMA) on body temperature in the mouse. British journal of pharmacology. 2008 Feb;153(3):591-7. [Content Brief]
- [4]. Alsufyani HA, et al. Both α- and α-adrenoceptor subtypes are involved in contractions of rat spleen. Pharmacological reports : PR. 2021 Feb;73(1):255-260. [Content Brief]
- [5]. Proudman RGW, et al. The affinity and selectivity of α-adrenoceptor antagonists, antidepressants, and antipsychotics for the human α1A, α1B, and α1D-adrenoceptors. Pharmacology research & perspectives. 2020 Aug;8(4):e00602. [Content Brief]
- [6]. Errasti AE, et al. Human umbilical vein vasoconstriction induced by epinephrine acting on alpha1B-adrenoceptor subtype. American journal of obstetrics and gynecology. 2003 Nov;189(5):1472-80. [Content Brief]
