guanadrel

Trade name: hylorel

Small moleculeapproved

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

Phase 1
0
Phase 2
0
Phase 3
0
Phase 4
0

Timeline

1980s

  1. Dec 29, 1982

    Pharmacia & Upjohn — Earliest FDA Approval

  2. Dec 29, 1982

    Pharmacia & Upjohn — NDA Organization

  3. Dec 29, 1982

    Pharmacia & Upjohn — NDA Secondary Org

Indications

Mechanism of action

Approval history

  • approvedDec 29, 1982

Chemistry & pharmacology

Loading structure…

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

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)

OrganizationOrg typeRelationshipDate
Pharmacia & UpjohnFor profitNDADec 29, 1982
Pharmacia & UpjohnFor profitNDA2Dec 29, 1982