guanadrel
Trade name: hylorel
Approved
Dec 29, 1982
Guanadrel is a postganglionic adrenergic blocking agent. Uptake of guanadrel and storage in sympathetic neurons occurs via the norepinephrine pump or transporter. Guanadrel slowly displaces norepinephrine from its storage in nerve endings and thereby blocks the release of norepinephrine normally produced by nerve stimulation. The reduction in neurotransmitter release in response to sympathetic nerve stimulation, as a result of catecholamine depletion, leads to reduced arteriolar vasoconstriction, especially the reflex increase in sympathetic tone that occurs with a change in position. Guanadrel is used to treat and control hypertension. — NCATS
Clinical trial activity
0 trials · 0 clinical orgs · 1 marketing orgs
Timeline
1980s
- Dec 29, 1982
Pharmacia & Upjohn — Earliest FDA Approval
- Dec 29, 1982
Pharmacia & Upjohn — NDA Organization
- Dec 29, 1982
Pharmacia & Upjohn — NDA Secondary Org
Indications
Approved for
Mechanism of action
- Norepinephrine transporterSUBSTRATE
SLC6A2 substrate
Taken up by transporter and displaces NE from vesicles
Approval history
- approvedDec 29, 1982
Chemistry & pharmacology
SMILES
N=C(N)NCC1COC2(CCCCC2)O1.N=C(N)NCC1COC2(CCCCC2)O1.O=S(=O)(O)O- Mol. weight
- 524.64 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Discontinued
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL3184143 ↗
- WikipediaGuanadrel ↗
- NCATS765C9332T4 ↗
- ChEMBLCHEMBL1200594 ↗
- ChEMBLCHEMBL1037 ↗
Also known as
- (1,4-dioxaspiro(4.5)dec-2-ylmethyl)guanidine
- cl-1388r
- cl-1388r
- guanadrel
- guanadrel
- guanadrel
- guanadrel
- guanadrel
- guanadrel
- guanadrel
- guanadrel
- guanadrel
- guanadrel sulfate
- guanadrel sulfate
- guanadrel sulfate
- guanadrel sulfate
- guanadrel sulfate
- guanadrelum
- guanadrelum
- hylorel
- hylorel
- hylorel
- hylorel
- hylorel
- hylorel
- hylorel
- u-28288d
- u-28288d
Organizations
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Pharmacia & Upjohn | For profit | NDA | Dec 29, 1982 |
| Pharmacia & Upjohn | For profit | NDA2 | Dec 29, 1982 |